FMC 2015

Frontiers in Medicinal Chemistry

 Antwerp, Belgium    September 14-16, 2015

Programme


15:00

Optional excursions

18:30

Welcome reception with Belgian Beers

08:00

Registration

08:45

Welcome address

Plenary Session

Session Chair

Prof. Koen AUGUSTYNS
UNIVERSITY OF ANTWERP, Antwerp, Belgium

09:00

Discovery and Development of Bedaquiline: A Rocky Road

Prof. Koen ANDRIES
JANSSEN PHARMACEUTICA NV, Beerse, Belgium

09:45

Regulated Necrosis: Disease Relevance and Therapeutic Opportunities

Prof. Peter VANDENABEELE
UNIVERSITY OF GHENT, Ghent, Belgium

10:30

Coffee break and Exhibition

11:00

The Role of CXCR4 Modulators in Controlling HIV Entry, Stem Cell Mobilisation and Certain Types of Cancer

Prof. Dennis LIOTTA
EMORY UNIVERSITY, Atlanta, United States

11:45

Lunch and Exhibition

Session 1 - Molecular Chaperones and their Therapeutic Potential

Session Chair

Prof. Brian S. J. BLAGG
UNIVERSITY OF KANSAS, Lawrence, United States

13:00

Story of the Hsp27 Inhibitor Apatorsen

Dr Palma ROCCHI
MARSEILLE CANCEROLOGY RESEARCH CENTER, Marseille, France

13:30

Targeting Protein-Protein Interactions in the Heat Shock Protein 70 (Hsp70) Complex

Prof. Jason GESTWICKI
UNIVERSITY OF CALIFORNIA, San Francisco, United States

14:00

Update on Hsp90 Inhibitors as Cancer Therapeutics

Dr Weiwen YING
SYNTA PHARMACEUTICALS, Lexington, United States

Oral Communications

14:30

The Discovery of Chemical Probes for Bromodomain Containing Proteins
Prize winner EFMC-YMCS 2014

Dr Duncan HAY
EVOTEC, Abingdon, United Kingdom

14:45

The Discovery Of A New Validated Target For Tuberculosis Via Phenotypic Screening

Ms Raquel FERNANDEZ
GLAXOSMITHKLINE, Tres Cantos, Spain

15:00

Measuring The Dynamics Of Target Engagement Inside Cells Using Bret

Dr Matthew ROBERS
PROMEGA, Madison, United States

15:15

Outcome EFMC video competition

15:30

Coffee break and Exhibition

16:00

Poster Session 1
(posters with odd numbers)

17:30

City Tour

Session 2 - Unexplored Chemical Space: Experiences from the European Lead Factory and the NIH

Session Chair

Dr Peter MOLENVELD
MERCACHEM-SYNCOM, Nijmegen, The Netherlands

08:30

Sanford-Burnham’s Experience with the NIH’s Molecular Libraries Program

Dr Anthony PINKERTON
SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE, La Jolla, United States

09:00

Sharing Compound Collections: UCB's First Experiences from the European Lead Factory

Dr Jeremy DAVIS
UCB, Slough, United Kingdom

09:30

Privileged Structures Unlocking Therapeutic Target Families

Dr Gerhard MÜLLER
MERCACHEM, Martinsried, Germany

10:00

Coffee break and Exhibition

Session 3 - Emerging Advances in GPCR Research

Session Chair

Dr Laurent PROVINS
UCB, Braine-l'Alleud, Belgium

10:30

Revealing The Structural Basis for GPCR Drug Action through Atomic-Level Simulation

Prof. Ron DROR
STANFORD UNIVERSITY, Stanford, United States

11:00

Towards 3rd Generation Antihistamines: Fact or Fiction?

Prof. Rob LEURS
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands

11:30

The Design of mGlu2 Negative Allosteric Modulators for the Treatment of Neuropsychiatric Disorders

Dr Michiel VAN GOOL
JANSSEN R&D, Toledo, Spain

12:00

Lunch and Exhibition

12:45

Poster Session 2
(posters with even numbers)

Session 4 - Novel Strategies for Anti-Thrombotic Therapy

Session Chairs

Dr Amjad ALI
MERCK & CO. INC., Kenilworth, United States
Dr Amy RIPKA
WUXI APPTEC, Cambridge, United States

14:15

Targeting Factor XII in Thrombosis and Inflammation

Prof. Thomas RENNE
KAROLINSKA INSTITUTET, Stockholm, Sweden

14:45

Structure-Based Design of Inhibitors of Factor XIa

Dr James CORTE
BRISTOL MYERS SQUIBB, Princeton, United States

15:15

Vorapaxar Discovery and Clinical Benefits

Dr Patrick ANDRE
MERCK & CO., Kenilworth, United States

15:45

Coffee break and Exhibition

Session 5 - Academic Drug Discovery (+ Panel discussion)

