08:00
Registration & Welcome Coffee
09:00
RICT 2016 Opening
Prof. Patrick DALLEMAGNE
UNIVERSITY OF CAEN, Caen, France
Dr Luc VAN HIJFTE
SCT & NOVALIX, Nijmegen, The Netherlands
Prof. Pierre DENISE
UNIVERSITY OF CAEN, Caen, France
Session 1: Paul Ehrlich Award Lecture
Sponsored by Janssen Research & Development
Session Chairs
Mrs Magali MOTTE
JANSSEN R&D, Val de Reuil, France
Dr Luc VAN HIJFTE
SCT & NOVALIX, Nijmegen, The Netherlands
09:30
Paul Ehrlich Prize Lecture
Trip in Drug Discovery (PL01)
Prof. Jean-Daniel BRION
UNIVERSITÉ PARIS-SUD, Chatenay-Malabry, France
Jean-Daniel Brion is currently Professor of Medicinal Chemistry at the School of Pharmacy of the University Paris-Sud (Châtenay-Malabry) and mission head at the Institute of Chemistry of CNRS sincel four years. As pharmacist, he defended his PhD thesis in Medicinal chemistry in 1978, then passed the Aggregation of Pharmacy in 1983. In the same year, he was appointed as Full Professor at the university of Nantes. From 1989 to 1995, he was director of a medicinal chemistry division at Servier Research Institute at Suresnes (near Paris).
In 1995, Jean-Daniel Brion was appointed as Full Professor at the University of Paris-Sud. From 1998 to 2007, he was head of a joint research centre of CNRS (UMR CNRS 8076 BioCIS) at the Paris-Sud University. The activity of this unit is essentially centered on chemistry in natural products, new methodology development in organic and organometallic synthesis and medicinal chemistry. In recent years, he was appointed as director of the Federative Institute of Research (IPSIT, Institute Paris-South of Therapeutic Innovation) at the University of Paris-Sud, which gathers more than five hundred scientists, among them, there are chemists, biologists, clinicians and engineers.
Jean-Daniel Brion and Mouad Alami team is a member of research unity UMR 8076 BioCIS and a member of the Laboratory of Excellence in Research on Medication and Innovative Therapeutics (LabEx LERMIT) and it consists of more than twenty scientists.
Their group is involved in the design, synthesis, and evaluation of biologically active agents. Current therapeutic areas include mainly cancer, but also pulmonary arterial hypertension, epilepsy and neurodegenerative diseases. These projects require the development of synthetic methods and structure-activity studies aimed at improving the therapeutic efficacy of lead compounds, including natural products and hits from high throughput screening.
J.-D. Brion is the co-author of more than 200 scientific publications in peer-reviewed journals and co-inventor of 20 patents. He was also a co-author in the series of the handbook of Medicinal chemistry (AFECT, 7 volumes). He is also a member of the National Academy of Pharmacy and Chevalier de l’Ordre du Mérite.
10:30
Coffee break & Exhibition
Session 2: Target Identification
Session Chair
Mr Jean-Damien CHARRIER
VERTEX PHARMACEUTICALS, OXON, United Kingdom
11:00
Human Proteomes – from Basic Biology to Understanding Drug Action (PL02)
Prof. Bernhard KÜSTER
TECHNICAL UNIVERSITY MUNICH, Munich, Germany
Bernhard Kuster is a chemist by training and obtained is PhD in Biochemistry from the University of Oxford. He went on to do a PostDoc funded by an EMBO long-term fellowship at the EMBL in Heidelberg and the University of Southern Denmark in Odense. After seven years at the biotech firm Cellzome, he became full professor of Proteomics at the Technische Universität München in 2007 where he is also the Chair of the Department for Biosciences and Co-Director of the Bavarian Biomolecular Mass Spectrometry Center. Bernhard’s research focuses on mass spectrometry based proteomics and its application to chemical and systems biology.
11:45
Target Deconvolution Efforts Around Wnt Pathway Screen Reveal Parallel Mechanisms of Action for 1,2,3-Thiadiazole-5-Carboxamide Series (PL03)
Dr Andrew ZHANG
ASTRAZENECA, Waltham, United States
Andrew Zhang is a Senior Scientist in Chemical Biology within Discovery Sciences at AstraZeneca R&D Waltham.
His research field of interest is target deconvolution, using chemoproteomics as a primary method for identifying targets, profiling selectivity, and confirming engagement. Previously, he has conducted research at the interface between small molecules and antibodies, on small molecule immunomodulators as well as antibody-drug conjugates.
