Plenary Speakers
Paul Ehrlich Prize Lecture
Trip in Drug Discovery (PL01)
Trip in Drug Discovery (PL01)
Prof. Jean-Daniel BRION
UNIVERSITÉ PARIS-SUD
Chatenay-Malabry, France
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.
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.
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
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.
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.
Conquering the p53-MDM2 Protein-Protein Interaction Target at Novartis (PL21)
Dr Pascal FURET
NOVARTIS
Basel, Switzerland
Basel, Switzerland
Pascal Furet
28 year experience as molecular modeller in the pharmaceutical industry (Ciba and Novartis- Basel) covering more than 30 research projects (enzyme, receptor and protein-protein interaction projects). Around 230 papers and patents published. Key contributions to marketed drugs Diovan®, Femara®, Tasigna® and clinical compounds (kinase inhibitors: Abl, EGF-R, VEGF, FGF-R, PI3K-mTOR and PPI inhibitors p53-MDM2).
CAREER HISTORY
• Since 2005: senior research investigator and now director in the global CADD (Computer-Assisted Drug Design) group of Novartis.
• 1997-2004: Lab head (molecular modeling and design) in the oncology research department of Novartis.
• During 1996: CAMM expertise coordinator in the core technologies department of Ciba.
• 1988-1995: research scientist in the CAMM (Computer-Assisted-Molecular Modeling) group of the pharma division of Ciba (Basel).
• Postdoctoral year during 1987 in molecular modelling (Ciba-Geigy. Basel)
• Teaching assistant in the chemistry department of the University of Houston (USA) during 1983-1985.
• Research work in synthetic organic chemistry in the petrochemical division of Rhône-Poulenc (Lyon) during 1982.
AWARDS
• American Chemical Society " Heroes of Chemistry" award (2000) for the discovery of the cardiovascular drug Diovan®
• Novartis "Leading Scientist" award (2000)
• Recipient of the first "Dolphin Prize" for scientific excellence of the Pharma Division of Ciba (1995).
DIPLOMA
• Ph.D. in Theoretical Chemistry-Chemical Physics (University of Houston-USA).
• Master degree in industrial chemistry (with emphasis on organic chemistry)-École Supérieure de Chimie Industrielle de Lyon (France).
EDUCATION HISTORY
• 1976: Baccalauréat-Scientific Option ("mention bien").
• 1976/1979: Classes de Mathématiques Supérieures et Spéciales- Lycée Châteaubriand (Rennes, France).
• 1979/1982: École Supérieure de Chimie Industrielle de Lyon.
• 1982/1985: Ph.D. program in theoretical chemistry-chemical physics of the University of Houston (USA).
28 year experience as molecular modeller in the pharmaceutical industry (Ciba and Novartis- Basel) covering more than 30 research projects (enzyme, receptor and protein-protein interaction projects). Around 230 papers and patents published. Key contributions to marketed drugs Diovan®, Femara®, Tasigna® and clinical compounds (kinase inhibitors: Abl, EGF-R, VEGF, FGF-R, PI3K-mTOR and PPI inhibitors p53-MDM2).
CAREER HISTORY
• Since 2005: senior research investigator and now director in the global CADD (Computer-Assisted Drug Design) group of Novartis.
• 1997-2004: Lab head (molecular modeling and design) in the oncology research department of Novartis.
• During 1996: CAMM expertise coordinator in the core technologies department of Ciba.
• 1988-1995: research scientist in the CAMM (Computer-Assisted-Molecular Modeling) group of the pharma division of Ciba (Basel).
• Postdoctoral year during 1987 in molecular modelling (Ciba-Geigy. Basel)
• Teaching assistant in the chemistry department of the University of Houston (USA) during 1983-1985.
• Research work in synthetic organic chemistry in the petrochemical division of Rhône-Poulenc (Lyon) during 1982.
AWARDS
• American Chemical Society " Heroes of Chemistry" award (2000) for the discovery of the cardiovascular drug Diovan®
• Novartis "Leading Scientist" award (2000)
• Recipient of the first "Dolphin Prize" for scientific excellence of the Pharma Division of Ciba (1995).
DIPLOMA
• Ph.D. in Theoretical Chemistry-Chemical Physics (University of Houston-USA).
