RICT 2012 - Interfacing Chemical Biology and Drug Discovery

DNA Methylation Inhibitors In Cancer: Recent and Future Approaches

Dr Paola B. ARIMONDO

INSTITUT PASTEUR - CNRS, Paris, France
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Dr Paola B. ARIMONDO

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Head of the Unité de Service et de Recherche mixte CNRS-Pierre Fabre n°3388 – EtaC (Epigenetic Targeting of Cancer) After a training in Chemistry (Laurea in Chimica de l’Università degli Studi di Pisa (1995) and Ph.D. from the Scuola Normale Superiore, Italy (1999)) and in Biophysics (Ph.D. from the MNHN, Paris, France, 1999), I was appointed, in October 2001, researcher at the CNRS. My research is situated at the interface of chemistry and biology, with potential applications both in biology and in therapeutics. My main interest has been to develop a strategy to target at a specific DNA site a class of antitumor agents directed against human DNA topoisomerases I and II. We developed a pair of “DNA scissors” that cleave the DNA at oncogenes in cancer cells. This project has been the subject of the defense of my Habilitation à Diriger des Recherches in Chemistry at the Université Pierre et Marie Curie, in 2005. After a six-months sabbatical in 2005 in the Laboratory of Prof. Nick Cozzarelli at the University of California in Berkeley to acquire new knowledge and expertise, I started a new project for the development of an antitumor strategy aiming the epigenetic control of gene expression in cancers. Since January 1st, 2011, I am head of the Laboratory of Epigenetic Targeting of Cancer (ETaC), USR3388 CNRS-Pierre Fabre in Toulouse, France.

Sometimes You Just Have to Break the Rules ..

Dr Yves P. AUBERSON

NOVARTIS INSTITUTE FOR BIOMEDICAL RESEARCH, Basel, Switzerland
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Dr Yves P. AUBERSON

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Yves P. Auberson is Head of Chemistry for Neurosciences and Nuclear Imaging at the Novartis Institute for BioMedical Research in Basel, Switzerland. He obtained his Ph.D. in asymmetric organic synthesis with Prof. Pierre Vogel at the Swiss Federal Institute of Technology in Lausanne, then did a post-doc on catalytic antibodies with Prof. Peter Schulz at Affymax in Palo Alto, USA. He joined Novartis in 1992, where he led several drug discovery programs for psychiatric and neurodegenerative diseases, as well as for imaging tracers. His main published contributions describe the discovery of the antiepileptic drugs Becampanel and Selurampanel, as well as of the clinical tracer 11C-ABP688 for imaging mGluR5 receptors, and 123I-BZM055 for the study of Gylenia (FTY720) in multiple sclerosis patients.

A Yeast-based Model for Prion Disease Allowed Isolation of Specific and Competitive Inhibitors of a New Protein Chaperone Activity Borne by the Ribosome that are Active Against Other Amyloid-based Diseases

Prof. Marc BLONDEL

INSERM, Brest, France
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Prof. Marc BLONDEL

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Professor of Cell Biology at the Medical Faculty of the “Université de Bretagne Occidentale” (UBO) in Brest, France, since 2006. He leads a research group (in INSERM U1078, for which he is also vice-director) focused on the use of budding yeast Saccharomyces cerevisiae to model human diseases. These yeast-based models served to screen for compounds or genes that are active against the modeled diseases. After a PhD in the Cell Cycle Lab of Dr. Carl Mann, CEA Saclay (France), he held a postdoctoral position for four years at the Swiss Institute of Cancer Research in the Cell Cycle team of Prof. Matthias Peter (Epalinges, Switzerland). Then he was appointed as a CNRS Research Investigator in the Amyloids and Cell Division Cycle Group headed by Dr. Laurent Meijer in Roscoff, until 2006. In 2004 he received the CNRS Bronze Medal and since 2005 he is Senior Editor for Biotechnology Journal (Wiley-Blackwell). Areas of expertise: drug screening, cell cycle/cancer, prion-based diseases, neurodegenerative diseases, budding yeast.

