pgp4, an atp binding cassette p-glycoprotein, catalyzes ...pgp4, an atp binding cassette...

19
PGP4, an ATP Binding Cassette P-Glycoprotein, Catalyzes Auxin Transport in Arabidopsis thaliana Roots W Kazuyoshi Terasaka, a,1 Joshua J. Blakeslee, b,1 Boosaree Titapiwatanakun, b,1 Wendy A. Peer, b Anindita Bandyopadhyay, b Srinivas N. Makam, b Ok Ran Lee, b Elizabeth L. Richards, b Angus S. Murphy, b,2 Fumihiko Sato, a and Kazufumi Yazaki c a Laboratory of Molecular and Cellular Biology of Totipotency, Division of Integrated Life Science, Graduate School of Biostudies, Kyoto University, Kitashirakawa, Kyoto 606-8502, Japan b Department of Horticulture, Purdue University, West Lafayette, Indiana 47907-2010 c Laboratory of Plant Gene Expression, Research Institute for Sustainable Humanosphere, Kyoto University, Gokasho Uji 611-0011, Japan Members of the ABC (for ATP binding cassette) superfamily of integral membrane transporters function in cellular detoxification, cell-to-cell signaling, and channel regulation. More recently, members of the multidrug resistance P-glycoprotein (MDR/PGP) subfamily of ABC transporters have been shown to function in the transport of the phytohormone auxin in both monocots and dicots. Here, we report that the Arabidopsis thaliana MDR/PGP PGP4 functions in the basipetal redirection of auxin from the root tip. Reporter gene studies showed that PGP4 was strongly expressed in root cap and epidermal cells. PGP4 exhibits apolar plasma membrane localization in the root cap and polar localization in tissues above. Root gravitropic bending and elongation as well as lateral root formation were reduced in pgp4 mutants compared with the wild type. pgp4 exhibited reduced basipetal auxin transport in roots and a small decrease in shoot-to-root transport consistent with a partial loss of the redirective auxin sink in the root. Seedlings overexpressing PGP4 exhibited increased shoot-to-root auxin transport. Heterologous expression of PGP4 in mammalian cells resulted in 1-N-naphthylthalamic acid–reversible net uptake of [ 3 H]indole-3-acetic acid. These results indicate that PGP4 functions primarily in the uptake of redirected or newly synthesized auxin in epidermal root cells. INTRODUCTION Members of the ATP binding cassette (ABC) transporter super- family have been identified in all prokaryotic and eukaryotic or- ganisms (Henikoff et al., 1997). Although ABC transporters are often associated with the export of cytotoxic compounds (Gottesman and Pastan, 1993), they also function in mating hormone trans- port (Ketchum et al., 2001), ATP/ADP sensing (Bryan and Aguilar- Bryan, 1999), channel regulation (Anderson et al., 1991), and iron homeostasis (Kushnir et al., 2001). ABC transporters have also been shown to mediate the cellular uptake of urea (Beckers et al., 2004), iron (Brown et al., 2002; Danese et al., 2004), small peptides (Lamarque et al., 2004), choline (Dupont et al., 2004), and bilirubin (Ieiri et al., 2004). In contrast with other organisms, a broad proliferation of ABC transporters has occurred in plants (Sanchez-Fernandez et al., 2001; Martinoia et al., 2002; Jasinski et al., 2003; Garcia et al., 2004). Members of the multidrug resistance–associated protein (MRP) subfamily involved in the vacuolar sequestration of toxins or xenobiotics are the best characterized (Martinoia et al., 1993; Rea et al., 1998; Rea, 1999; Theodoulou, 2000). MRP1, MRP2, and MRP3 transport glutathione conjugates of endogenous and arti- ficial substrates into vacuoles (Lu et al., 1997, 1998; Tommasini et al., 1998), and MRP4 and MRP5 have been implicated in the complex regulation of stomatal aperture and guard cell ion flux (Gaedeke et al., 2001; Klein et al., 2003, 2004). Members of the pleiotropic drug resistance protein (PDR) subfamily, such as PDR1 from Nicotiana plumbaginifolia (Jasinski et al., 2001; Stukkens et al., 2005) and TURION2 from Spirodela polyrrhiza (van den Brule et al., 2002), export antifungal diterpene defense compounds to the leaf surface, and a half-size ABC protein, ECERIFERUM5, is responsible for wax export to the plant cuticle (Pighin et al., 2004). Although first identified in an unsuccessful attempt to enhance herbicide resistance (Sidler et al., 1998), the majority of plant multidrug resistance P-glycoproteins (MDR/PGPs; hereafter re- ferred to as PGPs) characterized to date have been implicated in the transport of the phytohormone auxin: PGP1 and PGP19 were identified as the principal Arabidopsis thaliana plasma mem- brane (PM) proteins binding the auxin efflux inhibitor 1-N- naphthylthalamic acid (NPA) with high affinity (Murphy and Taiz, 1999a, 1999b; Noh et al., 2001; Murphy et al., 2002). Loss of PGP19 and PGP1 function results in reduced auxin transport and growth defects of varying severity in Arabidopsis (pgp1, pgp19/mdr1), maize (Zea mays; brachytic2), and sorghum 1 These authors contributed equally to this work. 2 To whom correspondence should be addressed. E-mail murphy@ purdue.edu; fax 765-494-0391. The authors responsible for distribution of materials integral to the findings presented in this article in accordance with the policy described in the Instructions for Authors (www.plantcell.org) are: Angus S. Murphy ([email protected]) and Kazufumi Yazaki ([email protected]). W Online version contains Web-only data. Article, publication date, and citation information can be found at www.plantcell.org/cgi/doi/10.1105/tpc.105.035816. The Plant Cell, Vol. 17, 2922–2939, November 2005, www.plantcell.org ª 2005 American Society of Plant Biologists

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Page 1: PGP4, an ATP Binding Cassette P-Glycoprotein, Catalyzes ...PGP4, an ATP Binding Cassette P-Glycoprotein, Catalyzes Auxin Transport in Arabidopsis thaliana Roots W Kazuyoshi Terasaka,a,1

PGP4, an ATP Binding Cassette P-Glycoprotein, CatalyzesAuxin Transport in Arabidopsis thaliana Roots W

Kazuyoshi Terasaka,a,1 Joshua J. Blakeslee,b,1 Boosaree Titapiwatanakun,b,1 Wendy A. Peer,b

Anindita Bandyopadhyay,b Srinivas N. Makam,b Ok Ran Lee,b Elizabeth L. Richards,b

Angus S. Murphy,b,2 Fumihiko Sato,a and Kazufumi Yazakic

a Laboratory of Molecular and Cellular Biology of Totipotency, Division of Integrated Life Science, Graduate School

of Biostudies, Kyoto University, Kitashirakawa, Kyoto 606-8502, Japanb Department of Horticulture, Purdue University, West Lafayette, Indiana 47907-2010c Laboratory of Plant Gene Expression, Research Institute for Sustainable Humanosphere, Kyoto University,

Gokasho Uji 611-0011, Japan

Members of the ABC (for ATP binding cassette) superfamily of integral membrane transporters function in cellular

detoxification, cell-to-cell signaling, and channel regulation. More recently, members of the multidrug resistance

P-glycoprotein (MDR/PGP) subfamily of ABC transporters have been shown to function in the transport of the phytohormone

auxin in both monocots and dicots. Here, we report that the Arabidopsis thaliana MDR/PGP PGP4 functions in the basipetal

redirection of auxin from the root tip. Reporter gene studies showed that PGP4 was strongly expressed in root cap and

epidermal cells. PGP4 exhibits apolar plasma membrane localization in the root cap and polar localization in tissues above.

Rootgravitropicbendingandelongationaswell as lateral root formationwere reduced inpgp4mutantscomparedwith thewild

type.pgp4exhibited reducedbasipetal auxin transport in roots andasmall decrease in shoot-to-root transport consistentwith

a partial loss of the redirective auxin sink in the root. Seedlings overexpressing PGP4 exhibited increased shoot-to-root auxin

transport. Heterologous expression of PGP4 in mammalian cells resulted in 1-N-naphthylthalamic acid–reversible net uptake

of [3H]indole-3-acetic acid. These results indicate that PGP4 functions primarily in the uptake of redirected or newly

synthesized auxin in epidermal root cells.

INTRODUCTION

Members of the ATP binding cassette (ABC) transporter super-

family have been identified in all prokaryotic and eukaryotic or-

ganisms (Henikoff et al., 1997). AlthoughABC transporters are often

associated with the export of cytotoxic compounds (Gottesman

and Pastan, 1993), they also function in mating hormone trans-

port (Ketchumet al., 2001), ATP/ADP sensing (Bryan andAguilar-

Bryan, 1999), channel regulation (Anderson et al., 1991), and iron

homeostasis (Kushnir et al., 2001). ABC transporters have also

been shown tomediate the cellular uptake of urea (Beckers et al.,

2004), iron (Brown et al., 2002; Danese et al., 2004), small

peptides (Lamarque et al., 2004), choline (Dupont et al., 2004),

and bilirubin (Ieiri et al., 2004).