• Master degree in industrial chemistry (with emphasis on organic chemistry)-École Supérieure de Chimie Industrielle de Lyon (France).
EDUCATION HISTORY
• 1976: Baccalauréat-Scientific Option ("mention bien").
• 1976/1979: Classes de Mathématiques Supérieures et Spéciales- Lycée Châteaubriand (Rennes, France).
• 1979/1982: École Supérieure de Chimie Industrielle de Lyon.
• 1982/1985: Ph.D. program in theoretical chemistry-chemical physics of the University of Houston (USA).
Advances in Structure Based Drug Discovery of Membrane Protein Targets (PL14)
Dr Michael HENNIG
LEADXPRO
Villigen, Switzerland
Villigen, Switzerland
Michael Hennig, PhD, Prof. CEO, leadXpro AG, Villigen, Switzerland
• Drug discovery research manager with 20 years of experience in pharmaceutical industry
• Co-founder and CEO of leadXpro, a spin-out of the Paul Scherrer Institute dedicated to structure based drug discovery of membrane protein targets
• Formerly at Roche Research Basel, Global Head and Principle Leader of discovery technologies with responsibility for structure based drug discovery, protein science, assay development and HTS, corporate compound library, stem cell platform.
• Guest Professor at the University of Basel in structural biology, lecture series in pharmacy, author of >70 papers and lecturer at conferences, 8 patents in areas of technology, discovery and formulation of drug substances.
• Study of physics, biochemistry, PhD in structural biology at EMBL Hamburg, Germany, postdoc at Biozentrum, University of Basel, Switzerland.
• Drug discovery research manager with 20 years of experience in pharmaceutical industry
• Co-founder and CEO of leadXpro, a spin-out of the Paul Scherrer Institute dedicated to structure based drug discovery of membrane protein targets
• Formerly at Roche Research Basel, Global Head and Principle Leader of discovery technologies with responsibility for structure based drug discovery, protein science, assay development and HTS, corporate compound library, stem cell platform.
• Guest Professor at the University of Basel in structural biology, lecture series in pharmacy, author of >70 papers and lecturer at conferences, 8 patents in areas of technology, discovery and formulation of drug substances.
• Study of physics, biochemistry, PhD in structural biology at EMBL Hamburg, Germany, postdoc at Biozentrum, University of Basel, Switzerland.
Discovery of the Type II Kinase Inhibitor LY3009120; a Pan-RAF Inhibitor Showing Minimal Paradoxical Activation and Anti-Cancer Activity Against BRAF or RAS Mutant Tumor Cells (PL22)
Dr James R. HENRY
ELI LILLY & CO.
Indianapolis, United States
Indianapolis, United States
James R. Henry, Ph.D, obtained his Bachelor of Science degree in chemistry from Virginia Tech before earning his Doctoral degree from The Pennsylvania State University.
Following a National Institutes of Health Postdoctoral Fellowship at the University of Rochester, he joined the RW Johnson Pharmaceutical Research Institute as a medicinal chemist.
For the last 16 years, he has been in the Discovery Chemistry Department at Eli Lilly and Company where he currently holds the position of Research Fellow working primarily in oncology research.
Following a National Institutes of Health Postdoctoral Fellowship at the University of Rochester, he joined the RW Johnson Pharmaceutical Research Institute as a medicinal chemist.
For the last 16 years, he has been in the Discovery Chemistry Department at Eli Lilly and Company where he currently holds the position of Research Fellow working primarily in oncology research.