JNJ-42153605: A Novel Positive Allosteric Modulator of mGluR2 for the Treatment of CNS Disorders

Dr Jose CID

JANSSEN RESEARCH AND DEVELOPMENT, Toledo, Spain
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Dr Jose CID

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Jose Cid received his MSc and Bs (1990) in Pharmacy and his PhD in Medicinal Chemistry (1995) both from the University of Santiago de Compostela, (Spain) working on the Synthesis and analysis of the interaction of aminoalkylcycloalcanones with dopamine and serotonin receptors as a potential antipsychotics under the supervision of Prof. E. Ravina. This was followed by a postdoctoral stay (1996/97) at University of Montreal working with Prof. S. Hanessian. His research was focused on Conceptually novel approach to the design of antibacterial compounds in the quinolone family of antibiotics and Molecular recognition and assembly based on amino alcohols with a unique 3-dimensional topology. Since 1997, he holds a research position as Principal Scientist at Johnson & Johnson Pharmaceutical Research & Development. During this time he was involved on the discovery of novel heterocyclic compounds with activities mainly in the area of Central Nervous System. Jose is inventor on 25 patent applications and has (co)-authored 30 peer-reviewed journal articles.

Accelerating Drug Discovery through High Throughput Medicinal Chemistry - Alternative Lead Finding & Optimisation Approaches Including Representative Project Examples

Dr Werngard CZECHTIZKY

SANOFI, Frankfurt am Main, Germany
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Dr Werngard CZECHTIZKY

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Werngard Czechtizky studied Technical chemistry at the TU Graz in Austria. She obtained her PhD at ETH Zürich working on the synthesis of backbone-modified DNA analogues. After a postdoctoral stay at Harvard on natural product chemistry, her industrial career started at Aventis in Frankfurt. She first worked in a global chemical biology GPCR platform, and then, in Sanofi-Aventis, moved into a parallel synthesis team working on various medicinal chemistry projects. Currently, she is a group leader of a high throughput medicinal chemistry team at Sanofi-Aventis in Frankfurt.

Squalenoyl Nanomedicines as Potential Therapeutics

Dr Didier DESMAËLE

UNIVERSITÉ PARIS SUD, Châtenay-Malabry, France
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Dr Didier DESMAËLE

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Didier Desmaële earned his PhD at the University P&M Curie (Paris, France) in 1984, working on the total synthesis of cholecalciferol. After a post-doctoral research position at Yale University in the group of Professor S. L. Schreiber, he was appointed scientist at the CNRSand he moved to the Ecole de Chimie & Physique de la Ville de Paris, where he developed new asymmetric synthesis methodologies. In 1992, he moved to the school of Pharmacy of Université Paris-Sud and took the position of head of team within the CNRS research unit BIOCIS. His main interests were total synthesis of natural products, asymmetric synthesis and medicinal chemistry. Since 1998 he is highly involved in in the design of new drug delivery systems. In January 2011, he joined the CNRS research unit UMR 8612 “Physico-chimie, Pharmacotechnie et Biopharmacie” at the University Paris Sud. His current research activities focus on the design and the synthesis of bioconjugates for nanoparticular drug delivery.

Reduce to the Max – Probing Biology with Natural Product Fragments

Prof. Karl GADEMANN

UNIVERSITY OF BASEL, Zürich, Switzerland
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Prof. Karl GADEMANN

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Karl Gademann (born 1972) was educated at ETH Zürich and Harvard University (PhD with Prof. Dr. Dieter Seebach, postdoctoral studies with Prof. Dr Eric N. Jacobsen, Habilitation associated with Prof. Dr. Erick M. Carreira). After four years as assistant professor at EPFL in Lausanne, he moved in 2010 to the University of Basel, where he was recently promoted to Ordinarius (full professor) holding a chair in organic chemistry. Karl Gademann has had over seventy publications, holds two patents, and received several awards including a Novartis Early Career Award 2010, the national Latsis Prize 2011, the Lilly Lecture Award, the Ruzicka Medal and the Liebig Lectureship of the GDCh. He was awarded the European Young Investigator grant related to natural product synthesis and his research interests include the synthesis and chemical biology of natural products.

