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DIPARTIMENTO DI FARMACIA-Claudia MARTINI-

THE MISSION: Therapeutic/diagnostic/theranostic agent development

New chemicalentitiesChemical

synthesis

Biologicalactivity

Computer-aided Drugdesign

Pharmacokineticstudies

Extraction from natural sources

LEAD OPTIMIZATION

IP protection (patent)

Drug/Diagnosticcandidates

Out-licensing Pre-clinicaldevelopment

Clinicaldevelopment

PharmaceuticalTechnology

Formulative studies

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Ala394

Glu343

Met345

KEY ACTIVITIES:Computer-Aided Drug Design

Receptor–based approach

Pharmacophore‐based approach

Ligand–based approach

S

NO

H3CO

(CH2)2N(CH3)2

N

N

N

O

(CH2)2N(CH3)2N S

NN

H3C

H2NO2S

N

Cl

Cl

NO

ON

NN

NH(CH2CH2)2N(CH3)2

H

N

N

NN

OCl

N S

NN

NH2

Cl

OCH3

N

NN N

HNO

OCH3Cl

O

N N O

O

NH

F

N

O

NH

O

F

H3CO

N

O

NH

O

F

N N O

O

NH

O

N

O

H3CO

OCH3

NH

O

N N NH

SOCH3

CH3

NBr NH

O

O

OOBn

OH2N

O

H2NOO

H2NOiPr

O

O

BnO

OBnO

AcHN

OAc

OAc

OO

AcHN

OAc

OAc

OiPr

OOH

O

HOHO

HO

O

HOH2N

HO

NH2

HNMe

AcO

OAc

OAc

BnO

HO

O

N

Ms

CH(CO2Me)2BnO

OH

OOH

O

HOHO

HO

O

HOHO

HO

N3

KEY ACTIVITIES:Chemical synthesis

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INTRACELLULARSIGNALINGPATHWAYS

CELL SURVIVAL,DEATH AND DIFFERENTIATION

PHARMACOLOGICALPROFILE

DRUG-TARGETINTERACTION

•Nucleic acids•Proteins•Enzymes•Kinases

Biochemical and Pharmacological

tests

KEY ACTIVITIES: Drug target identification and validation

PHARMACOKINETICS STUDIES IN VIVO, IN VITRO, EX VIVO

OPTIMIZATION OF PHARMACOKINETIC PROPERTIES:

-Improvement of biodisponibility- Limitation of first pass metabolism

- Increase of the half-life

PHARMACODYNAMIC STUDIESIN VIVO, IN VITRO,

EX VIVO

OPTIMIZATION OF PHARMACODYNAMIC PROPERTIES:

- Limitation of the toxicity- Improvement of the efficacy

- Improvement of the compliance

KEY ACTIVITIES: Optimization of drug properties

OPTIMIZATION OF

PHARMACEUTICAL FORMULATION

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RESULTS: Research projects, Pubblications and Patents(2010‐2014)

Tech-transfer ability

� 5 International projects funded (4x EU, 1x US-NIH)

� 10 national projects funded (9 PRIN, 1 FIRB)

Fundraising ability

� Scientific publications/year = 124 (average value over the past 4 years)

� 11 International patents

� 10 National patents

� 2 Products on the market

Productivity

� 3 outlicensed patents

� 1 spinoff

� numerous research contracts(with external companies/agencies)

� Tumors

� Neurodegenerative Diseases

� Osteoporosis

MAIN RESEARCH AREAS:

Modified from “Evolution of the Molecular Biology of Brain Tumors and the Therapeutic Implications. 2013. Terry LichtorEditor, ISBN 978-953-51-0989-1, InTech Publisher. Chapter 6, An Q. Dang et al., pag 167-200

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BASIC RESEARCH FOCUS ON NOVELTY

TRANSLATIONAL RESEARCH FOCUS ON EFFICACY AND SAFETY

Others Applications I:solvents and catalysts

1) Biomass transformation using Ionic Liquids: green fuels,building blocks or polymers.

2) Algae cell lysis using Ionic Liquids: biodiesel synthesisand other by-products recovery.

3) From fatty acids methyl esters to lubricants using IonicLiquids as solvents-catalysts.

Contract # 3500032679Research project: Poloptel

Contract PI0007

Contract # 3500024371IL

1 grant from Regione Toscana

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Others Applications II

MIMI-ELISA TESTING METHOD

1) New tests for detection of protein-proteininteractions.

2) Proteomic approach in disease diagnosis.

FIRB 2010Unipi PhD Plus andInternational MBA jointproject

3) MMP selective inhibitors as probes for Optical Imaging or as PET tracers.

B CA B C

24 h

WO 2010010079;WO 2008113756EP 2147684 ;EP 1972617;TO2006A000575;WO2008015139

1 grant from Regione Toscana

2012

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1940

2012