Nanocyclix: a Chemical Biology Approach for Next Generation Kinase Inhibitors (PL08)
Dr Jan HOFLACK
ONCODESIGN
Dijon, France
Dijon, France
Current: Chief Scientific Officer and Executive Director, Oncodesign S.A., Dijon, France
Research Field: Drug Discovery, kinase inhibition, macrocyclic chemistry, oncology, CNS, autoimmune diseases
Previous: - GNI Ltd., External Director, Tokyo, Japan - Johnson & Johnson, VP Europe Medicinal Chemistry and enabling technologies, Beerse, Belgium - AstraZeneca, VP Enabling Sciences and Technologies, Gothenburg, Sweden - Astra, Director Structural Chemistry Laboratory, Gothenburg, Sweden - Novartis, Head Structural Biology and molecular modeling, Basel, Switzerland - Marion Merrell Dow Research Laboratories, Research Scientist computational chemistry, Strasbourg, France
Education: PhD. Organic Chemistry, State University Ghent, Belgium
Previous: - GNI Ltd., External Director, Tokyo, Japan - Johnson & Johnson, VP Europe Medicinal Chemistry and enabling technologies, Beerse, Belgium - AstraZeneca, VP Enabling Sciences and Technologies, Gothenburg, Sweden - Astra, Director Structural Chemistry Laboratory, Gothenburg, Sweden - Novartis, Head Structural Biology and molecular modeling, Basel, Switzerland - Marion Merrell Dow Research Laboratories, Research Scientist computational chemistry, Strasbourg, France
Education: PhD. Organic Chemistry, State University Ghent, Belgium
Molecular Imaging Agents Based on Lanthanide Complexes (PL17)
Dr Eva JAKAB-TOTH
CNRS
Orléans, France
Orléans, France
Eva Jakab Toth (DR1 CNRS) is expert in the design, synthesis and characterization of metal chelates related to imaging applications.
After a PhD from the University of Debrecen, Hungary in lanthanide coordination chemistry, she occupied research positions at EPF Lausanne and was appointed as CNRS research director in 2005.
Since 2012, she is director of the Centre of Molecular Biophysics, CNRS UPR 4301, Orléans. She published over 140 original papers and edited “The Chemistry of Contrast Agents in Medical Magnetic Resonance Imaging”, Wiley, 2001 and 2013 (2nd Ed.).
She chaired the European COST Network “Metal-Based Systems for Molecular Imaging Applications”.
Her recent research focuses on imaging probes to detect enzymatic activities, neurotransmitters and amyloid peptides.
After a PhD from the University of Debrecen, Hungary in lanthanide coordination chemistry, she occupied research positions at EPF Lausanne and was appointed as CNRS research director in 2005.
Since 2012, she is director of the Centre of Molecular Biophysics, CNRS UPR 4301, Orléans. She published over 140 original papers and edited “The Chemistry of Contrast Agents in Medical Magnetic Resonance Imaging”, Wiley, 2001 and 2013 (2nd Ed.).
She chaired the European COST Network “Metal-Based Systems for Molecular Imaging Applications”.
Her recent research focuses on imaging probes to detect enzymatic activities, neurotransmitters and amyloid peptides.
Optimization and Exploration of Bradykinin 1 Receptor Antagonists for Inflammation (PL07)
Dr Sven KÜHNERT
GRUENENTHAL GMBH
Aachen, Germany
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.
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.
Human Proteomes – from Basic Biology to Understanding Drug Action (PL02)
Prof. Bernhard KÜSTER
TECHNICAL UNIVERSITY MUNICH
Munich, Germany
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.
Protein Total Synthesis and the Challenge of Understanding MET Tyrosine Kinase Receptor Activation (PL11)
Dr Oleg MELNYK
CNRS / UNIVERSITY OF LILLE / PASTEUR INSTITUTE OF LILLE
Lille, France
Lille, France
Oleg Melnyk graduated as an engineer in chemistry in 1989 from the Ecole Nationale Supérieure de Chimie de Paris (now Chimie ParisTech).
During his Ph.D (1991-1994) he developed a novel total synthesis of cortisone.
He’s working since 1996 as a researcher from the Centre National de la Recherche Scientifique (CNRS) in Lille. He’s main research interests are today at the frontiers between peptide and protein chemistry and biology. In particular, he’s deeply involved in the development of novel chemoselective ligation chemistries for protein total synthesis, but also in the study of the mechanisms of activation of some growth factors such as hepatocyte growth factor using chemical biology approaches.
He is member of the scientific board of the Journal of Peptide Science, of Frontiers in Chemical Biology and of the International Journal of Peptide Therapeutics.
During his Ph.D (1991-1994) he developed a novel total synthesis of cortisone.
He’s working since 1996 as a researcher from the Centre National de la Recherche Scientifique (CNRS) in Lille. He’s main research interests are today at the frontiers between peptide and protein chemistry and biology. In particular, he’s deeply involved in the development of novel chemoselective ligation chemistries for protein total synthesis, but also in the study of the mechanisms of activation of some growth factors such as hepatocyte growth factor using chemical biology approaches.