In contrast with other organisms, a broad proliferation of ABC

transporters has occurred in plants (Sanchez-Fernandez et al.,

2001; Martinoia et al., 2002; Jasinski et al., 2003; Garcia et al.,

2004). Members of the multidrug resistance–associated protein

(MRP) subfamily involved in the vacuolar sequestration of toxins or

xenobiotics are the best characterized (Martinoia et al., 1993; Rea

et al., 1998; Rea, 1999; Theodoulou, 2000). MRP1, MRP2, and

MRP3 transport glutathione conjugates of endogenous and arti-

ficial substrates into vacuoles (Lu et al., 1997, 1998; Tommasini

et al., 1998), and MRP4 and MRP5 have been implicated in the

complex regulation of stomatal aperture and guard cell ion flux

(Gaedeke et al., 2001; Klein et al., 2003, 2004). Members of the

pleiotropic drug resistanceprotein (PDR) subfamily, suchasPDR1

from Nicotiana plumbaginifolia (Jasinski et al., 2001; Stukkens

et al., 2005) andTURION2 fromSpirodela polyrrhiza (vandenBrule

et al., 2002), export antifungal diterpene defense compounds to

the leaf surface, and a half-size ABC protein, ECERIFERUM5, is

responsible for wax export to the plant cuticle (Pighin et al., 2004).

Although first identified in an unsuccessful attempt to enhance

herbicide resistance (Sidler et al., 1998), the majority of plant

multidrug resistance P-glycoproteins (MDR/PGPs; hereafter re-

ferred to as PGPs) characterized to date have been implicated in

the transport of the phytohormone auxin: PGP1 and PGP19were

identified as the principal Arabidopsis thaliana plasma mem-

brane (PM) proteins binding the auxin efflux inhibitor 1-N-

naphthylthalamic acid (NPA) with high affinity (Murphy and

Taiz, 1999a, 1999b; Noh et al., 2001; Murphy et al., 2002). Loss

of PGP19 and PGP1 function results in reduced auxin transport

and growth defects of varying severity in Arabidopsis (pgp1,

pgp19/mdr1), maize (Zea mays; brachytic2), and sorghum

1These authors contributed equally to this work.2 To whom correspondence should be addressed. E-mail [email protected]; fax 765-494-0391.The authors responsible for distribution of materials integral to thefindings presented in this article in accordance with the policy describedin the Instructions for Authors (www.plantcell.org) are: Angus S. Murphy([email protected]) and Kazufumi Yazaki ([email protected]).WOnline version contains Web-only data.Article, publication date, and citation information can be found atwww.plantcell.org/cgi/doi/10.1105/tpc.105.035816.

The Plant Cell, Vol. 17, 2922–2939, November 2005, www.plantcell.orgª 2005 American Society of Plant Biologists

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Figure 1. Expression Profile of PGP4 in Arabidopsis.

(A) Organ-specific expression of PGP4. Total RNA (5 mg) prepared from each Arabidopsis organ was probed with 32P-labeled PGP4 fragment (0.7 kb)

(top gel). The amount of total RNA applied to each lane is shown by 18S rRNA (bottom gel). RL, rosette leaf; CL, cauline leaf; S, stem; R, root; F, flower.

Abundances of PGP4 transcripts were quantified and confirmed via in silico analysis of microarray expression data and semiquantitative real-time PCR

analysis. Relative expression values were determined using the radioimaging analyzer BAS 1800 (Fuji Film Co.). The expression level of the PGP4mRNA

was normalized by the 18S rRNA values. The experiment was repeated twice with similar results.

(B) Response of PGP4 expression to various treatments. Cont., untreated control. Fourteen-day seedlings were treated for 24 h with 10 mM

1-naphthaleneacetic acid (NAA), 10 mM IAA, 10 mM 2,4-D, 10 mM 6-benzyladenine (BA), 10 mM kinetin (kin.), 10 mM abscisic acid (ABA), 10 mM gibberellic

acid (GA3), 10 mM brassinolide (BL), 100 mM methyl jasmonate (JA), 100 mM salicylic acid (SA), and 10 mM stigmasterol (St) and at 48C (cold)/low light

and dark (dark). Total RNA (8 mg) prepared fromwhole seedlings was probed with a 32P-labeled PGP4 fragment (top gel). Loading controls are shown by

b-actin (bottom gel). Relative expression values were determined using the radioimaging analyzer BAS 1800. The expression level of the PGP4 mRNA

was normalized by the actin values. The experiment was repeated twice with similar results.

PGP4 Catalyzes Auxin Transport in Roots 2923

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(Sorghum bicolor; dwarf3) (Noh et al., 2001; Geisler et al., 2003,

2005; Multani et al., 2003). Auxin transport reduction and dwarf

phenotypes are more exaggerated in Arabidopsis pgp1 pgp19

double mutants, suggesting overlapping function (Geisler et al.,

2003, 2005). Recently, PGP1 and PGP19 have been shown to

mediate the ATP-dependent cellular efflux of natural and syn-

thetic auxins as well as oxidative auxin breakdown products in

Arabidopsis protoplasts and whole plants (Geisler et al., 2003,

2005). Furthermore, heterologous expression of PGP1 in yeast

and mammalian cells resulted in increased auxin efflux (Geisler

et al., 2005). Although all of the evidence reported to date in-

dicates a role for PGPs in auxin efflux, structural differences

observed among the 21 expressedmembers of the PGP family of

Arabidopsis (Jasinski et al., 2003; E.L. Richards andA.S.Murphy,

unpublished data) suggest that energy-dependent PGP media-

tion of active auxin uptake is also possible.

Previously, we identified a PM PGP transporter, MDR1, in the

model isoquinoline alkaloid producer, Coptis japonica, and

demonstrated that the protein mediated ATP-dependent ber-

berine uptake (Yazaki et al., 2001; Sakai et al., 2002; Shitan et al.,

2003; Yazaki, 2005). A survey of the Arabidopsis genome for

a homolog of CjMDR1 indicated that a predicted protein of 1286

amino acids, AtPGP4 (At2g47000; hereafter referred to as

PGP4), was the most similar Arabidopsis homolog (71% amino

acid identity, 68% nucleotide identity). Because Arabidopsis

does not produce isoquinoline alkaloids, we considered the

possibility that PGP4 might be involved in auxin transport, as

PGP4 shares sequence similarity with both PGP1 and PGP19 (60

and 61%, respectively). However, the predicted PGP4 amino

acid sequence also contains a unique coiled-coil protein in-

teractive domain at its N terminus and exhibits substantial

sequence divergence from PGP1 and PGP19 in the loop region

adjoining the first conserved nucleotide binding domain. To

clarify the physiological function of PGP4 in Arabidopsis and

determine whether PGP4 might function as an uptake trans-

porter, we have analyzed PGP4 expression and characterized

PGP4 protein function.

RESULTS

Expression of PGP4

RNA gel blot analysis with aPGP4-specific 0.7-kb probe showed

that PGP4 expression is tissue-specific. PGP4 was strongly

expressed in roots and weakly expressed in stems and leaves,

but it was not detected in flowers (Figure 1A). PGP4 expression

(determined by quantitative real-time PCR) in both primary and

lateral root tips remains high throughout development (data not

shown), although a transient decrease in seedling expression

has been reported between 4 and 7 d after germination (Santelia

et al., 2005).

In 14-d-old seedlings, the effects of hormones, signaling

molecules, and abiotic factors on PGP4 expression were ana-

lyzed: PGP4 expression was upregulated by treatment with

natural and synthetic auxins and the cytokinin kinetin, whereas

abscisic acid and cold treatments downregulated PGP4 expres-

sion (Figure 1B). A time course of PGP4 expression in 5-d seed-

lings in response to indole-3-acetic acid (IAA), kinetin, and

abscisic acid was analyzed by quantitative real-time PCR to

further refine PGP4 responsiveness to these stimuli (Table 1).

Like PGP1 and PGP19 (Noh et al., 2001; Geisler et al., 2005),

PGP4 expression increased after exogenous IAA treatment (P <

0.001) (Table 1); however, the expression did not increase until

8 h after treatment, indicating that PGP4 is a late auxin response

gene. Consistent with a correlation between late auxin response

and stress gene induction by stress and wounding (Smith et al.,

2003), abscisic acid treatment resulted in a 4-h oscillation pattern

(peak to peak) of PGP4 expression (P < 0.001), whereas only

a small transient increase in expression was seen at 4 to 6 h after

kinetin treatment (P¼ 0.002) (Table 1). The abundances of PGP4

transcripts in Figure 1 were confirmed via radioimaging, semi-

quantitative RT-PCR (see Supplemental Figure 1 online), and

comparisons with published microarray data (http://bbc.

botany.utoronto.ca/affydb/cgi-bin/affy_db_exprss_browser_in.

cgi?p; http://www.arexdb.org/index.jsp; http://signal.salk.edu/

cgi-bin/tdnaexpress).

