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
Dr Tony Pinkerton is currently head of medicinal chemistry for the Conrad Prebys Center for Chemical Genomics, which is the early stage drug discovery center at the Sanford-Burnham Medical Research Institute (SBMRI). Tony received his B.S. (1995) degree in Chemistry from UC San Diego, was a Fulbright Scholar at ETH Zurich (1995-1996, with Professor Dieter Seebach) and obtained his Ph.D. (2001) from Stanford University (with Professor Barry M. Trost). Prior to joining SBMRI in 2010, Tony spent 10 years in industry at Merck Research Laboratories, Kalypsys, and Ardea Biosciences working on a wide range of targets and therapeutic areas.
09:00
Sharing Compound Collections: UCB's First Experiences from the European Lead Factory
Dr Jeremy DAVIS
UCB, Slough, United Kingdom
Jeremy Davis is Director of Hit Discovery and Enabling Technologies at UCB with 20 years’ experience as a medicinal chemist in the Biotech/ Pharmaceutical industry. He obtained his PhD from Southampton University researching the application of organozirconium complexes to organic synthesis. He joined Celltech as a bench chemist in 1993 and has worked on a diverse range of protein targets, but with a strong bias towards structure-based drug design across immunology, inflammation and oncology disease areas. His current role is leading hit discovery at UCB to identify small molecule leads for the Immunology and CNS therapeutic areas. He also is responsible for a technology group focused on developing advanced NMR and Mass Spectrometry applications for protein-ligand complexes. More recently research at UCB has focused on antibody-guided identification of small molecule modulators of protein-protein interactions (Lawson; Nature Rev. Drug Disc., 2012, 11, 519-525). Jeremy is the project lead representing UCB in the European Lead Factory.
09:30
Privileged Structures Unlocking Therapeutic Target Families
Dr Gerhard MÜLLER
MERCACHEM, Heidelberg, Germany
Gerhard Müller received his PhD with Prof. Horst Kessler from the Technical University of Munich in 1993 on bioactive RGD peptides. From 1993 to 1995 he worked at Glaxo’s research site in Verona, Italy, before he joined Bayer AG in Germany. In 2001, he took a Section Head Medicinal Chemistry position at Organon bv, where he was responsible for all Lead Finding activities addressing a variety of disease areas and target classes. In 2003 he became Chief Scientific Officer of Axxima Pharmaceuticals in Munich, Germany, later he held the VP Research position at GPC Biotech AG where he headed a portfolio of lead finding and optimization programs within oncology. Since 2011 Gerhard is in charge of all medicinal chemistry activities at Mercachem bv, Nijmegen, working across numerous therapeutic areas. Gerhard has published and co-authored more than 75 scientific publications and patents.
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
Ron Dror is an Associate Professor of Computer Science and, by courtesy, Molecular and Cellular Physiology at Stanford University. Dr. Dror employs a broad range of computational methods to study the spatial organization and dynamics of biomolecules and cells. Before joining Stanford, Dr. Dror served as second-in-command of D. E. Shaw Research, a hundred-person company, where he focused on high-performance computing and biomolecular simulation (part of a project highlighted by Science as one of the top 10 scientific breakthroughs of 2010). Dr. Dror earned a PhD in Electrical Engineering and Computer Science at MIT and an MPhil in Biological Sciences as a Churchill Scholar at the University of Cambridge.
11:00
Towards 3rd Generation Antihistamines: Fact or Fiction?
Prof. Rob LEURS
VU UNIVERSITY AMSTERDAM, Amsterdam, The Netherlands
Professor Rob Leurs studied Medicinal Chemistry at VU University Amsterdam and graduated in 1987. He performed his PhD research on G-protein coupled receptors and obtained his PhD degree from VU University in 1991. As a postdoctoral fellow at INSERM in Paris, he was involved in the cloning of genes encoding histaminergic and serotonergic receptors. In 1993, he was awarded with a 5-year fellowship of the Royal Netherlands Academy of Arts and Sciences.Rob Leurs was appointed as assistant and full professor of the Division of Medicinal Chemistry in respectively 1998 and 2000. From 2003 to 2005, he was one of the two scientific directors of the Leiden-Amsterdam Center of Drug Research. From 2005 to 2008, he was member of the executive board of the Top Institute Pharma. Professor Leurs served as director of the Department of Chemistry and Pharmaceutical Sciences in 2006 and as vice-dean of the Faculty of Science from 2007 until 2010. He was awarded the Galenus Research Prize in 1997, the Organon Award for Pharmacology in 2000, a Pfizer Academic Award and a STW/NWO Pionieer grant both in 2001. Moreover, the research group was selected as one of the Dutch center of excellence in Chemistry in 2014 and awarded a 2 M€ TOP-PUNT grant of the Dutch foundation for Chemical Sciences.