He is member of the scientific board of the Journal of Peptide Science, of Frontiers in Chemical Biology and of the International Journal of Peptide Therapeutics.
The Realisation of Activity-Directed Synthesis (PL19)
Prof. Adam NELSON
UNIVERSITY OF LEEDS
Leeds, United Kingdom
Leeds, United Kingdom
Adam Nelson is Professor of Chemical Biology at the University of Leeds.
His current research focuses on the discovery of novel bioactive small molecules, and their application in the interrogation of biological mechanisms. A major theme is the development of approaches to enable the exploration of biologically-relevant chemical space including lead-oriented synthesis and activity-directed synthesis.
Professor Nelson received a first class BA in Natural Sciences (Chemistry) from Churchill College Cambridge in 1993, before undertaking a PhD in Synthetic Organic Chemistry with Dr Stuart Warren, also at the University of Cambridge.
He was a postdoctoral researcher at Manchester before starting his independent academic career at Leeds in 1998.
His current research focuses on the discovery of novel bioactive small molecules, and their application in the interrogation of biological mechanisms. A major theme is the development of approaches to enable the exploration of biologically-relevant chemical space including lead-oriented synthesis and activity-directed synthesis.
Professor Nelson received a first class BA in Natural Sciences (Chemistry) from Churchill College Cambridge in 1993, before undertaking a PhD in Synthetic Organic Chemistry with Dr Stuart Warren, also at the University of Cambridge.
He was a postdoctoral researcher at Manchester before starting his independent academic career at Leeds in 1998.
Discovery of Selective Dopaminergic D3 Receptor Antagonists with Potent 5HT6 Affinity (PL10)
Dr Jean-Claude ORTUNO
INSTITUT DE RECHERCHES SERVIER
SURESNES, France
SURESNES, France
Dr Jean-Claude Ortuno, Scientific Director in charge of Exploratory Projects since 2015 in Chemistry Pole of Expertise, Institut de Recherches Servier, Suresnes France.
He obtained a PhD degree in Organic Chemistry in 1991 from Université d’Orsay (ParisXI) under the supervision of Prof Y. Langlois at the Institut de Chimie des Substances Naturelles Gyf sur Yvette and joined the Université Catholique de Louvain-la-Neuve, Belgium as a Postdoctoral Researcher in the group of Prof. L. Ghosez.
He joined Les Laboratoires Fournier in 1993 where he was involved in cardiovascular projects. In the last 18 years at the Institut de Recherches Servier as a Medicinal Chemist then as a Division Director, he was involved in different therapeutic areas in particular Oncology and CNS.
He obtained a PhD degree in Organic Chemistry in 1991 from Université d’Orsay (ParisXI) under the supervision of Prof Y. Langlois at the Institut de Chimie des Substances Naturelles Gyf sur Yvette and joined the Université Catholique de Louvain-la-Neuve, Belgium as a Postdoctoral Researcher in the group of Prof. L. Ghosez.
He joined Les Laboratoires Fournier in 1993 where he was involved in cardiovascular projects. In the last 18 years at the Institut de Recherches Servier as a Medicinal Chemist then as a Division Director, he was involved in different therapeutic areas in particular Oncology and CNS.
Innovative Approaches to Control Metabotropic Glutamate Receptor Activity in the Brain (PL15)
Dr Jean-Philippe PIN
CNRS-UNIVERSITY OF MONTPELLIER
Montpellier, France
Montpellier, France
Jean-Philippe Pin get trained at the Ecole Normale Supérieure in Paris, and got his PhD in Molecular Biology in 1987 at the University of Montpellier (France).
He is internationally recognized for his participation in the discovery of metabotropic glutamate receptors, and his studies related to the allosteric modulation and activation mechanism of this family of G protein coupled receptors.
Since 2003, he is head of the Molecular Pharmacology Department within the Institute of Functional Genomics (Montpellier, France), and became director of this Institute in January 2011. His research is focused on the molecular and cellular dynamics of GPCRs, mostly mGlu and GABAB receptors. Over the recent years he developed innovative approaches to study cell surface receptors, including biosensors and photoswitchable ligands. His studies led to new concepts in the GPCR field, such as: the activation of cell surface receptors by intracellular proteins; the regulation of GPCRs by both negative and positive allosteric modulators, the asymmetric functioning of GPCR dimers.