Wild-type plants were transformed with ProPGP4:GUS, con-

sisting of a 2.2-kb sequence upstream of the PGP4 start site

fused to a b-glucuronidase (GUS) reporter gene, and the T2 or

T3 generations were histochemically stained with 5-bromo-4-

chloro-3-indolyl-b-glucuronic acid (X-Gluc) at different develop-

mental stages. Consistent with the RNA gel blot analysis, PGP4

was strongly expressed in the roots of seedlings and mature

plants (Figures 2A and 2E). In the mature portion of the root,

PGP4was expressed in the epidermis and cortex (Figures 2F and

2G). In the root elongation zone, GUS staining was restricted to

the epidermis (Figures 2H and 2I), and in the root tip, GUS signal

was observed only in the root cap, S3 columella, and epidermal

cells (Figures 2J and 2K). No staining was evident in aerial

tissues, although extended X-Gluc treatment resulted in weak

staining at hydathodes and silique junctions (Figures 2B to 2D).

Table 1. Time Course of PGP4 Expression in Response to Various Hormones via Quantitative Real-Time PCR Analysis

Time (h)

Hormone 0 2 4 6 8 12

IAA 1.0 6 0.8 3.0 6 0.4 3.3 6 0.2 2.3 6 0.7 22 6 2.0a 44 6 2.5a

Abscisic acid 1.0 6 0.8 7.6 6 2.2a 2.0 6 0.5 8.4 6 0.7a 2.5 6 0.7 5.0 6 0.5a

Kinetin 1.0 6 0.8 0.9 6 0.6 4.3 6 1.5a 5.1 6 1.6a 1.9 6 0.3 3.0 6 1.1

PGP4 expression was measured relative to time 0 with b-tubulin as the endogenous correction factor. Values shown are means 6 SD.a Significantly different from time 0 as determined by analysis of variance, followed by Dunnett’s posthoc analysis (P < 0.05).

2924 The Plant Cell

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Figure 2. GUS Staining of ProPGP4:GUS Transformants.

(A) GUS activity is seen throughout the root in a 5-d ProPGP4:GUS seedling.

(B) GUS activity in a ProPGP4:GUS rosette leaf.

PGP4 Catalyzes Auxin Transport in Roots 2925

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Localization of PGP4

Previously, an unidentified high molecular mass protein band

was observed after SDS-PAGE of NPA-affinity purification of

PGP1 and PGP19 from microsomal fractions (Murphy et al.,

2002; Geisler et al., 2003). Amino acid sequencing of that band

indicated that it contained amixture of PGP1, PGP19, and PGP4

(Table 2). Sucrose density gradient fractionation of microsomal

membranes suggested that PGP4 is found inmultiple membrane

fractions (Figure 3A). However, the PGP4peak fraction coincided

with that of the PM Hþ-ATPase W1D (Figure 3A) to a greater

extent than with the endoplasmic reticulum lumenal marker bind-

ing protein (BiP) (Haas, 1994) and the Hþ-pyrophosphatase (Hþ-

PPase) multiple-compartment marker ARABIDOPSIS VACUOLAR

PYROPHOSPHATASE1 (AVP1) (Li et al., 2005). Furthermore, when

wild-type microsomal membranes were separated via aqueous

two-phase partitioning, PGP4 was found predominantly in the

PM-enriched upper phase, along with the PM Hþ-ATPase W1D

(Figure 3B). This distribution is consistent with a recent report of

PGP4,Hþ-ATPase, andBiP retention in detergent-resistantmicro-

domains (Borner et al., 2005). PGPs have also been localized

in detergent-resistantmicrodomains involved in vesicular cycling

between endomembrane compartments and the PM in mam-

mals (Kipp and Arias, 2002; Brown and London, 1998a, 1998b).

Both PM and endomembrane localization of PGP4 was appar-

ent in immunofluorescence localizations of the protein (Figures 3D

to 3I) using antisera generated against the unique N-terminal

domain of PGP4 (see mutant characterization below). Apical

(bottom) PM localization of PGP4 was seen in mature root

epidermal cells from the proximal elongation zone to two to three

cell stories below the root–shoot junction (Figures 3D and 3E);

although PGP4 is expressed in mature root cortical tissues,

cortical PGP4 signals were very weak, attributable perhaps to

posttranscriptional regulation, poor confocal laser penetration, or

limited antibodypenetration in this tissue. These tissues coincided

exactly with tissues where the PGP1 efflux transporter was

previously shown to be predominantly basally localized (Geisler

et al., 2005). However, in a short region (three cell stories) of the

root transition (distal elongation) zone, basal (top) PM localization

of PGP4 was observed (Figures 3F and 3G). Interestingly, PGP1

was shown previously to exhibit increased apical PM localization

in this region (Geisler et al., 2005). Similar to PGP1 (Geisler et al.,

2005), apolar PM and some apparent endomembrane localization

of PGP4was observed at the root apex. Apolar PGP4 localization

was restricted to S3 columella and adjacent root cap cells

(Figures 3H and 3I), where PGP1 localization is not seen (Geisler

et al., 2005) and where ALTERED RESPONSE TO AUXIN AND

GRAVITY1 (AUX1) also exhibits apolar localization (Swarup et al.,

2001, 2004). Figure 3C shows a differential interference contrast

(DIC) image of a root for reference.

Phenotypic Characterization of pgp4Mutants

Five T-DNA insertional lines in the PGP4 genewere obtained from

the SALK collection (Alonso et al., 2003), and three homozygous

mutant lines were selected after PCR analysis of the insertion

sites: pgp4-1 (SALK_063720), pgp4-3 (SALK_067653), and pgp4-4

(SALK_088311) (Figure 4A). In all three lines, no PCR product was

obtained with primers designed for either the full-length cDNA or

sequences flanking the insertion site. In pgp4-1 seedlings, PGP4

mRNA was not detected via RNA gel blot analysis using a gene-

specific probe (Figure 4B). Furthermore, PGP4 protein was not

detected when pgp4-1 membrane fractions were immunoblotted

with PGP4-specific antisera (Figure 4B). The PGP4 antisera cross-

reacted with a single band of the expected apparent molecular

mass (140 kD) on SDS gels prepared from wild-type Arabidopsis

seedlingmembranes. The antisera also did not cross-react with the

closest homolog, PGP21 (;129 kD), which is expressed in seed-

lings at levels similar to those ofPGP4 (Figure 4B; seeSupplemental

Table 2. PGPs Identified in NPA Binding Fractions

Band Size

125 to 140 kD Protein Sequence Data

PGP4 EEEEEVKa–GYTGGQVLNIIIAVLTG–

VLLLDEATSALDAESERb

PGP10 PSVSFLK–LFSFADFYDXVLc–LLEPSE–

VVQQALDRc

PGP19 FDYLLMFVGSLGAIVHGSS–GFAGDTAK–

DGATESEVIDAA

Microsomal proteins were isolated and subjected to NPA-affinity chro-

matography, as described by Murphy et al. (2002). Select protein bands

from SDS-PAGE were isolated and sequenced. Unique sequence data

were used to identify proteins present in each band. –, break in amino

acid sequence; X, indeterminate amino acid.a Sequence in PGP4 and also in four other unrelated sequences.b Sequence also found in PGP17.c Sequence also found in PGP2.

Figure 2. (continued).

(C) GUS activity in a ProPGP4:GUS silique.

(D) GUS activity in the hydathodes of a ProPGP4:GUS rosette leaf (magnification of [B]).

(E) GUS activity is seen primarily in the roots of a 14-d ProPGP4:GUS plant.

(F) GUS activity is seen in the epidermis and the cortex in a radial section of the mature root region in a ProPGP4:GUS plant. Cx, cortex; Ed, endodermis;

Ep, epidermis.

(G) GUS activity in a longitudinal section of the mature root region in a ProPGP4:GUS plant.

(H) GUS activity in the epidermis of a radial section of the root elongation zone in a ProPGP4:GUS plant.

(I) Magnification of (H).

(J) GUS activity in the root cap and the epidermis in a radial section of a ProPGP4:GUS root tip. Rc, root cap.

(K) GUS activity in the root cap, the S3 columella cells, and the epidermis in a longitudinal section of a ProPGP4:GUS root tip.

Bars ¼ 1 mm in (A) to (D), 2.5 cm in (E), and 50 mm in (F) to (K).

2926 The Plant Cell

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Figure 3. Subcellular Localization of PGP4.