Professor Leurs is currently involved in research on G-protein coupled receptors, with specific emphasis on ligands and receptor proteins for histamine and chemokines and in the area of fragment based drug discovery on a variety of targets, including parasitic phosphodieasterases. Moreover, he is co-founder of Griffin Discoveries, a company that is valorizing the G-protein coupled receptor expertise and is currently involved in the discovery and development of GPCR receptor ligands.
Currently he has published 300 > papers and book chapters with >11000 citations (h-index = 56)
11:30
The Design of mGlu2 Negative Allosteric Modulators for the Treatment of Neuropsychiatric Disorders
Dr Michiel VAN GOOL
JANSSEN R&D, Toledo, Spain
Michiel Van Gool got his chemistry degree at the University of Ghent in 1994, where he started his PhD research on the Total Synthesis of Vitamine D3 analogues, under the supervision of Prof. M. Vandewalle and Prof. P. De Clercq. After obtaining his PhD degree in 1999 he moved to the Autonoma University of Madrid, Spain as a postdoctoral researcher in the supramolecular chemistry group of J. de Mendoza working on chiral bicyclic guanidiniums. Then in 2002 he joined the Neuroscience Medicinal Chemistry team of Janssen in Toledo, Spain. The current focus of this team is the discovery of assets for neurodegenerative diseases. Currently Michiel is Chemistry Team Leader of the mGlu2 NAM project.
12:00
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
Professional Experience:
2013-present: Professor of Clinical Chemistry, University Medical Center Hamburg-Eppendorf, Hamburg, Germany. Shared appointment and dual affiliation with Karolinska Institute and University Hospital
2009-present: PI at the Center of Molecular Medicine, CMM, Karolinska Institute, Stockholm Sweden
2008-present: Professor of Clinical Chemistry, Chair of Division, Karolinska Institute and Hospital, Stockholm Sweden
2005-2008: Assistant Professor and senior consultant in Laboratory Medicine, University of Würzburg, Germany
2002-2005: Docent and independent Juniorgroup-leader, University of Würzburg, Germany
Honors and Awards:
2013: Investigator Recognition Award for Contributions to Haemostasis from the International Society on Thrombosis and Haemostasis (ISTH), Amsterdam, the Netherlands
2011: Theodor Naegeli Award, Basel, Switzerland
2007: Alexander Schmidt Award and Lecture of the Society for Thrombosis and Hemostasis research, GTH
2004-present: Chair and Co-chain of the SSC subcommittee of the ISTH on Factor XI and the plasma contact system
2005: Gábor-Szász Award of the German Society for Clinical Chemistry and Laboratory
2002: Ivar-Trauschold Award and Lecture of the German Society for Clinical Chemistry
Reviewer: European Research Council (ERC), German Research Society (DFG), Science Foundation Ireland, Swiss National Science Foundation, and several other distinguished foundations; Journals: Cell, Nature Medicine, Journal of Experimental Medicine, Journal of Clinical Investigation, Blood, Journal of Immunolology, The Journal of Biological Chemistry, Arteriosclerosis, Thrombosis, and Vascular Biolology, Proceedings of the National Academy of Sciences journal, Journal of Thrombosis and Haemostasis
Editorial work: Section Editor: Thrombosis and Haemostasis, (2010-). Editorial Boards: Hämostasiologie, (2013-); Thrombosis Research (2014-)
14:45
Structure-Based Design of Inhibitors of Factor XIa
Dr James CORTE
BRISTOL MYERS SQUIBB, Princeton, United States
Dr. James Corte is currently a Principal Scientist at Bristol-Myers Squibb Pharmaceutical Company. Jim received his B.S. (1992) degree in Chemistry from Eckerd College and his Ph.D. (1999) degree in Organic Chemistry from Stanford University under the direction of Professor Barry M. Trost. His graduate work focused on the total synthesis of (+)-saponaceolide B. Jim joined the Medicinal Chemistry Department of Bristol-Myers Squibb in 1999. During his career, Jim has worked on many targets in the therapeutic areas of osteoporosis and thrombosis which included estrogen receptor beta modulators, calcium-sensing receptor antagonists, nonsteroidal progesterone receptor agonists, factor Xa inhibitors and factor XIa inhibitors. He has authored and co-authored over 30 scientific publications and patents.
15:15
Vorapaxar Discovery and Clinical Benefits
Dr Patrick ANDRE
MERCK & CO., Kenilworth, United States
Dr. Patrick Andre is Principal Scientist in the Thrombosis-Cardiometabolic department at Merck Research Laboratories. Prior to joining Merck in April 2013, he was Senior Director Biology at Portola Pharmaceuticals (South San Francisco, CA, USA).
Dr. Andre is a former Research Fellow in Pathology at Harvard Medical School. He earned his PhD at the University of Paris VII, Denis Diderot (France). He has authored more than 40 publications and reviews and is co-inventor on more than 10 patents in the field of thrombosis, coagulation and inflammation.