Session Chair

Prof. Henk TIMMERMAN
VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands

16:15

Translating Medicinal Chemistry Research into Targeted Therapeutics. Building on Academic Knowledge

Prof. Roberto PELLICCIARI
UNIVERSITY OF PERUGIA, Corciano, Italy

16:45

Science, Business & Innovation in Medicinal Chemistry

Prof. Iwan DE ESCH
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands

17:15

Panel Discussion - Introduction by the moderator

Panellist 1

Prof. Christa MÜLLER
UNIVERSITY OF BONN, Bonn, Germany

Panellist 2

Prof. Chas BOUNTRA
UNIVERSITY OF OXFORD, Oxford, United Kingdom

Panellist 3

Prof. Dennis LIOTTA
EMORY UNIVERSITY, Atlanta, United States

Panel Discussion with Roberto Pellicciari, Iwan de Esch, Christa Müller, Chas Bountra and Dennis Liotta, and discussion with the audience

18:15

End of Panel Discussion

20:00

Banquet at Grand Café Horta

Session 6 - Non-Small Molecules

Session Chair

Prof. Steven FIRESTINE
WAYNE STATE UNIVERSITY, Detroit, United States

08:30

High Affinity Bicyclic Peptides: Application to Payloads in Oncology

Dr Gavin BENNETT
BICYCLE THERAPEUTICS , Cambridge, United Kingdom

09:00

Exploring Macrocycles for Protein-protein Interaction Targets: the Discovery of Novel Bifunctional XIAP Antagonists

Dr Nick TERRETT
ENSEMBLE THERAPEUTICS CORPORATION, Kriens, Switzerland

09:30

Discovery and Optimisation of Bioactive Macrocycles from DNA-Encoded Libraries

Dr Patrick MCENANEY
THE SCRIPPS RESEARCH INSTITUTE, La Jolla, United States

10:00

Coffee break and Exhibition

Session 7 - Emerging Topics

Session Chair

Dr Pascal GEORGE
SCT & INDEPENDENT SCIENTIFIC EXPERT & ADVISER, Longvilliers, France

10:30

Discovery of Highly Efficacious Potentiators for the Treatment of Cystic Fibrosis

Dr Steven VAN DER PLAS
GALAPAGOS, Mechelen, Belgium

10:55

Discovery & Optimisation of Novel Antagonists to the Human Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders: From Hit to Clinic

Dr Hamid HOVEYDA
EUROSCREEN, Woluwe-Saint-Lambert, Belgium

11:20

Selective JAK1 Inhibitor for the Treatment of Autoimmune Diseases

Dr Michael L. VAZQUEZ
PFIZER, Cambridge, United States

11:45

Discovering A Potent Allosteric Kinase Modulator Employing A Computational And Synthetic Toolbox

Mr Edwin KROON
UNIVERSITY OF GRONINGEN, Groningen, The Netherlands

12:10

Lunch and Exhibition

Session 8 - Kinetics and Thermodynamics of Ligand Binding

Session Chair

Dr Matthias FRECH
MERCK, Darmstadt, Germany

13:15

Kinetics in Drug discovery - A Case for the Adenosine Receptors

Mr Dong GUO
LEIDEN UNIVERSITY, Leiden , The Netherlands

13:45

Drug Target Residence Time: HSP90, a Model to Gain Insight into the Molecular Mechanism of Binding

Dr Matthias FRECH
MERCK, Darmstadt, Germany

14:15

Novel JAK Inhibitors for Inhaled and Topical Delivery

Dr Peter JONES
PFIZER, Cambridge, United States

14:45

Coffee break and Exhibition

Session 9 - Rational Design of Non-Oral Drugs

Session Chair

Dr Jordi GRACIA
ALMIRALL, Sant Feliu de Llobregat, Spain

15:15

Inhaled PDE4 Inhibitors with Low Emetic Potential and Long Duration of Action for the Treatment of COPD

Dr Chris DE SAVI
ASTRAZENECA R&D, Boston, United States

15:45

A Novel Retinoic Acid Receptor Agonist for Dermatological Indications with Specific Design Parameters for Topical Administration to Manage Safety

Dr Claire BOUIX-PETER
GALDERMA R&D, Sophia-Antipolis, France

16:15

Locally-acting ROCK Inhibitors for the Treatment of Eye Diseases

Dr Olivier DEFERT
AMAKEM, Diepenbeek, Belgium

16:45

Closing remarks