(A) Membrane fractionation and immunodetection of PGP4. Fractionation of total microsomes from Arabidopsis seedlings was done on a non-

continuous sucrose gradient consisting of 20, 30, 40, and 50% (w/v) sucrose. Membrane fractions were collected from the interfaces between different

PGP4 Catalyzes Auxin Transport in Roots 2927

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Figure 1 online). No signal was detected when the PGP4 antisera

was used in immunofluorescence localizations of pgp4-1 mutants

at the dilution used with the wild type (Figures 3J to 3M).

The root lengths of 10-d pgp4-1 seedlings were 30% shorter

than those of the wild type, and the number of lateral roots was

also significantly reduced (;61% of wild type; P < 0.01) (Figures

4C to 4E). Similar results were observed for pgp4-3 and pgp4-4

(see Supplemental Table 1 online). These root phenotypes were

reproducible when seedlings were grown atmoderate light levels

(100 to 120mmol�m�2�s�1) using sucrose concentrations of 0.5 to

1% (see Methods). The conditions under which these pheno-

types are most visible in pgp4 (Figures 4C and 4D; see Supple-

mental Figure 2 online) are similar to those under which pgp1

growth phenotypes are most evident (Geisler et al., 2005).

However, when pgp4 mutants were grown under high light or

on sucrose concentrations >1.5%, the root lengths and number

of lateral roots observed were greater than or equal to those of

the wild type (data not shown). Root phenotypes in pgp4-1 could

be complemented by transformation with Pro35S:PGP4 (P > 0.05)

(Figure 4D; see Supplemental Figure 2 online).

pgp4-3 and pgp4-4 seedlings exhibited reductions in the rate

of root gravitropic bending similar to the observed decreases in

linear root growth (P < 0.05) (Figure 4F); pgp4-1 root gravitropic

responses were not statistically different from those of the wild

type, perhaps because of the large standard deviations ob-

served (P > 0.05). Furthermore, no changes in ProPGP4:GUS

expression patterns were evident in roots up to 6 h after

gravistimulation (data not shown). Because of this, observed

differences in root gravitropism were assumed to be the result of

reduced linear root growth in pgp4 mutants, not an intrinsic

defect in the gravitropic response. An alternative explanation

could be that the slight gravitropism phenotype observed in

pgp4-3 and pgp4-4 may be a dominant negative effect.

Consistent with the observed root-specific expression of

PGP4, no obvious morphological differences between pgp4-1

and wild-type plants were observed in the aerial parts of seed-

lings and adult plants. The lack of a visible phenotype of pgp4-1

mutants in aerial tissues may also result from functional re-

dundancy in these tissues because other PGPs implicated in

auxin transport (such as PGP19, PGP6, and PGP10) are ex-

pressed in aerial tissues at much higher levels than PGP4

(Blakeslee et al., 2005b). This is in contrast with root tissues, in

which PGP4 appears to be the most highly expressed PGP.

PGP4Overexpression

PGP4 was also overexpressed under the control of a 35S pro-

moter (Pro35S:PGP4; hereafter referred to as PGP4OX). Roots of

PGP4OX lines were only slightly longer than wild-type roots

(Figures 4C and 4D), and no changes were evident in shoot

phenotypes. Similar growth phenotypes were observed in mul-

tiple independent PGP4OX lines. PGP4 expression in PGP4OX

roots was twofold to fourfold that of the wild type (P < 0.05) but

did not increase significantly in shoots (P > 0.05). As similar

expression patterns were observed in all recovered PGP4OX

lines, it appears that PGP4 transcript abundance is posttran-

scriptionally regulated in overexpressor lines.

Immunolocalization of PGP4 in PGP4OX was similar to that in

the wild type, except that the signal was stronger in the root cap

and elongation zone. No change in subcellular localization was

seen in the root cap (data not shown), but PGP4 signals in three

stories of epidermal cells in the elongation zone expanded

slightly to lateral membranes as well (Figures 3N and 3O). This

localization pattern was observed in all PGP4OX lines recovered,

consistent with the posttranscriptional regulation of ectopic

PGP4 expression.

Figure 3. (continued).

sucrose concentrations and analyzed via SDS-PAGE and protein gel blotting. Blots were probed with antisera to PGP4, PM Hþ-ATPase (W1D),

multicompartment Hþ-PPase (AVP1), and endoplasmic reticulum BiP (BiP).

(B) Two-phase separation of PM and immunodetection of PGP4. Microsomal membranes (M) from Arabidopsis seedlings were fractionated by the

aqueous two-phase portioning method, by which PM was enriched in the upper phase (U) and other intracellular membranes remained in the lower

phase (L). Proteins from each fraction (5 mg per lane) were blotted and probed with antisera to PGP4, PM Hþ-ATPase, multicompartment Hþ-PPase,

and endoplasmic reticulum BiP.

(C) DIC image of a 5-d seedling root. Top bracket, mature root ([D], [E], [J], and [K]); middle bracket, root transition zone ([F], [G], and [L] to [O]);

bottom bracket, root tip ([H] and [I]). Bar ¼ 100 mm.

(D) Confocal image of immunohistochemical localization of PGP4 in a wild-type mature root region. Apical (bottom) PGP4 signal is observed.

(E) DIC overlay of (D).

(F) Confocal image of immunohistochemical localization of PGP4 in a wild-type root transition zone. Basal (top) PGP4 signal is restricted to three cell

stories in the root transition zone.

(G) DIC overlay of (F).

(H) Confocal image of immunohistochemical localization of PGP4 in a wild-type root tip. PGP4 signal is seen in the root cap, S3 columella cells, and

epidermis.

(I) DIC overlay of (H).

(J) Confocal image of immunohistochemical localization of PGP4 in pgp4-1 in a mature root region. Only nonspecific epidermal signal is observed.

(K) DIC overlay of (J).

(L) Confocal image of immunohistochemical localization of PGP4 in pgp4-1 in the root transition zone. Only nonspecific epidermal signal is observed.

(M) DIC overlay of (L).

(N) Confocal image of immunohistochemical localization of PGP4 in PGP4OX in the root transition zone. Basal and lateral PGP4 signal is restricted to

three cell stories in the root transition zone.

(O) DIC overlay of (N).

2928 The Plant Cell

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Figure 4. Genomic Structure of PGP4 and Phenotypes of pgp4.

PGP4 Catalyzes Auxin Transport in Roots 2929

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Gain or loss of PGP4 expression does not alter the expression

of PGP1 and PGP19, as expression of these genes (determined

by quantitative real-time PCR) was not different from that of the

wild type in pgp4-1 and PGP4OX (P > 0.05). Similarly, although

the PIN-FORMED2 (PIN2) auxin efflux protein is basally localized

in thesameepidermal andcorticalcells asPGP4 (Chenetal., 1998;

Luschnig et al., 1998; Muller et al., 1998; Peer et al., 2004), as was

the case with pgp1 mutants (Geisler et al., 2005), no alteration

in PIN1 or PIN2 localization and abundance was apparent in

pgp4-1 or PGP4OX (see Supplemental Figures 3 and 4 online).

Polar Auxin Transport in pgp4 and PGP4OX

Auxin transport and free IAA levels were measured in pgp4-1

seedlings as described previously (Geisler et al., 2003, 2005). A

slight decrease of basipetal transport observed in pgp4-1

hypocotyls (P < 0.05) (Figure 5A) and increased free IAA con-

centrations in the lower part of the hypocotyls (P < 0.05) (Figure

5B) may be the result of the elimination of low levels of PGP4

expression in hypocotyls, but they are more likely the result of

a diminished root tip auxin uptake sink. Consistent with this

interpretation, reduced auxin uptake and basipetal auxin trans-

port were observed at pgp4-1 root tips (P < 0.05) (Figure 5C), and

free IAA levels were significantly increased in the first 1.5 mm of

the root tip in pgp4-1 (P# 0.01) (Figure 5D). Furthermore, aggre-

gations of the flavonol quercetin have been shown to accumulate

near the root tip when auxin concentrations increase (Peer et al.,

2004). Similar aggregations were observed in pgp4-1 (Figures 5E

and 5F; see Supplemental Figure 5 online).

The light/sucrose dependence of pgp4 seedling growth phe-

notypes suggested that differences in basipetal auxin transport

observed between pgp4 and thewild typewould decrease under

light conditions of >120 mmol�m�2�s�1. This proved to be the

case (data not shown). Higher light conditions have been shown

to increase both sucrose production and apoplastic acidification

in roots (Le Bot and Kirkby, 1992; Stewart and Lieffers, 1994).

Lower apoplastic pH was recently shown to increase chemios-

motically driven auxin efflux and uptake in Arabidopsis roots (Li

et al., 2005). On the other hand, if PGP4 is a hydrophobic anion

uptake transporter, decreased apoplastic pHwould be expected

to decrease PGP4-mediated transport.

Analysis of auxin transport in PGP4OX supports a primary

function of PGP4 in establishing an auxin uptake sink in the root

cap, as shoot basipetal and root acropetal auxin transport in

PGP4OX seedlings both increased by;240% (P < 0.05) (Figure

5A), despite no increase in PGP4 expression in shoot tissues.