Antagonists of the p53/hdm2 Protein-Protein Interaction - Path to the Clinic

Dr Carlos GARCIA-ECHEVERRIA

SANOFI, Vitry sur Seine, France
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Dr Carlos GARCIA-ECHEVERRIA

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Carlos Garcia-Echeverria, Ph.D. has served as Global Head of Oncology Medicinal Chemistry & Pharmacology and Deputy Global Head of Oncology Drug Discovery and Preclinical Development at Sanofi since April 2010. From June 1993 to March 2010, Dr. Garcia-Echeverria held several positions of increasing responsibility at the Novartis Institutes for BioMedical Research. In his last position as Executive Director of Oncology Drug Discovery, he was responsible for managing the late drug discovery programs at the Novartis Oncology Research site in Basel, Switzerland. His research activities have been mainly focused on the identification and development of inhibitors of protein and lipid kinases, proteolytic enzymes and antagonists of intracellular protein-protein interactions. Dr Garcia-Echeverria received the Leonidas Zervas Award from the European Peptide Society in 2006, and has made significant contributions to the identification and development of targeted cancer therapies advancing seven drug candidates to Phase I/II clinical trials. He is an inventor on 30 patents, and has published more than 150 peer-reviewed articles, book chapters and review papers. Dr Garcia-Echeverria received his Ph.D. in organic chemistry from the University of Barcelona (Spain) in 1993.

Bicyclic Peptide Antagonists Isolated From Phage Display Libraries

Prof. Christian HEINIS

ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE (EPFL), Lausanne, Switzerland
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Prof. Christian HEINIS

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Christian Heinis is a Tenure-track Assistant Professor at the Institute of Chemical Sciences and Engineering (ISIC) of the Ecole Polytechnique Fédérale de Lausanne (EPFL) in Switzerland. The research goal of Christian Heinis is the development of novel and innovative therapeutic strategies. A main focus is the engineering of bicyclic peptides binding to disease targets using phage display and the testing of their therapeutic potential in vitro and in vivo. Christian Heinis had studied biochemistry at the Swiss Federal Institute of Technology in Zurich (ETHZ) where he also did a PhD in the research group of Prof. Dr. Dario Neri. He was a postdoctoral fellow in the group of Prof. Dr. Kai Johnsson at the EPFL and in the group of Sir Gregory Winter at the Laboratory of Molecular Biology (LMB) in Cambridge, UK. In 2008 he was appointed Assistant Professor with tenure track for Bioorganic Chemistry at EPFL and since 2009 he is holding a professorship of the Swiss National Science Foundation. Christian is a scientific founder of the start-up company Bicycle Therapeutics.

Perspectives in Structure and Fragment Based Drug Discovery

Prof. Rod HUBBARD

UNIVERSITY OF YORK / VERNALIS, York, United Kingdom
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Prof. Rod HUBBARD

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Rod Hubbard has been working with methods for analysis and exploitation of protein structure for over 30 years. In the 1980s, he developed molecular modelling methods; in the 1990s he helped build the Structural Biology Lab at the University of York. Since 2001, he has spent varying amounts of his time with Vernalis, establishing and applying structure and fragment-based methods for drug discovery

Structure and Function of Acid-Sensing Ion Channels

Dr Stephan KELLENBERGER

UNIVERSITÉ DE LAUSANNE, Lausanne, Switzerland
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Dr Stephan KELLENBERGER

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Stephan Kellenberger received his PhD in 1994 from the University of Bern for research on GABAA receptor function performed with Erwin Sigel. He did then a post-doctoral training with W.A. Catterall at the University of Washington, Seattle, on the topic of voltage-gated Na channels. He joined the Department of Pharmacology of the University of Lausanne in 1997. He has been leading his own research team since 2001. The main interests of his laboratory are the study of acid-sensing ion channels (ASICs) which are involved in pain sensation, expression of fear, learning, and neurodegeneration after ischemia. By applying a number of different techniques, the laboratory aims at understanding 1) the roles of ASICs in neuronal signaling, and 2) the molecular details of the control of channel opening by protonation.

Targeting Protein Interactions Mediated by Epigenetic Acetyl-lysine Reader Domains of the Bromodomain Family

Prof. Stefan KNAPP

OXFORD UNIVERSITY, Oxford, United Kingdom
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Prof. Stefan KNAPP

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Dr Knapp studied chemistry at the University of Marburg (Germany) and University of Illinois (Urbana-Champaign, USA). He did his PhD in protein crystallography at the Karolinska Institute (Stockholm, Sweden) where he also continued his career as postdoctoral scientist. In 1999 he joined Pharmacia & Upjohn (Nerviano Italy) where he worked as a principal scientist until the acquisition of the company by Pfizer in 2004. Since 2004 he is principal investigator at the SGC and Professor for Structural Biochemistry at the Nuffield Department of Clinical Medicine at Oxford University