MT5-MMP, a New Potential Therapeutic Target in Alzheimer’s Disease (PL09)
Dr Santiago RIVERA
CNRS / AIX-MARSEILLE UNIVERSITY
Marseille, France
Marseille, France
Santiago Rivera. Director of research at CNRS. Team leader at UMR7259 NICN, Marseille, France.
Research field. Neuroscience and Alzheimer’s disease.
Education
• 1990. Ph. D. Neuroscience. University of Barcelona.
• 1987. MSc Biochemistry and Physiology. University of Barcelona. Former professional experience
• 1999 - 2010. Researcher at CNRS and team leader.
• 1994 - 1998. Research associate, U29 Inserm, Paris.
• 1990 - 1994 Research associate, University of California, Irvine, USA
• 1990. Ph. D. Neuroscience. University of Barcelona.
• 1987. MSc Biochemistry and Physiology. University of Barcelona. Former professional experience
• 1999 - 2010. Researcher at CNRS and team leader.
• 1994 - 1998. Research associate, U29 Inserm, Paris.
• 1990 - 1994 Research associate, University of California, Irvine, USA
Development of Novel Antiangiogenic Agents for the Treatment of Retinal Neovascularization via Integration of Chemistry and Biology (PL12)
Prof. Young-Ger SUH
SEOUL NATIONAL UNIVERSITY
Pocheon-si, Korea, South
Pocheon-si, Korea, South
Young-Ger Suh is a Professor of College of Pharmacy, Seoul National University, Korea.
He graduated from Seoul National University with a B.S. degree in Pharmacy in 1975 and received Ph.D. degree from University of Pittsburgh in 1987.
He has been a president of Pharmaceutical Society of Korea (2013-2014) and Korean Society of Organic Synthesis (2015).
Currently, he is a full member of The Korean Academy of Science and Technology, a Fellow of Asian Federation for Medicinal Chemistry, and a Member of Editorial Board of Asian Journal of Organic Chemistry.
His research interests include development of selective cellular signaling regulators, and natural products syntheses as well as elucidation of mode of actions.
He is currently actively working on development of anticancer agents inhibiting AIMP2-DX2 or STAT3 and anti-angiogenic agents inhibiting HIF1 for the treatment of retinal neovascularization.
He graduated from Seoul National University with a B.S. degree in Pharmacy in 1975 and received Ph.D. degree from University of Pittsburgh in 1987.
He has been a president of Pharmaceutical Society of Korea (2013-2014) and Korean Society of Organic Synthesis (2015).
Currently, he is a full member of The Korean Academy of Science and Technology, a Fellow of Asian Federation for Medicinal Chemistry, and a Member of Editorial Board of Asian Journal of Organic Chemistry.
His research interests include development of selective cellular signaling regulators, and natural products syntheses as well as elucidation of mode of actions.
He is currently actively working on development of anticancer agents inhibiting AIMP2-DX2 or STAT3 and anti-angiogenic agents inhibiting HIF1 for the treatment of retinal neovascularization.
Protein Modification: from Chemical Biology to Drug Discovery (PL04)
Prof. Edward TATE
IMPERIAL COLLEGE LONDON
London, United Kingdom
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.
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.
Novel Fluorogenic Probes for In Vivo Imaging of Tiny Tumors and Super-Resolution Imaging in Living Cells (PL18)
Prof. Yasuteru URANO
THE UNIVERSITY OF TOKYO
Tokyo, Japan
Tokyo, Japan
Name: Yasuteru URANO
Current title and position:
Professor
Graduate School of Pharmaceutical Sciences (2013-) and Graduate School of Medicine (2010-) The University of Tokyo
Research field:
Chemical Biology (Development of photo-functional probes)
Education and former professional experience:
Bachelor of Pharmaceutical Sciences, The University of Tokyo, 1990
Doctor of Pharmaceutical Sciences, The University of Tokyo, 1995
1997-2005 Assistant Professor, Graduate School of Pharmaceutical Sciences, The University of Tokyo
2005-2009 Associate Professor, Graduate School of Pharmaceutical Sciences, The University of Tokyo
Current title and position:
Professor
Graduate School of Pharmaceutical Sciences (2013-) and Graduate School of Medicine (2010-) The University of Tokyo
Research field:
Chemical Biology (Development of photo-functional probes)
Education and former professional experience:
Bachelor of Pharmaceutical Sciences, The University of Tokyo, 1990
Doctor of Pharmaceutical Sciences, The University of Tokyo, 1995
1997-2005 Assistant Professor, Graduate School of Pharmaceutical Sciences, The University of Tokyo
2005-2009 Associate Professor, Graduate School of Pharmaceutical Sciences, The University of Tokyo
The Design of mGluR Modulators for CNS Disorders (PL16)
Dr Michiel VAN GOOL
JANSSEN R&D
Toledo, Spain
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 Principal Scientist and Chemistry Team Leader of the mGlu2 NAM project.