The lack of increased root basipetal transport observed in

PGP4OX (Figure 5C) suggests that the increased lateral locali-

zation of PGP4 seen in root transition/distal elongation zone cells

has either a negative or a negligible impact on basipetal trans-

port. However, root basipetal auxin transport was restored to

wild-type levels after complementation of pgp4-1 with PGP4OX

(see Supplemental Figure 2 online).

Vanadate-Induced Nucleotide Trapping of PGP4

As the nucleotide binding affinity and ATPase activity of ABC

transporters greatly increases in the presence of preferred

substrates when combined with vanadate (Urbatsch et al.,

1995), vanadate-induced nucleotide trapping can be used to

screen for ABC transporter substrates (Sakai et al., 2002;

Terasaka et al., 2003). However, this method cannot be used

with crude membranes from Arabidopsis because of the large

number of ABC transporters present. PGP4 was expressed in

Sf9 insect cells, which have low background vanadate-trapping

activity and are used extensively to characterize the ATPase

activity and substrate specificity of ABC transporters (Sarkadi

et al., 1992; Rao, 1998; Cortes-Selva et al., 2005). Photoaffinity

labeling of an;140 kD protein could be seen when recombinant

PGP4 was expressed in Sf9 cells (Figures 6A and 6B). As was

seen with the human PGPHsMDR1 (Ueda et al., 1997), this basal

level of PGP4 ATPase activity required both Mg2þ and vanadate

(Figure 6B).

Natural and synthetic growth regulators and their precursors

were screened using this system as a first approximation to

determine possible substrates of PGP4. IAA, the weak auxin

indole-3-propionic acid, the competitive auxin transport inhibitor

tri-iodobenzoic acid, and the PGP binding auxin efflux inhibitor

NPA (Noh et al., 2001; Murphy et al., 2002; Geisler et al., 2003) all

increased vanadate-trapping signals, whereas other growth

regulators and artificial auxins (2,4-D and 1-naphthaleneacetic

acid) did not (Figure 6C). In addition, two nonbioactive structural

analogs of auxin, syringic acid and vanillic acid, also increased

the vanadate-trapping signal (Figure 6C). The vanadate-trapping

method could not be used to further resolve the auxin specificity

Figure 4. (continued).

(A) Genomic structure of PGP4 T-DNA insertion sites of pgp4-1 (SALK_063720), pgp4-3 (SALK_067653), and pgp4-4 (SALK_088311). Rectangles

represent exons, and lines represent untranslated regions, including the introns of the PGP4 gene. T-DNA, represented by triangles, is not drawn to

scale. The black box in the 6th exon indicates the first nucleotide binding fold (NBF1), and those in 10th and 11th exons indicate the second nucleotide

binding fold (NBF2).

(B) RNA and protein gel blot analyses of pgp4-1. Ten micrograms of total RNA and 30 mg of microsomal protein from either wild-type or mutant

seedlings were analyzed. Neither PGP4 mRNA nor protein was detected in pgp4-1, indicating that this is a null allele.

(C) Root phenotype of pgp4-1and PGP4 overexpressor 7-d seedlings, and complementation of pgp4-1. Bar ¼ 1 cm.

(D) pgp4-1 seedlings have shorter roots. Asterisk indicates statistically significant difference in root length between the wild type and the pgp4-1mutant

(P < 0.01, n ¼ 16). Experiments were done in triplicate.

(E) pgp4-1 seedlings have fewer lateral roots. Asterisk indicates statistically significant differences in lateral root number between the wild type and

pgp4-1 mutant (P < 0.01, n ¼ 16). Experiments were done in triplicate.

(F)Gravitropic phenotypes in pgp4-3 and pgp4-4. The angle of curvature is reduced in both pgp4 alleles compared with the wild type. Twenty seedlings

were used per replicate (n ¼ 3). Asterisks indicate significant difference from the wild type by Student’s t test (P < 0.05).

2930 The Plant Cell

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Figure 5. Auxin Transport in pgp4-1 and PGP4OX.

(A) Basipetal hypocotyl and acropetal root transport in Columbia wild-type, pgp4-1, and PGP4OX 5-d seedlings. Data are presented as percentage of

auxin transport, relative to Columbia wild type. Mean wild-type values were 4245.5 and 648 dpm for shoot basipetal and root acropetal transport,

respectively. n ¼ 2 groups of 10 seedlings each. Asterisks indicate significant difference from the wild type by Student’s t test (P # 0.05).

PGP4 Catalyzes Auxin Transport in Roots 2931

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of PGP4, as increased concentrations of IAA or indole-3-

propionic acid did not increase PGP4 photoaffinity labeling

(data not shown).

Cellular Transport Assays of Auxin by PGP4

PGP4 was expressed in the vaccinia virus–HeLa mammalian

expression system commonly used to analyze PGP activity and

recently used to demonstrate NPA-sensitive, PGP1-mediated

net efflux of [3H]IAA and [3H]1-naphthaleneacetic acid (Elroy-

Stein and Moss, 1991; Moss, 1991; Hrycyna et al., 1998; Geisler

et al., 2005). PGP4 expression and protein localization on the PM

were verified as described previously (Geisler et al., 2005) (Figure

7B). Unlike PGP1 (Geisler et al., 2005), expression of PGP4

resulted in a net increase in auxin retention comparedwith empty

vector controls (Figure 7A), indicating that PGP4 may transport

IAA into HeLa cells. A range of PGP4 expression levels were

assayed to determine whether an increased abundance of PGP4

resulted in mistargeting of the protein: at all concentrations

tested, net [3H]IAA retention was observed (data not shown).

These IAA uptake data are consistent with a recent report of

increased sensitivity to the toxic auxin analog 5-fluorol indole

seen in JK93da yeast expressing Arabidopsis PGP4 and similar

sensitivity to IAA seen in yap1-1 mutant yeast also expressing

PGP4 (Santelia et al., 2005).

The effects of auxin transport and ABC transport inhibitors on

net auxin retention were examined. NPA treatment abolished IAA

retention in HeLa cells expressing PGP4 (P# 0.006) (Figure 7A),

whereas treatment with the natural auxin transport inhibitor

quercetin (Peer et al., 2004) and the ABC inhibitors verapamil

and cyclosporin A significantly reduced IAA retention (P# 0.006)

(Figure 7A). Although auxin efflux inhibitors such as NPA, cyclo-

propyl propane dione, and quercetin have been shown to inhibit

PGP-mediated auxin efflux both in planta and in membrane

vesicles (Murphy et al., 2000; Geisler et al., 2005), in planta

effects on PGP4-mediated uptake are difficult to determine in

a background in which PGP1 and/or PGP19 are expressed.

However, NPA treatment (5 mM) resulted in a 35% 6 12%

reduction of IAA retention (P < 0.05) in pgp4-1 roots. Similar

results have been reported by Santelia et al. (2005).

Both PGP1 and PGP19 have been shown to transport oxida-

tive auxin breakdown products in addition to IAA (Geisler et al.,

2005). When cells expressing PGP4 were incubated with a mix-

ture of 50% radiolabeled auxin and 50% nonlabeled oxidative

auxin breakdown products, the IAA retention activity was

strongly inhibited (P # 0.006) (Figure 7A), indicating that IAA

metabolites are also likely PGP4 substrates. However, PGP4

does exhibit relative substrate specificity, as is the case with

PGP1 and PGP19 expression (Geisler et al., 2005; J.J. Blakeslee

and A.S. Murphy, unpublished data), PGP4 expressed in HeLa

cells did not transport the mammalian PGP substrates rhoda-

mine 123, daunomycin, or vinblastine (data not shown).

DISCUSSION

Evidence is presented here that PGP4 is a mediator of auxin

transport at the root apex and participates in basipetal auxin

transport in root epidermal tissues. Support for this conclusion

comes from analysis of PGP4 expression, PGP4 protein local-

ization and function, pgp4 growth phenotypes, auxin transport,

and auxin accumulation. These results also add to the growing

body of evidence supporting a major role of PGPs in auxin

transport (Noh et al., 2001, 2003; Geisler et al., 2003, 2005;

Multani et al., 2003; Santelia et al., 2005). Analysis of PGP gene

expression and pgp mutant growth phenotypes suggests that

PGPs function in a tissue-specific manner similar to what is seen

with the PIN proteins (Blakeslee et al., 2005a).