Protein-binding Prodrugs and Drug Conjugates in Oncology: From Design, Applications to Combination Therapy

Prof. Felix KRATZ

TUMOR BIOLOGY CENTER, Freiburg, Germany
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Prof. Felix KRATZ

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The Division Macromolecular Prodrugs was founded in 1994 by Dr. Felix Kratz in the Clinical Research Department at the Tumor Biology Center, Freiburg, Germany. Felix Kratz graduated in Chemistry from the University of Heidelberg in 1991. The primary goal of his research team is the development of novel drug delivery concepts for improving the efficacy and toxicity of anticancer agents. He has 20 years of experience in the preclinical development of anticancer drugs and profound knowledge of translational research from the laboratory to the clinic and has successfully transferred a first albumin-binding doxorubicin prodrug (INNO-206) into the clinic which is currently undergoing phase II trials. His research areas are drug targeting, drug delivery systems, prodrugs, receptor targeting, bioconjugate chemistry, polymer therapeutics and nanocarriers. He has authored approximately 240 scientific publications, book articles and proceedings and is the inventor or co-inventor of 28 patents and patent applications.

Pharmacophore-based Parallel in Silico Screening: An Interesting Concept for Efficient Activity Profiling in Drug Discovery

Prof. Thierry LANGER

PRESTWICK CHEMICAL, Vienna, Austria
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Prof. Thierry LANGER

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Thierry Langer is CEO and President of Prestwick Chemical, a medicinal chemistry company located in Strasbourg, France. Prior to joining Prestwick in 2008, he was Professor for medicinal chemistry at University of Innsbruck and CEO of Inte:Ligand GmbH. His research interests range from computer assisted molecular design to medicinal chemistry, with a strong focus on method development for pharmacophore modeling, and his scientific work has culminated in more than 170 original articles, book chapters, and invited reviews. range from computer assisted molecular design to medicinal chemistry, with a strong focus on method development for pharmacophore modeling, and his scientific work has culminated in more than 170 original articles, book chapters, and invited reviews.

Translating Structural-biology & Preclinical Activity of Nilotinib into Efficacy in Leukemia Patients

Dr Paul W. MANLEY

NOVARTIS PHARMA, Basel, Switzerland
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Dr Paul W. MANLEY

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Executive Director / Novartis Leading Scientist. Dr. Paul W. Manley received his Ph.D. in Organic Chemistry from Liverpool University. He has over 30 years of medicinal chemistry experience in the pharmaceutical industry, across several therapeutic areas. Since year 2000, he has been engaged in the discovery and development of drugs to treat haematological malignancies, with the invention of nilotinib (Tasigna®), marketed worldwide for the treatment of chronic myelogenous leukemia, being a significant achievement. He has published over 110 scientific papers on leukaemia and oncology drugs, medicinal and organic chemistry, and is co-inventor of over 60 patents.

Two Chemical/Biological Approaches to Alzheimer's Disease: Prevention and Therapy
Charles Mentzer Prize Lecture

Dr Laurent MEIJER

MANROS THERAPEUTICS, Roscoff, France
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Dr Laurent MEIJER

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Laurent MEIJER obtained Doctorate degrees from the Universities of Lille (1978) and Paris (1983). After a post-doctoral stay at the Stanford University marine laboratory, Pacific Grove (David EPEL) (1978-1979), he obtained a position at the C.N.R.S. in Roscoff, France. He was on sabbatical leave at the University of Washington, Seattle (Edwin KREBS and Bennett SHAPIRO) (1985-1986) and at the Rockefeller University (Paul GREENGARD) (2001-2004). All his work has focused on basic aspects of protein phosphorylation, as it relates to cancer, neurodegenerative disorders and unicellular parasites. Besides this fundamental research, the group has focused on the identification, optimization and characterization of pharmacological inhibitors of disease-relevant kinases. These efforts have led to the discovery of potent and selective inhibitors of protein kinases (olomoucine, roscovitine, purvalanol, paullones, indirubins, hymenialdisine, aloisines, mériolines, leucettines, etc…). These molecules are widely used as pharmacological tools. They are also undergoing pre-clinical and clinical evaluation against cancers and various neurodegenerative diseases. (R)-roscovitine (CYC202, Seliciclib), is currently in phase 2 clinical trials against NSCL cancer and nasopharyngeal cancer, in phase 1 against renal diseases, and in pre-clinical tests against Alzheimer’s disease, stroke and polycystic kidney disease. To facilitate and speed up the preclinical/clinical development of second generation pharmacological inhibitors of specific kinases, he and Prof. Hervé GALONS (University of Paris Descartes) have founded a small biotech company, ManRos Therapeutics (“From Sea to Pharmacy”) (http://www.manros-therapeutics.com) focused on the development of kinase inhibitors in the treatment of various kidney diseases (short term), cancer & leukaemia (mid-term) and Alzheimer's disease (long term).

