| Sunday September 13, 2015 |
| 15:00 | Optional excursions |
|
| 18:30 | Welcome reception with Belgian Beers |
|
| Monday September 14, 2015 |
| 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, Notre Dame, 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 |
Mr 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 |
|
| Tuesday September 15, 2015 |
| 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, Heidelberg, 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 |
|
| Wednesday September 16, 2015 |
| 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
(ITEOS THERAPEUTICS, 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, Toulouse, France) |
| 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, Loos, France) |
| 16:45 | Closing remarks |
|