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 Principal Scientist and Chemistry Team Leader of the mGlu2 NAM project.
Design of Chemical Probes Acting on Emerging Targets Assisted by Online Computational Tools (PL13)
Dr Bruno VILLOUTREIX
INSERM/UNIVERSITY PARIS DIDEROT
Paris, France
Paris, France
Dr. Bruno Villoutreix is the head of the Inserm (French National Institute of Health and Medical Research)-University Paris Diderot research unit MTi (Therapeutic Molecules in silico) that he created in 2009. This unit aims at developing new computational approaches to assist chemical biology and drug discovery projects and at applying such methods across several therapeutic areas.
Bruno has been investigating several protein targets by combining structural bioinformatics-chemoinformatics and experimental approaches in different countries, in both, the private and academic sectors.
Presently he is focusing, with several collaborators, on designing chemical compounds that target novel molecular mechanisms. He has designed a small compound that is entering Phase II clinical trial.
After completing his PhD in the U.S., he moved in a biotech company in Finland, then to Malmo General Hospital in Sweden and joined as research director and Inserm Avenir team leader a research unit located in Paris in 2001. He has also been consultant in structural bioinformatics during several years in a US big pharma.
Bruno has been investigating several protein targets by combining structural bioinformatics-chemoinformatics and experimental approaches in different countries, in both, the private and academic sectors.
Presently he is focusing, with several collaborators, on designing chemical compounds that target novel molecular mechanisms. He has designed a small compound that is entering Phase II clinical trial.
After completing his PhD in the U.S., he moved in a biotech company in Finland, then to Malmo General Hospital in Sweden and joined as research director and Inserm Avenir team leader a research unit located in Paris in 2001. He has also been consultant in structural bioinformatics during several years in a US big pharma.
Pierre Fabre Award for Therapeutic Innovation
A Scien-trepreneur Journey From Digital to In-vivo Organic Chemistry (PL23)
A Scien-trepreneur Journey From Digital to In-vivo Organic Chemistry (PL23)
Dr Alain WAGNER
CNRS/UNIVERSITY OF STRASBOURG
Illkirch, France
Illkirch, France
Alain Wagner obtained his PhD in synthetic chemistry at the University of Strasbourg in 1991. During his post-doctoral training in a start-up of the Silicon Valley (Affymax, 1991-1994) he got interested in the promising domains of catalytic antibodies and combinatorial synthesis. Alain Wagner joined CNRS in 1994 to develop projects involving solid phase chemistry, combinatorial screening and medicinal chemistry. Between 2002 and 2008 Alain took a 5 years sabbatical to found and lead Novalyst Discovery SAS a chemical technology-based company. In 2008 Alain resigned from Novalix to return to academia and found the team of Functional ChemoSystem with the objective of investigating the possibilities offered by controlling exogenous chemistry in living organisms. In 2014 Alain participated in the creation of Syndivia SAS a start-up that ambition to become a key technology provider in the field of Antibody Drug Conjugates (ADC).
Altogether Alain Wagner published more than 130 articles in peer-reviewed journals, he is an inventor of 17 patents and founder of 4 start-ups. He directed 18 PhD's and supervised more than 20 post-docs. Alain Wagner is currently Research Director 1st class at CNRS, Vice Director of LabEx MEDALIS and UMR 7199. He is member of the CoNRS section 16, and member of the scientific advisory board of eNovalys SAS, Inoviem SAS and Syndivia SAS.
A Role of SIRT2 in Cellular Response to Environmental Signals (PL05)
Dr Minoru YOSHIDA
RIKEN ADVANCED SCIENCE INSTITUTE (ASI)
Saitama, Japan
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.
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.
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
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.
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.