From ApoA1 Upregulation to BET Family Bromodomain Inhibition: Unlocking the Potential of an Epigenetic Target Class

Dr Olivier MIRGUET

GLAXOSMITHKLINE, Les Ulis, France
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Dr Olivier MIRGUET

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Olivier Mirguet has been a principal investigator in medicinal chemistry at GlaxoSmithKline (Les Ulis, France) since 2003. His research is in the field of cardiovascular diseases and metabolism with special interest in epigenetics. Olivier completed his doctoral work on the synthesis of paroxetine using ring expansion methodologies in 2001 at the University Pierre et Marie Curie (Paris, France) under the direction of Professor Janine Cossy. Subsequently, he accepted a postdoctoral position with Professor James H. Rigby at Wayne State University (Detroit, MI, USA) working on the total synthesis of the diterpene ingenol before joining GSK.

Synthetic Carbohydrates in the Search for Tailor-made Antibacterial Vaccines: Shigellosis as a Challenge

Dr Laurence MULARD

PASTEUR INSTITUTE, Paris, France
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Dr Laurence MULARD

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Laurence A. Mulard graduated as an engineer from the Ecole Supérieure de Physique et Chimie Industrielles (ESPCI, Paris, France) and completed her MSc at the Université Pierre et Marie Curie (Paris, France) in 1988. She received her PhD in chemistry from the same University (1991) working under the supervision of Prof. Czernecki. After three postdoctoral years at the National Institutes of Health (NIH, Bethesda, MD, USA) studying glycochemistry in the group of Dr Glaudemans, she joined the Institut Pasteur (Paris, France) as research assistant. Involved in the field of glycosciences, she received her “Habilitation” in 2003 and was promoted Senior Scientist in 2007, while acting as Head of the Unité de Chimie Organique. In 2008, she was appointed Head of the Unit “Chemistry of Biomolecules” at the Institut Pasteur. Her research interests are in the area of chemical biology with focus on carbohydrates and glycoconjugates in relation to diseases and biological recognition. Major investigations are on polysaccharide antigen/antibody interactions by use of synthetic chemistry in combination with structural, physicochemical and immunochemical analysis. Current focus is on the identification and synthesis of well-defined mimics of selected bacterial polysaccharides – and conjugates thereof – for the development of novel carbohydrate-based vaccines.

Chemical space exploration via Natural Product-like compounds

Dr Jean-Yves ORTHOLAND

EDELRIS, Lyon, France
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Dr Jean-Yves ORTHOLAND

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Jean-Yves Ortholand, Ph.D. is currently the CEO of Edelris, a French research and services-based company he co-founded and has led for the past seven years. Jean-Yves worked as an undergraduate student in Pr.Stoddart's team in UK, then received his Ph.D. in Organic Chemistry from Cl.Bernard University in Lyon in 1991, under the guidance of Dr.Greiner, and then did postdoctoral studies at Harvard University on DNA repair enzymes inhibition in Pr.Verdine's group. On his return to France he spent 4 years at Rhône-Poulenc, then at Merck as the Combichem project leader supporting Medchem teams targeting diabetes. Between 2002 and 2004 he was on leave in New-Haven, CT. working in a biotech company on PTP-1B inhibitors for diabetes related research. His current interest lies in the area of biorelevant space exploration via 3D, NP-like compounds and fragments, and optimization chemistry for Life Sciences applications.