He obtained his Bachelors of Science at the University of California, Berkeley, and conducted PhD training with Professor David Spiegel at Yale University.
Prior to joining AstraZeneca, he spent one year in the Drug Discovery Program at the Ontario Institute for Cancer Research (Toronto, Canada) as a postdoctoral fellow.
12:30
13:30
Session 3: Chemical Biology
Session Chair
Dr Gordon TANG
ROCHE R&D CENTER (CHINA) LTD, Shanghai, China
15:00
Protein Modification: from Chemical Biology to Drug Discovery (PL04)
Prof. Edward TATE
IMPERIAL COLLEGE LONDON, London, United Kingdom
Edward Tate is Professor of Chemical Biology in the Department of Chemistry at Imperial College London. He completed his Ph.D. in organic chemistry at the University of Cambridge in the group of Prof. Steve Ley.
Following postdoctoral research in chemistry and biology on an 1851 Research Fellowship at Ecole Polytechnique and the Pasteur Institute in Paris, he moved to Imperial College London where he now leads a team of more than 40 scientists working on the design and application of chemical approaches to understand and manipulate living systems, with a particular focus on drug target discovery and validation.
He is a Fellow of the Royal Societies of Chemistry (FRSC) and of Biology (FRSB), and received the 2012 Wain Medal, the 2013 MedImmune Protein and Peptide Science Award, and the 2014 Norman Heatley Award in recognition of his group’s research in chemical biology and drug discovery.
15:45
A Role of SIRT2 in Cellular Response to Environmental Signals (PL05)
Dr Minoru YOSHIDA
RIKEN ADVANCED SCIENCE INSTITUTE (ASI), Saitama, Japan
Minoru Yoshida is Chief Scientist at RIKEN. He received his Ph.D. degree from the University of Tokyo in 1986, where he started mode of action studies of natural products. He identified histone dacetylase and Crm1 exportin 1 as the specific targets of trichostatin A (TSA) and leptomycin B (LMB), respectively, which greatly contributed to the field of epigenetics and nuclear transport.
After he was promoted to Associate Professor in 1995 in the University of Tokyo, he moved to RIKEN and started the Chemical Genetics Laboratory as Chief Scientist in 2002.
In 2013, he was also appointed as Group Director, Chemical Genomics Research Group at RIKEN CSRS. At RIKEN, he identified spliceostatin, the first inhibitor of pre-mRNA splicing, and many other unique compounds.
His major interest is the interface between chemistry and biology.
16:30
Coffee break & Exhibition
Session 4: Inflammation and Nociception
Session Chair
Dr Henning STEINHAGEN
APTUIT, Verona, Italy
17:00
The Discovery and Optimization of Benzimidzoles as Selective NAV1.8 Blockers for the Treatment of Pain (PL06)
Dr Alan BROWN
STRATIFIED MEDICAL, Deal, United Kingdom
In 1990 Alan joined Pfizer after completing his doctoral research with Ernie Colvin at the University of Glasgow.
He has worked as a medicinal chemist for over 25 years and has been involved in the discovery of multiple clinical development candidates across several therapeutic areas including pain, cardiovascular, allergy and respiratory, urogenital and sexual health and has also been involved in the discovery of candidates in several non-traditional areas of chemistry such as synthetic vaccines.
From 2011 to 2016 Alan was Head of Chemistry for Pfizer's Pain and sensory Disorders Research unit in Cambridge, UK.
Following the closure of that site earlier this year Alan has taken up the position of Director of Chemistry at Stratified Medical in London.
17:45
Optimization and Exploration of Bradykinin 1 Receptor Antagonists for Inflammation (PL07)
Dr Sven KÜHNERT
GRUENENTHAL GMBH, Aachen, Germany
Dr. Sven Kühnert is heading the department of Drug Discovery Technologies at Grünenthal GmbH since August 2015, being responsible for parallel synthesis, compound management, compound characterization, molecular modeling and discovery informatics.
In the previous 13 years he has worked as Medicinal Chemist and Research Project Leader on various targets mainly GPCRs and Ion-channels from the field of pain and inflammation.
His experience includes steering of contract research organizations and leading IT projects. He has more than 50 scientific publications and patents/applications pending.
He studied chemistry at the Eberhard Karls University in Tübingen, Germany, from where he also received a PhD in natural product synthesis in 2002.
18:30
20:30