custom peptide synthesis services

1

2

Outline

Market & Technology Trends

LifeTein Technology Portfolio

LifeTein Services

3

Synthetic Therapeutic Peptides

More than 60 synthetic therapeutic peptides under 50 amino acids in

size have reached the pharmaceutical market as APIs or generics.

4

Chemical Optimization

Strategies for Lead Peptide Optimization

Drug Discovery Today Volume 15, Numbers 1/2 January 2010

5

Technology Trends

Using Nitroalkanes as Acyl Anion

Equivalents

Microwave Synthesis

Green Chemistry for Synthesis

www.nature.com/doifinder/10.1038/nature09125

6

LifeTein Technology Portfolio

PeptideSynTM Platform

Provides high-yield

peptide synthesis

Combines SPPS and

LPPS for the highest

synthesis success rate

possible

Ensures shorter

turnaround

7

LifeTein Technology Portfolio

PeptideSynTM Ligation

Synthesizes long

peptides (up to 120

amino acids)

Ensures high yield and

short turnaround

8

LifeTein Technology Portfolio

A: H-MEDSTYYKASKGC-NH2

B: H-MEDST(PTyr)YKASKGC-NH2

C: H-PKYLQNTLKLATGMRNVPEKQTT-OH

D: H-MEDSTYYKASKGC-NH2

E: H-MEDST(PTyr)YKASKGC-NH2

F: H-PKYLQNTLKLATGMRNVPEKQTT-OH

9

LifeTein Services

Custom Peptide Synthesis Service

Custom Peptide Library Synthesis Service

Custom Polyclonal Antibody Service

Custom Monoclonal Antibody Service

10

LifeTein Services

Increases yields and reduces costs

Shortens production cycle

Combines the advantages of both solid and solution phase methods

Can scale up projects rapidly to over 100 kg

Avoids solubility problems for long segments in solution phase

Advantages of PeptideSynTM Technology

11

Peptide Synthesis Service

Peptide Length 5-120 amino acids

Peptide Scale From mg to kg

Peptide Purity Crude, desalted, >75%, >85%, >90%, >95%, 98%, and >99%

Peptide

Modifications 2-5 phosphorylation sites, methylation, acetylation, amidation, MAPs(2, 4 or 8 chains), more…

Peptide Labels FITC, Biotin, 5-FAM, Rhodamine, Dansyl, TAMRA, more…

Carrier Proteins KLH, BSA, OVA

Cyclic Peptides Amide cyclic peptide (head to tail, side chain), 1, 2, or 3 disulfide bond bridges

Analysis HPLC, MS, Amino Acid Analysis (AAA), solubility testing, microbial analysis, more…

Peptide Libraries Peptide sequence length of 5-20 amino acids, 48, 96 peptides

Others Free aliquots, spacers and linkers (Ahx, mini-PEG), more…

12

Free Aliquot Service

13

Case Studies

Cell Penetrating Peptides

Name Origin Sequence

Tat family

Tat (48-60) HIV-1 protein GRKKRRQRRRPPQQ

Oligoarginine Tat derivative Rn

Penetralia family

p-Antp Antermapedia homeodomain RQIKIWFQNRRMKWKK

plsl Igl-1 homeodomain RVIRVWFQNKRCKDKK

Chimeric CPPs

Transportan Galanin-mastoparan GWTLNSAGYLLGKINLKALAA

LAKKIL

14

Case Studies

Cell Penetrating Peptides

Attached to a CPP, therapeutic cargo is delivered to an intracellular target,

thus overcoming the entry restrictions set by the plasma membrane.

15

Case Studies

Chemically synthesized peptides have free amino and carboxyl termini.

N-terminal acetylation and C-terminal amidation reduce the overall charge of the peptide. This can

increase the stability of the peptide and its resemblance to the native protein.

N-Terminal Acetylation and C-Terminal Amidation

Both modifications are free of charge

16

Peptide Antigen Design

Continuous versus Discontinuous Epitopes?

17

Peptide Antigen Design

Sequence Length 8-20 amino acids

Peptide Purity • >75% for antibody generation,

• >90% for phosphorylated peptide antibody (recommended)

Peptide Solubility • Keep the hydrophobic amino acid content below 50%

• At least one charged residue for every five amino acids

Difficult Amino Acids

• Cys and Met can undergo rapid oxidation

• Avoid multiple Ser or Pro

• Avoid multiple or adjacent β-sheet forming amino acids: Glu, Iso, Leu, Phe, Thr, Tyr, Val

Carrier Proteins KLH, BSA, OVA

Multiple Antigenic Peptides (MAPs)

18

Custom Antibody Service

Peptide Antigen Antibody Services • Polyclonal Antibodies

• Monoclonal Antibodies

Phosphorylated-Peptide Antibody Services • Polyclonal Antibodies

• Monoclonal Antibodies

Methylated-Peptide Antibody Services • Polyclonal Antibodies

• Monoclonal Antibodies

AdjuBoosterTM Adjuvant Technology

19 More information, please visit www.lifetein.com

20

Contact Information

Let us be a partner to your growth!

LifeTein LLC

150 Maple Ave

South Plainfield, NJ 07080

USA

info@lifetein.com

1-732-444-3282

1-888-791-1618 (Toll Free)

1-888-791-1618 (Fax)