Discovery of RG1678, a First in Class Glycine Reuptake Inhibitor for the Treatment of Schizophrenia

Dr Emmanuel PINARD

F. HOFFMANN-LA ROCHE, Basel, Switzerland
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Dr Emmanuel PINARD

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Current position: project leader in medicinal chemistry department at Hoffmann-La Roche. Currently leading the GlyT1 project. Research field: Experience in targeting enzymes, GPCR, transporters for CNS indications like Schizophrenia, Alzheimer, Parkinson, Insomnia Education: 1991: PhD in Chemistry from the university of P. et M. Curie in Paris (France) 1992-1993: Post-doc in the group of Professor L. Paquette at the Ohio State University Columbus (Ohio) on synthesis of natural products In 1994, Joined the Drug Discovery Chemistry unit of Hoffmann-La Roche, Basel, as medicinal chemist

A Look at Some Innovative Chemical Aspects in Medicinal Chemistry, about Heterocycles, Microwaves, Chemical Libraries, Boronics and Garlands
Paul Ehrlich Prize Lecture

Prof. Sylvain RAULT

UNIVERSITÉ DE CAEN, Caen Cedex, France
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Prof. Sylvain RAULT

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Sylvain RAULT- Pharmacist 1975, Docteur d’Etat es Sciences ( Organic chemistry) 1982 Professor of Medicinal Chemistry –Faculty of Pharmacy- University of Caen -1986 …. Director of CERMN - Centre d’Etudes et de Recherche sur le Médicament de Normandie - 1998- 2011 Assistant Director of the French Chemical librairy - 2003 … Current area of research in organic chemistry: Synthesis of heterocyclic compounds oriented by diversity and drugability, organization of chemical librairies, exploration of new areas of the chemical field. Synthesis of boronic species and their use for the preparation of garlands as new foldamers. Main domains of application in medicinal chemistry: cancerology ( PPI’s) and neurosciences ( 5-HT) Other position: French Ministry of Environment: President of the “ Commission des produits chimiques et biocides, CPCB ” 2003….

Combined Use of Noncovalent Mass Spectrometry and Other Biophysical Techniques in Early-stage Drug Discovery

Dr Jean-Paul RENAUD

NOVALIX, Ostwald, France
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Dr Jean-Paul RENAUD

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Jean-Paul Renaud isCSOat NovAliX, an innovative technology company dedicated to early-stage drug discovery that resulted from the merger in 2009 of Novalyst Discovery (chemistry) and AliX (structural biology& biophysics). He was the creator and CEO-CSO of AliX (2002-2008). He waspreviouslyCNRS Research Associate (1993-2000) then CNRS Research Director (2000-2002) in the Dept. of Structural Biology and Genomics of IGBMC (Illkirch), whereheworked on the structural biology of nuclearreceptors, and CNRS Research Associate in the Lab. of Pharmacological and Toxicological Chemistry and Biochemistry (UniversitéParis 5) (1988-1993).He was a post-doctoral fellow at the MRC Laboratory of Molecular Biology in Cambridge, UK (1987-1988). He obtained a PhD in bio-inorganic chemistry from Université Paris 6 (1986) and an Engineering Diploma from ENSCP (1982).

Sorafenib – A Signal Transduction Inhibitor for the Treatment of Liver Cancer

Dr Bernd RIEDL

BAYER PHARMA, Wuppertal, Germany
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Dr Bernd RIEDL

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Bernd Riedl studied chemistry at the university of Stuttgart and received his Ph.D in 1991 focusing on natural product synthesis in the group of U. Schmidt. After postdoctoral research with U. Schmidt he joined Bayer Pharma at Wuppertal, Germany, in 1992 as a Senior Scientist and Lab Head working on lead optimization projects in the field of antibacterials. In the course of a job rotation he worked from 1996 to 1998 in the Bayer US Research Center in West Haven CT in the field of anticancer research. Back in Wuppertal he was project leader in the field of CNS research. In 2000 he was appointed Director of combinatorial chemistry and since 2001 he holds his current position as Director of Medicinal Chemistry at Bayer Pharma in Wuppertal being responsible for Medicinal Chemistry research in the antithrombotic segment. Since 2009 he is a lecturer for medicinal chemistry at the University of Duesseldorf.