Keynote Speakers
Development of Potent Inhibitors of the DNA-Dependent Protein Kinase (DNA-PK) (KL03)
Dr Céline CANO
NEWCASTLE CANCER CENTRE
Newcastle upon Tyne, United Kingdom
Newcastle upon Tyne, United Kingdom
Céline studied Organic Chemistry at the University of Poitiers (France) where she received her Ph.D. degree in 2004 for research on the synthesis of biomolecules by 1,3-dipolar cycloadditions with carbohydrates. From 2004-5, she carried out post-doctoral work in the group of Professor John A. Joule at the University of Manchester working on the synthesis of analogues of cofactors of oxomolybdoenzymes.
In November 2005 she joined the Northern Institute for Cancer Research at Newcastle University as a research associate, working along Professors Roger Griffin and Bernard Golding on the synthesis of inhibitors of DNA-dependent protein kinase (DNA-PK).
She was appointed to a lectureship at Newcastle in 2008, promoted to senior lectureship in 2013, and has since played a key role in helping to establish Newcastle as an internationally recognised centre for anti-cancer drug development.
In November 2005 she joined the Northern Institute for Cancer Research at Newcastle University as a research associate, working along Professors Roger Griffin and Bernard Golding on the synthesis of inhibitors of DNA-dependent protein kinase (DNA-PK).
She was appointed to a lectureship at Newcastle in 2008, promoted to senior lectureship in 2013, and has since played a key role in helping to establish Newcastle as an internationally recognised centre for anti-cancer drug development.
Original Serotonergic Multi-Target Directed Ligands against Alzheimer's Disease (KL02)
Dr Sylvie CLAEYSEN
INSTITUT DE GÉNOMIQUE FONCTIONNELLE / CNRS / INSERM
Montpellier , France
Montpellier , France
Sylvie CLAEYSEN, PhD of the Montpellier University (1995, Molecular Biology) and permanent researcher at INSERM since 2002, conducts her research at the Institute of Functional Genomics, Montpellier, France.
She is an expert in neuropharmacology, G protein-coupled receptors (GPCR) and neurodegenerative disorders. She proposes innovative strategies to cure Alzheimer's disease (α-secretase activation, Multi-Targeted drugs), based on a deep knowledge, accumulated during the past 20 years on molecular and cellular mechanisms induced by GPCRs in neuroprotection.
In connection with a network of clinicians and chemists, she conducts ground-breaking projects to fight against this major public health concern. Sylvie has been awarded the Junior Faculty Award at the AD/PD™ 2013 (The Alzheimer's & Parkinson's Conference) and Chercheuse d'Avenir 2011 of the French Languedoc Roussillon Region. She was also a recipient of the Soroptimist International (French Union) medal (2011).
She is a regular expert for national and international funding agencies and a member of the France Alzheimer' Scientific Board.
She is an expert in neuropharmacology, G protein-coupled receptors (GPCR) and neurodegenerative disorders. She proposes innovative strategies to cure Alzheimer's disease (α-secretase activation, Multi-Targeted drugs), based on a deep knowledge, accumulated during the past 20 years on molecular and cellular mechanisms induced by GPCRs in neuroprotection.
In connection with a network of clinicians and chemists, she conducts ground-breaking projects to fight against this major public health concern. Sylvie has been awarded the Junior Faculty Award at the AD/PD™ 2013 (The Alzheimer's & Parkinson's Conference) and Chercheuse d'Avenir 2011 of the French Languedoc Roussillon Region. She was also a recipient of the Soroptimist International (French Union) medal (2011).
She is a regular expert for national and international funding agencies and a member of the France Alzheimer' Scientific Board.
Discovery of GLPG1690: a First-in-Class Autotaxin Inhibitor in Clinical Development for the Treatment of Idiopathic Pulmonary Fibrosis ( KL01)
Dr Nicolas DESROY
GALAPAGOS
Romainville, France
Romainville, France
Fragment-Based Design of ITK Inhibitors (KL06)
Dr Steven DURRANT
VERTEX PHARMACEUTICALS (EUROPE) LTD
Abingdon, United Kingdom
Abingdon, United Kingdom
Steven completed his undergraduate and postgraduate studies at the University of Bath where he carried out a PhD with Prof J.MJ Williams investigating the potential application of “catalytic chiral auxiliaries” in the Diels-Alder reaction.