Until now, PGPs were thought to function exclusively in auxin

efflux. Together with recently published evidence that PGP4

expression increases the sensitivity of yeast to auxins and toxic

auxin analogs (Santelia et al., 2005), the results presented here

suggest that PGP4 functions as an energy-dependent uptake

transporter. Such a role for PGP4 is not unexpected in light of its

homology with the uptake transporter CjMDR1 and the energetic

requirements of transporting auxin anions against the chemios-

motic gradient. At the apoplastic pH of;5.5 seen in roots, only

;16% of the IAA (pKa 4.75) present is protonated (neutral and

lipophilic). As such, only a small portion of apoplastic IAA can be

taken up by hydrophobic diffusion. Anionic IAAmust be taken up

by a process that directly uses ATP, as is the case with an ABC

transporter such as PGP4, or by secondary active transport, as is

seen with the putative proton symporter AUX1 (Marchant et al.,

1999; Swarup et al., 2001). Although lipophilic uptake appears to

be sufficient in most tissues, additional uptake mechanisms

would be expected to be required at the root apex, where auxin

must be retained and redirected rapidly into the basipetal trans-

port stream.

However, based on the modest loss of root gravitropism

seen in some pgp4 alleles (equivalent to that seen in agr1/

pin2) compared with the severe agravitropism seen in aux1

Figure 5. (continued).

(B) Basipetal root auxin transport in a root segment 2 mm from the site of auxin application at the root apex. Data are presented as percentage of auxin

transport, relative to Columbia wild type. The mean wild-type value was 6473.5 dpm. n ¼ 2 groups of 10 seedlings each. Asterisk indicates significant

difference from the wild type by Student’s t test (P # 0.05).

(C) Quantitations of free IAA in wild-type and pgp4-1 hypocotyl sections. Fifty seedlings were used per replicate (n ¼ 3). Asterisk indicates significant

difference from the wild type by Student’s t test (P # 0.05).

(D) Quantitations of free IAA in wild-type and pgp4-1 root sections. Fifty seedlings were used per replicate (n ¼ 3). Asterisk indicates significant

difference from the wild type by Student’s t test (P # 0.01).

(E) Wild-type seedlings do not accumulate quercetin in the root elongation zone. Bar ¼ 100 mm for (E) and (F).

(F) pgp4-1 seedlings accumulate aggregations of quercetin in the corresponding region of the root elongation zone.

2932 The Plant Cell

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(Bennett et al., 1996), the contribution of PGP4 to auxin uptake in

these tissues appears to be less than that of AUX1. This makes

sense, as a symporter such as AUX1 would be expected to be

more sensitive to changes in pH associated with root gravisti-

mulation (Hou et al., 2004). The amelioration of pgp4 growth

phenotypes by increased light and sucrose also supports this

relationship, as light and sucrose enhance ATP-driven proton

extrusion (Le Bot and Kirkby, 1992; Stewart and Lieffers, 1994)

and, thus, chemiosmotically driven transport in roots (Li et al.,

2005).

Figure 6. Expression of Recombinant PGP4 in Sf9 Cells, and Vanadate Trapping.

(A) Immunoblot of PGP4 in Sf9 cells and Arabidopsis seedlings. Lane 1, membrane protein control from Sf9 cells; lane 2, 20,000g supernatant from cells

expressing PGP4; lane 3, 20,000g pellet from cells expressing PGP4; lane 4, Arabidopsis seedling microsomal membrane fraction. For membrane

proteins, 10 mg (lanes 1 to 3) or 30 mg (lane 4) was loaded per lane, respectively. CBB, Coomassie Brilliant Blue.

(B) Photoaffinity labeling of recombinant PGP4 expressed in Sf9 cells. Membrane proteins from recombinant AtPGP4 expressed in Sf9 cells were

incubated with 10 mM 8-azido-[a-32P]ATP in the presence or absence of 3 mM MgSO4 (Mg2þ) and 0.2 mM orthovanadate (Vi) for 10 min at 378C.

Proteins were photoaffinity-labeled with UV irradiation after removal of unbound ligands and analyzed by SDS-PAGE.

(C) Effect of putative substrates on the photoaffinity labeling of recombinant PGP4. Cont., control (no treatment). Seedlings were treated with 50 mM

naphthaleneacetic acid (NAA), 50 mM IAA, 50 mM 2,4-D, 50 mM 6-benzyladenine (BA), 50 mM kinetin (kin.), 50 mM abscisic acid (ABA), 50 mM gibberellic

acid (GA3), 25 mM brassinolide (BL), 50 mM vanillic acid (Va), 50 mM syringic acid (Sa), 50 mM indole-3-propionic acid (IPA), 50 mM NPA, or 50 mM

tri-iodobenzoic acid. Relative expression values were determined using the radioimaging analyzer BAS 1800 (Fuji Film Co.). The experiment was done in

duplicate. Representative results are shown.

PGP4 Catalyzes Auxin Transport in Roots 2933

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The localization of PGP4 is also consistent with uptake

function. Very little expression or protein abundance is seen in

the columella initials, S1 or S2 cell layers. Expression in the S3

layer is consistent with an uptake function, especially because

AUX1 has not been localized in these cells (Swarup et al., 2004),

but exhibits a similar apolar localization in epidermal/lateral root

cap cells. PGP4 localization in S3 and S3-derived cells in the

lateral root cap is also consistent with a lack of expression of

the PGP1 efflux transporter in those cells. PGP4 could also be

expected to maintain minimal levels of auxin uptake under

conditions of apoplastic alkalinization that would severely inhibit

lipophilic or AUX1/LIKE AUX1 uptake.

The apical (bottom) localization of PGP4 in the epidermal

cells of the proximal elongation zone and above is also

consistent with both an uptake function and the observed

pgp4 root growth phenotypes. What is more difficult to un-

derstand is the reversal of this orientation seen in three stories

of epidermal cells within the root transition/distal elongation

zone. However, it is interesting that PGP1 subcellular localiza-

tion changes from apolar to basal in the root transition zone

(Geisler et al., 2005). More significantly, these cells exhibit the

first changes in elongation after gravistimulation (Ishikawa and

Evans, 1997). As PGP4 expression does not appear to change

in these tissues in response to gravistimulation, we hypothesize

that PGP4 serves to increase auxin retention in these cells to

enhance graviresponsiveness. Functional green fluorescent

protein fusions of PGP4 now in progress will allow the analysis

of possible dynamic protein relocalization during gravitropic

responses.

Finally, these results suggest that PGP4-mediated auxin

uptake requires other factors to enhance auxin specificity. PIN

proteins are the most likely candidates for this role (Blakeslee

et al., 2005a). Although PGP4 is localized in the same cells as

PIN2, a direct interaction between these proteins is unlikely

because they are at opposite ends of the cell. Furthermore, in the

three cell stories of the transition zone where the two proteins

colocalize, PIN2 is more weakly expressed. However, as it is

likely that specific PIN–PGP pairings act to provide specificity

and directionality to polar auxin transport (Blakeslee et al.,

2005a), PGP4 interaction with one or more PIN proteins cannot

be ruled out. Using recently developed cellular assays of auxin

transport (Geisler et al., 2005), a functional analysis of interac-

tions between PGP4 and members of the PIN protein family is

now under way.

METHODS

Plant Material and Growth Conditions

Arabidopsis thaliana plants (ecotype Columbia) were grown on soil in

growth chambers with 100 or 120 mmol�m�2�s�1 light in a 16-h-light/8-h-

dark cycle at 218C. For growth under sterile conditions, seeds were

surface-sterilized (20-min incubation in 30% [v/v] sodium hypochlorite

and 0.02% [v/v] Triton X-100 and rinsed four times in sterile distilledwater;

or 2-min incubation in 20% [v/v] sodium hypochlorite, rinsed in distilled

water three times, with a final rinse of 95% ethanol) and sown on half-

strengthMurashige and Skoog (MS) salts supplemented with no sucrose,

0.5%, 1.0%, or 1.5% (w/v) sucrose, pH 5.8, and 0.8% (w/v) bactoagar or

phytagar in Petri dishes.

Figure 7. PGP4-Mediated Auxin Influx.

Net efflux is expressed as dpm/500,000 cells: the amount of auxin retained by cells transformed with empty vector minus the amount of auxin retained

by cells transformed with the gene of interest. Reductions in retained auxin (efflux) are presented as positive values, and increases in retention (influx)

are presented as negative values. Values shown are means with sum of the standard deviations (n ¼ 3).

(A) PGP4 expressed in HeLa cells had increased influx of radiolabeled IAA compared with cells transformed with empty pTM1 vector. For inhibitor

studies, cells were incubated with radiolabeled IAA in the presence of 10 mM NPA, 200 nM quercetin (Quer.), 1 mM cyclosporin A (CsA), or 5 mM

verapamil (Ver.). NPA treatment reverses PGP4-mediated influx. For radiolabeled auxin degradation product assays, cells were loaded with 63 nM

radiolabeled IAA and 63 nM nonlabeled IAA oxidative breakdown products (Deg.). Asterisks indicate significance as determined by Student’s t test (P#

0.006): PGP4 activity was compared with empty vector control; PGP4 activity þ inhibitors was compared with empty vector control þ inhibitors.