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
Roberto Pellicciari is Professor of Medicinal Chemistry in the Department of Pharmaceutical Sciences of the University of Perugia (Italy) and President and Scientific Director of TES Pharma (Perugia). Prior to that he has been pre-and postdoctoral fellow in the Istituto Superiore di Sanità, Rome, Visiting Professor in the Universidad de Carabobo, Valencia, Venezuela, Research Associate in the Department of Chemistry, Bloomington Indiana, and Visiting Professor in the Department of Chemistry, University of California at San Diego (UCSD), La Jolla. Prof.Pellicciari has been Director of the School of Medicinal Chemistry (ESMEC) of the Italian Chemical Society (SCI), President of the Italian Division of Medicinal Chemistry (SCI), President of the European Federation of Medicinal Chemistry (EFMC). Prof.Pellicciari is author or co-author of over 300 papers and 50 patents, has given seminars in important international congresses and institutions and has been the recipient of several awards. His main research fields have been the development of new synthetic methodologies and their applications to the synthesis of natural products, the design and synthesis of novel agents for CNS and liver and metabolic diseases.
16:45
Science, Business & Innovation in Medicinal Chemistry
Prof. Iwan DE ESCH
VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands
Prof. Dr. Iwan de Esch did his PhD research at the Department of Pharmacochemistry, VU University Amsterdam, The Netherlands. In 1998, he became research associate at the Drug Design Group of the University of Cambridge. He is a co-founder of De Novo Pharmaceuticals (2000) where he worked as a group and project leader. He returned to academia in 2003 and is now professor at the Medicinal Chemistry Department of VU University Amsterdam. The group focuses on two research lines, namely G-protein-coupled receptors (GPCRs) and Fragment-Based Drug Design (FBDD). Prof. de Esch is co-founder of IOTA Pharmaceuticals Ltd (2007) and Griffin Discoveries BV (2009). In 2011, he was awarded the Galenus Research Price for his work on FBDD.
17:15
Panel Discussion - Introduction by the moderator
Panellist 1
Prof. Christa MÜLLER
UNIVERSITY OF BONN, Bonn, Germany
Christa Müller studied pharmacy at the University of Tübingen, Germany, and received her Ph.D. in Pharmaceutical/Medicinal Chemistry from the same university. After a postdoctoral stay with John W. Daly (1989-1990 and 1992) at the Laboratory of Bioorganic Chemistry, National Institutes of Health, in Bethesda, Maryland, USA, she completed her habilitation thesis at the University of Tübingen in 1994, and became Associate Professor of Pharmaceutical Chemistry at Würzburg University in the same year. Since 1998 she is full professor of Pharmaceutical Chemistry at Bonn University. She is a co-founder of the Pharma-Center Bonn (www.pharmazentrum.uni-bonn.de), and has >300 publications in the field of medicinal chemistry and pharmacology (H-index >40). Her scientific interests are focused on the medicinal chemistry and molecular pharmacology of purine-binding membrane proteins (purine receptors, ectonucleotidases) and lipid-activated orphan G protein-coupled receptors. Disease indications include neurodegenerative and inflammatory diseases and cancer. Her activities are ranging from basic research to collaborative drug development projects with pharma industry partners.
http://mueller-group.pharma.uni-bonn.de
Panellist 2
Prof. Chas BOUNTRA
UNIVERSITY OF OXFORD, Oxford, United Kingdom
Chas Bountra is Head of the Structural Genomics Consortium (SGC), Professor of Translational Medicine, and an Associate Head of Medical Sciences at the University of Oxford.
Prior to coming back to Oxford, Chas was Head of Biology at GSK.
He has therapeutic expertise in neuro-psychiatry, gastro-intestinal, inflammation and cancer, and “know- how” of all stages of the drug discovery and development process. He has given over 300 invited lectures. In 2012 he was voted one of the “top innovators in the industry”.
His current research is aimed at determining the 3D X ray structures of novel proteins, generating novel small molecule inhibitors, using these to dissect disease networks and hence identifying new targets for drug discovery.
Panellist 3
Prof. Dennis LIOTTA
EMORY UNIVERSITY, Atlanta, United States
Dr. Liotta is the Samuel Candler Dobbs Professor of Chemistry at Emory University and the Executive Director of the Emory Institute for Drug Development. He did his doctoral studies at the City University of New York and postdoctoral studies at the Ohio State University. Dr. Liotta’s research focuses on the discovery and development of novel antiviral, anticancer and anti-inflammatory therapeutic agents. He is one of the leaders of the Emory team that discovered the antiviral drug, Emtriva (emtricitabine), which was approved for treating HIV in July 2003. Emtriva is a component of the ground breaking, once a day, triple combination therapy, Atripla, which is now universally accepted as the drug combination of choice for treating HIV infected patients. In addition, he is the inventor of record for several clinically important antivirals, including Epivir, Racivir and Elvucitabine. He is also the lead inventor of Q-122, a safe, orally available clinical agent for controlling hot flashes in post-menopausal women.
Panel Discussion with Roberto Pellicciari, Iwan de Esch, Christa Müller, Chas Bountra and Dennis Liotta, and discussion with the audience
18:15
20:00
Banquet at Grand Café Horta