Progress on Allosteric Modulation of mGluR5 and mGluR4: towards New Treatment Paradigms in Parkinson’s Disease

Dr Jean-Philippe ROCHER

ADDEX THERAPEUTICS, Plan-les-Ouates, Switzerland
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Dr Jean-Philippe ROCHER

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Addex Therapeutics 12, Chemin Des Aulx CH-1228, Plan les Ouates Geneva, Switzerland Since joining Addex at its inception in 2002, Dr. Rocher has been responsible for establishing the company’s chemistry capabilities and building Addex small molecule allosteric modulator chemistry platform. He has played a pivotal role in the success of both internal and partnered programs including Addex mGluR5 negative allosteric modulator and mGluR2 positive allosteric modulator programs which have both progressed into phase II clinical development. Prior to joining Addex, Dr Rocher was director of chemistry at Devgen NV, Gent, Belgium from 2001 to 2002; senior research scientist for GlaxoSmithKline KK in Tsukuba, Japan from 1997 to 2001. From 1995 to 1997, he was “guest scientist” at Mitsubishi Pharma in Yokohama, Japan. He completed a Pharm. D and obtained his PhD at the Faculty of Pharmacy of Lyon, France in 1987. Dr. Rocher started his career as a research scientist in the dermatology research centre of Galderma at Sophia-Antipolis, France.

Potent Antibody Drug Conjugates for Cancer Therapy: From the Lab to a Clinically Approved Drug

Dr Peter SENTER

SEATTLE GENETICS, Bothell, United States
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Dr Peter SENTER

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Peter Senter is the Vice President of Chemistry at Seattle Genetics. He has been with the company for 13 years, shortly after it was founded. Dr. Senter initiated and led the antibody drug conjugate (ADC) program that resulted in the recent approval of ADCETRIS, an ADC that recognizes the CD30 antigen on Hodgkin lymphoma and anaplastic large cell lymphoma. His group has focused attention on all aspects of ADC technology, starting with the development of highly potent cytotoxic drugs, conditionally labile linkers, conjugation technologies, antibody engineering, and ADC biology. Dr. Senter also serves as the Senior Editor for Bioconjugate Chemistry and is an Adjunct Professor in the Department of Bioengineering at the University of Washington in Seattle. He received an A.B. degree in Biochemistry from the University of California at Berkeley, a PhD in Chemistry from the University of Illinois in Urbana, and did postdoctoral research at the Max Planck Institute for Experimental Medicine in Göttingen, Germany. Prior to joining Seattle Genetics, Dr. Senter held various positions at the Dana Farber Cancer Institute, Bristol Myers Squibb Pharmaceutical Research Institute, and Cytokine Networks. His research interests include targeted drug delivery, protein chemistry, and the design of novel chemotherapeutic agents.

SV2 Proteins Beyond Levetiracetam: The Discovery of the First SV2C Selective Ligands

Dr Anne VALADE

UCB, Braine-l'Alleud, Belgium
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Dr Anne VALADE

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Anne VALADE, Ph.D. is Principal Scientist in Medicinal Chemistry, UCB Pharma, Braine l’Alleud, BELGIUM. Her research field focus on central nervous system (CNS) disorders and immunology diseases to deliver more convenient and effective treatments for patients and specialists. Education and past experience: Postdoctoral Research Fellow with Prof. David Hodgson, University of Oxford, U.K. (2004-2006) - Synthetic Studies Towards Squalestatin - Ph.D. in Organic Chemistry with Prof. J.-M. Beau, Paris XI University (Orsay), France (2001-2004). Selection of Glycosyltransferase Modulators by Dynamic Combinatorial Chemistry

Matched Triplicate Design Sets in the Optimisation of a New Series of Glucokinase Activators

Prof. Mike WARING

ASTRAZENECA, Newcastle upon Tyne, United Kingdom
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Prof. Mike WARING

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Mike is a medicinal chemist working for AstraZeneca in CVGI at Alderley Park. Mike received his degree (chemistry, 1996) and PhD (organic chemistry, 2000) from The University of Manchester working with Tim Donohoe then carried out post doctoral work at The University of Texas at Austin with Prof Phil Magnus working on The Total Synthesis of Guanacastepene. Mike then joined AstraZeneca at Alderley Park in 2001 and has worked in both cancer and CVGI, delivering 11 compounds into development including the glucokinase activator AZD1656. He is the winner of the 2010 Royal Society of Chemistry Capps-Green-Zomaya medal for outstanding contributions to medicinal chemistry and the 2010 runner up of the European Federation for Medicinal Chemistry award for an outstanding young medicinal chemist in industry. Mike is the author of 18 published papers, 21 patents and one book, he is also a member of the scientific advisory board for Medicinal Chemistry Communications (Royal Society of Chemistry). Mike is currently a Principal Scientist in CVGI Medicinal Chemistry at Alderley Park.