(B) Immunolocalization of hemagglutinin-tagged PGP4 expressed in HeLa cells. Hemagglutinin-tagged PGP4 was detected with an anti-hemagglutinin

antibody. Bar ¼ 10 mm.

2934 The Plant Cell

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To analyze the regulation of PGP4 transcripts by various growth

regulators, seeds were sown onto nylon mesh (20-mm pore) over the

MS medium and grown for 14 d under the same light cycle described

above. Roots were subjected to various treatments by gentle transfer of

the mesh to new medium. Treatments were stopped by immediate

freezing of seedlings in liquid N2.

Cloning of AtPGP4 cDNA and Construction of the Plant

Overexpression Construct

To isolate the cDNA of PGP4 (At2g47000) by RT-PCR, two primers were

designed that allowed the amplification of the entire PGP4 open reading

frame, adding to the 32-bp 59 untranslated region and the 58-bp 39

untranslated region (forward primer, 59-CGTCTAGAGCTTAGGATCGT-

GAGGTATCTG-39; reverse primer, 59-GCTGAGCTCATATAACGGGG-

CATAATTGAC-39). The underlined positions are nonnative sequences

representing XbaI and SacI restriction sites, respectively. The PCR

product was subcloned into pBluescript II SK� (Stratagene) for sequenc-

ing. The full-length cDNA was transferred into pENTR1A vector (Invitro-

gen) using SalI andNotI sites. This construct served as the entry vector to

transfer the cDNA of PGP4 into the binary destination vector pGWB2 for

constitutive expression via the Gateway system (Invitrogen) to create the

Pro35S:PGP4 construct with the cauliflower mosaic virus 35S promoter.

Agrobacterium tumefaciens GV3101 (pMP90) was transformed with the

binary vector, which was introduced into ArabidopsisColumbia wild-type

plants by floral dip (Clough and Bent, 1998). Kanamycin- and hygromycin-

resistant plants in the T1 and T2 generations were examined by

immmunoblot analysis.

RNA Isolation and RNA Gel Blot Analysis

Total Arabidopsis RNA was prepared from 200 mg of seedlings using the

RNeasy plant mini kit (Qiagen). Agarose gel electrophoresis, RNA trans-

fers onto Hybond-Nþ membranes (Amersham Bioscience), and hybrid-

izationwith the 0.7-kbAtPGP4 fragment (positionsþ1989 toþ2711) were

performed using standard procedures. The last stringent wash was

performed with 0.23 SSC (13 SSC is 0.15 M NaCl and 0.015 M sodium

citrate) and 0.1% SDS at 608C.

Promoter:GUS Fusion and GUS Expression Analysis

To create thePGP4 promoter:reporter construct (ProPGP4:GUS), twoPCR

primers flanking the regions from þ15 to �2196 were made (forward

primer, 59-GCTAAGCTTGGTAAAGGATTTGGGTCTATTCG-39; reverse

primer, 59-CTGTCTAGAGCTCTCTGAAGCCATTAGAGTTT-39). The un-

derlined positions are nonnative sequences representingHindIII and XbaI

restriction sites, respectively. PCRwas performed using genomic DNA as

a template and KOD-Plus polymerase (Toyobo). The PCR product was

inserted upstream of the GUS coding sequence in the pBI101 binary

vector. A. tumefaciens GV3101 (pMP90) was transformed with the binary

vector and introduced into wild-type Arabidopsis as described above.

Kanamycin-resistant plants in the T2 generation were histochemically

stained to detect GUS activity. For GUS staining, tissues were prefixed in

ice-cold 90% acetone for 20 min, rinsed with cold water, immersed with

staining solution (50 mM sodium phosphate buffer, pH 7.0, 0.1% Triton

X-100, 0.5 mM potassium ferrocyanide, 0.5 mM potassium ferricyanide,

and 1mMX-Gluc), and incubated at 378C for 2 to 5 h for roots and 20 h for

rosette leaves and siliques. For higher integrity of the DIC imaging,

destaining time was limited before fixation; therefore, very light staining

does not indicate signal. The stained samples were fixed in 50% ethanol,

5% acetic acid, and 3.7% formaldehyde, dehydrated through an ethanol

series, and embedded in Technovit 7100 (Heraeus Kulzer) according to

themanufacturer’s protocol. Tissue sections (10 mm thick) weremounted

on slides and examined with a light microscope (Zeiss).

Peptide Antiserum against PGP4

A keyhole limpet hemocyanin conjugate of an oligopeptide of PGP4, at

position 1 (n-MASESGLNGDPNILEEVSEC-c), was injected into rabbits

according to a standard protocol (Kurabo Industries). After the fourth

boost, the antiserum was recovered and used for immunoblot analysis

and immunohistochemical analysis without further purification.

Density Gradient Fractionation of Membrane Vesicles

For sucrose gradient fractionation, the method described by van den

Brule et al. (2002) was used with the following modifications. Arabidopsis

seedlings (5 g) were homogenized in 3 volumes of 50 mM HEPES-KOH,

pH 7.5, 5 mM EDTA, 2 mM DTT, 250 mM sucrose, and 1 mM phenyl-

methylsulfonyl fluoride using mortar and pestle. The homogenate was

centrifuged for 15 min to remove the debris, and the microsomal

membrane fraction was pelleted by ultracentrifugation at 100,000g for

30 min. The pellet was resuspended in 3 mL of gradient buffer (10 mM

Tris-MES, pH 7.0, 1 mM DTT, 250 mM sucrose, and 1 mM phenyl-

methylsulfonyl fluoride) and centrifuged at 100,000g for 3 h on a non-

continuous sucrose gradient from 13 to 40% (w/v) in the same buffer

using a Beckman SW41Ti rotor. Gradient fractions were collected from

the interface between different sucrose concentrations.

PM fractions were separated from microsomal preparations by parti-

tioning in an aqueous polymer two-phase system, as described pre-

viously (De Michelis et al., 1996). The upper (PM) phase as well as the

lower phase were used for immunoblot analysis.

For immunoblotting, proteins were denatured in the denaturation buffer

(10 mM Tris-HCl, pH 8.0, 40 mM DTT, 1 mM EDTA, 10% [w/v] sucrose,

10 mg/mL pyronine Y, and 2% [w/v] SDS) for 10 min at 508C, subjected to

SDS-PAGE (7%gel), and then transferred to an Immobilon polyvinylidene

difluoridemembrane (Millipore). Themembranewas treatedwithBlocking

One (Nacalai Tesque) for blocking, then incubated with primary anti-

bodies and subsequently with the secondary horseradish peroxidase–

conjugated anti-rabbit antibodies using standard procedures. The band

was visualized by chemiluminescence (Perkin-Elmer). Antisera used for

immunodetection were against PGP4, PM Hþ-ATPase, multicompart-

ment Hþ-PPase AVP1, and endoplasmic reticulum BiP from Arabidopsis.

Immunohistochemical Localization of PGP4

Seedlings were grown on 1% (w/v) phytoagar plates, one-quarter MS

basal salts, pH 4.85, and 1% sucrose. Immunohistochemical localiza-

tions and microscopy were as described previously (Geisler et al., 2005).

The antibody dilutions were 1:800 and 1:1200 for anti-PGP4 antisera.

Fluorescent staining was imaged by confocal laser-scanning micros-

copy. Indirectly visualized signals of the fluorescein isothiocyanate–

conjugated antibody are indicated in green. A confocal laser-scanning

microscope (Eclipse 800; Nikon) equipped with an argon laser (488 nm;

Bio-Rad) was used for immunofluorescence imaging. A green HeNe laser

(543 nm, 1.4 mW) and a red laser diode (638 nm, 5 mW) were used for

autofluorescence detection.

Isolation of pgp4Mutants

For identification of mutant lines carrying T-DNA insertions in the PGP4

gene, five T-DNA insertion lines available through the Arabidopsis stock

centers at Ohio State University (ABRC) and the University of Nottingham

(Nottingham Arabidopsis Stock Centre) were screened using the gene-

specific primers PGP4-int-Fw (59-CAGAGGAAACAGCCGCC-39), PGP4-

int-Rv (59-GCTACTTGGCTTGCTTCCCCGTAC-39), pgp4-3 forward

(59-CGAAAAGCCCAATAACGATTT-39), pgp4-3 reverse (59-CCTGAAG-

TACCCGAGCTGCAA-39), pgp4-4 forward (59-TCTGCAACAATGCAATC-

ACCG-39), and pgp4-4 reverse (59-CAGCGCTGATGCAAAGGTAAAC-39).

PGP4 Catalyzes Auxin Transport in Roots 2935

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PCR was performed using these primers in combination with LBb1

(59-GCGTGGACCGCTTGCTGCAACT-39) or LBa1 (59-TGGTTCACGTAG-

TGGGCCATCG-39), which anneals to the left border of the T-DNA

insertion, according to the protocol published on the Internet (http://

signal.salk.edu/tabout.html). We verified three homozygous T-DNA

insertional lines: pgp4-1 (SALK_063720), pgp4-3 (SALK_067653), and

pgp4-4 (SALK_088311).

Production of Recombinant Baculovirus

The recombinant donor plasmids were used to transform Escherichia

coli–competent DH10Bac cells (Invitrogen), which contained the parent

bacmid and a helper plasmid. Recombinant bacmids were selected on

Luria-Bertani plates containing 50 mg/mL kanamycin, 7 mg/mL gentami-

cin, 10 mg/mL tetracycline, 100 mg/mL X-Gluc, and 40 mg/mL isopro-

pylthio-D-galactoside. Sf9 cells were transfected with the purified

recombinant bacmids using Cellfectin reagent (Invitrogen). Three days

later, supernatant was recovered and used to infect fresh Sf9 cells.

Finally, amplified virus supernatants were prepared after two cycles of

this infection procedure. Their titer was determined and the virus was

stored at 48C. Sf9 cells were infected at a cell density of 0.63 106 cells/mL

in 25-cm2 tissue culture flasks. Cells were collected and disrupted via

Dounce homogenization to prepare membranes that contain the re-

combinant PGP4.

Photoaffinity Labeling of ABC Proteins with 8-Azido-ATP

Ten micrograms of membrane proteins from Sf9 cells was incubated in

a buffer mixture composed of 10 mM 8-azido-[a-32P]ATP (specific

activity, 12.5 Ci/mmol; Affinity Labeling Technologies), 2 mM ouabain,

0.1 mM EGTA, 3 mM MgSO4, 40 mM Tris-Cl, pH 7.5, and 0.2 mM

orthovanadate in a total volume of 8 mL for 10 min at 378C (Senior et al.,

1995). The reactions were stopped by the addition of 400 mL of ice-cold

TGMbuffer (40mMTris-Cl, pH 7.5, 0.1mMEGTA, and 1mMMgSO4), and

the membrane proteins were sedimented by centrifugation (15,000g,

10 min, 48C) to separate unbound ATP. Pellets were washed with fresh

ice-cold TGMbuffer, then irradiated with UV light at 254 nm (5.5mW/cm2)

in 8 mL of TGM buffer for 5 min on ice. Samples were electrophoresed on

a 7% SDS-polyacrylamide gel and autoradiographed. The radioactivity

trapped by ABC protein was analyzed with the radioimaging analyzer

BAS 1800 (Fuji Film).

Whole Plant Auxin Transport and Uptake Assays

Basipetal auxin transport assays in shoot tissues were performed as

described previously (Geisler et al., 2003). For root transport assays,

intact light-grown Arabidopsis seedlings were treated with a 0.1-mL

microdroplet of 1 mM auxin at the root apical meristem using techniques

described by Geisler et al. (2005), and root segments of 2 mm were

collected at 2, 4, and 6 mm from the root tip.

Root auxin uptake assays were performed as described by Murphy

et al. (2000) except that incubations used 2-mm root tip sections and

[3H]IAA as in transport assays. Sections were collectedwhole after 20min

and washed three times in 100 mM cold IAA before scintillation counting.

HeLa Cell Assays

PGP4 was expressed in mammalian HeLa cells using a vaccinia virus

cotransfection system as described previously (Geisler et al., 2005). Full-

length PGP4 cDNA was subcloned into the multiple cloning site of the

pTM1 vector (Hrycyna et al., 1998). For pTM1-PGP4, a PGP4 PCR

fragment containing XmaI-XmaI restriction sites was generated using the

following primers: PGP4 59, 59-TCCCCCGGGGCATGGCTTCAGA-

GAGCGGC-39; and PGP4 39, 59-CGCCCCGGGAGCGTAATCTGGTACG-

TCGTAAGAAGCCGCGGTTAGAT-39. Assays for the accumulation of

radiolabeled substrates were performed according to the method de-

scribed by Geisler et al. (2005). For inhibitor studies, cells were incubated

with radiolabeled IAA in the presence of 10 mM NPA, 200 nM quercetin,

1 mM cyclosporin A, or 5 mM verapamil.

Flavonoid Localization in pgp4

Seedlings were grown on 0.253 MS, 1% phytoagar plates and vertical

mesh transfer (Murphy and Taiz, 1995). Four-day seedlings were stained

with diphenylboric acid 2-aminoethyl ester and imaged using epifluor-

escence microscopy as described previously (Murphy et al., 2000; Peer

et al., 2001).

Auxin Quantitations

Quantitations of auxin in seedling tissues were performed as described

previously (Geisler et al., 2005).

Root Gravitropism Assay

Seedlings were grown on half-strength MS medium with 1% (w/v)

phytoagar, pH 4.85, for 5 d. Plates were kept in a vertical position. After

reorienting the plates by 908, the root tip position was marked every 3 h

over a 15-h time period, and again at 27 and 30 h. The angles of curvature

were measured with the Scion Image Beta 4.02 program (Scion), and the

data were analyzed by Microsoft Excel.

Quantitative Real-Time PCR

Seedlings were grown for 5 d on half-strength MSmedium, pH 5.8, under

16 h of light and then treated with 1 mM IAA, kinetin, or abscisic acid.

Whole seedlings, shoots, and roots were harvested for RNA isolation at 0,

2, 4, 6, 8, and 12 h after treatment. RNA isolation and quantitative real-

time PCR were performed as described previously (Peer et al., 2004)

except that 25 nM fluorescein was added for normalization. The primers

used were PGP4 forward (59-AAATGCGGATATGATCGCTG-39), PGP4

reverse (59-TGAACGACGTTTCCGTCAAT-39), b-tubulin forward (59-TGG-

GAACTCTGCTCATATCT-39), and b-tubulin reverse (59-GAAAGGAAT-

GAGGTTCACTG-39). The primer efficiencies forPGP4 and b-tubulinwere

equal (1.95 and 1.96, respectively).

Accession Numbers

Sequence data for the genes and mutants used in this study can be

found in the GenBank/EMBL data libraries under the following acces-

sion numbers: PGP4 (At2g47000), PIN1 (At1g73590), PIN2 (At5g57090),

b-tubulin (At5g12250), pgp4-1 (SALK_063720), pgp4-3 (SALK_067653),

and pgp4-4 (SALK_088311).

Supplemental Data

The following materials are available in the online version of this article.

Supplemental Table 1. Root Lengths of Wild-Type, pgp4-1, pgp4-3,

and pgp4-4 7-d Seedlings.

Supplemental Figure 1. Regulation of PGP4 and PGP21 Gene

Expressions by Chemical Stresses.

Supplemental Figure 2. Complementation of pgp4-1.

Supplemental Figure 3. PIN2 Localization in pgp4-1 and PGP4OX.

Supplemental Figure 4. PIN1 Localization in pgp4-1 and PGP4OX.

Supplemental Figure 5. Flavonol Accumulations in pgp4.

2936 The Plant Cell

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ACKNOWLEDGMENTS

We thank Markus Geisler, Enrico Martinoia, Dan Lewis, and Edgar

Spalding for discussions of the data and sharing their data with us

before publication. We thank Malcolm Bennett for helpful discussions.

We thank Jiri Friml and Klaus Palme for PIN1 antisera. We thank M.

Boutry (Universite Catholique de Louvain) for providing anti-Hþ-ATPase

antisera, N. Koizumi (Nara Institute of Science and Technology) for

providing anti-BiP antisera, and M.H. Sato (Kyoto University) and M.

Maeshima (Nagoya University) for anti-Hþ-PPase antisera. We thank the

Salk Institute Genomic Analysis Laboratory for providing the sequence-

indexed Arabidopsis T-DNA insertion mutants. The pGWB vectors and

A. tumefaciens GV3101 (pMP90) were generous gifts from T. Nakagawa

(Shimane University) and T. Shikanai (Kyushu University), respectively.

Funding for this project was provided by the Ministry of Education,

Culture, Sports, Science, and Technology of Japan (Grants 15031217

and 00L01605 to K.Y.) the Uehara Foundation (to K.Y.), and the National

Science Foundation (to A.S.M.).

Received July 6, 2005; revised September 22, 2005; accepted

September 27, 2005; published October 21, 2005.

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PGP4 Catalyzes Auxin Transport in Roots 2939

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DOI 10.1105/tpc.105.035816; originally published online October 21, 2005; 2005;17;2922-2939Plant Cell

Sato and Kazufumi YazakiBandyopadhyay, Srinivas N. Makam, Ok Ran Lee, Elizabeth L. Richards, Angus S. Murphy, Fumihiko

Kazuyoshi Terasaka, Joshua J. Blakeslee, Boosaree Titapiwatanakun, Wendy A. Peer, Anindita Rootsthaliana

ArabidopsisPGP4, an ATP Binding Cassette P-Glycoprotein, Catalyzes Auxin Transport in

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