On completion of his studies Steven joined Vertex Pharmaceuticals in 2001 where he is currently working. During his time with Vertex Pharmaceuticals, Steven has worked on a variety of different target classes and disease areas including immunology and oncology.
He has a particular interest in developing small molecule kinase inhibitors for the treatment of unmet medical needs,
On completion of his studies Steven joined Vertex Pharmaceuticals in 2001 where he is currently working. During his time with Vertex Pharmaceuticals, Steven has worked on a variety of different target classes and disease areas including immunology and oncology.
He has a particular interest in developing small molecule kinase inhibitors for the treatment of unmet medical needs,
E.coli Anti-Adhesives, Potential Therapeutics for Crohn's Disease? (KL08)
Dr Sébastien GOUIN
UNIVERSITY OF NANTES
Nantes, France
Nantes, France
Dr. Sébastien G. Gouin was born in Le Mans (France) in 1976. He studied Organic Chemistry at the University of Nantes (France) where he obtained his PhD in 2003.
After postdoctoral training with Prof. Paul V. Murphy at University College Dublin (Ireland), he was appointed as a CNRS researcher.
His present research in the CEISAM laboratory at the University of Nantes focuses on the synthesis of mono- and multivalent inhibitors of bacterial lectins and glycosidases.
After postdoctoral training with Prof. Paul V. Murphy at University College Dublin (Ireland), he was appointed as a CNRS researcher.
His present research in the CEISAM laboratory at the University of Nantes focuses on the synthesis of mono- and multivalent inhibitors of bacterial lectins and glycosidases.
Structure Guided Drug Discovery: Merits and Pitfalls Through the Example of Two Kinase Projects (KL04)
Dr Andras KOTSCHY
SERVIER RESEARCH INSTITUTE OF MEDICINAL CHEMISTRY
Budapest, Hungary
Budapest, Hungary
András Kotschy is the managing director of the Servier Research Institute of Medicinal Chemistry in Budapest, Hungary.
After completing his PhD degree in 1995 he joined the staff of Eötvös Loránd University where he rose through the ranks to associate professor also completing his habilitation and obtaining a DSc degree.
His research interests included the development of new synthetic methodologies, transition metal catalysis in particular, and their application to heterocyclic chemistry. In 2007 he joined the newly established Servier Research Institute of Medicinal Chemistry as director of the Discovery Chemistry division and in 2015 he became director of SRIMC. Since then he has been in charge of multiple research projects in oncology and metabolism.
András Kotschy is the author of 54 refereed publications, 1 book, and 2 book chapters. He is also the recipient of multiple scientific awards and fellowships.
After completing his PhD degree in 1995 he joined the staff of Eötvös Loránd University where he rose through the ranks to associate professor also completing his habilitation and obtaining a DSc degree.
His research interests included the development of new synthetic methodologies, transition metal catalysis in particular, and their application to heterocyclic chemistry. In 2007 he joined the newly established Servier Research Institute of Medicinal Chemistry as director of the Discovery Chemistry division and in 2015 he became director of SRIMC. Since then he has been in charge of multiple research projects in oncology and metabolism.
András Kotschy is the author of 54 refereed publications, 1 book, and 2 book chapters. He is also the recipient of multiple scientific awards and fellowships.
NMR for Chemical Biology and Drug Discovery (KL05)
Dr Isabelle KRIMM
CNRS / UNIVERSITY OF LYON 1
Lyon, France
Lyon, France
Isabelle Krimm, researcher at CNRS, Institut des Sciences Analytiques, CNRS, Université Lyon1, ENS-Lyon, Villeurbanne,
Isabelle Krimm is a research scientist at the France’s national scientific research centre (CNRS) since 2002. She received a Ph.D. in structural biology from the University of Lyon in 2000 and won the Young Researcher Award of Lyon the same year.
From 2000-2002, Isabelle studied lamin proteins by heteronuclear NMR at the Commissariat à l’Energie Atomique (CEA) in Saclay. In 2002, she became researcher at the Institute of Analytical Sciences where she was involved in the determination of protein 3D structures by NMR.
Subsequently, Isabelle started working on new projects related to the analysis of protein-ligand interactions, with a particular interest for fragment-based approaches for drug discovery, and created an NMR screening platform as well as her own fragment library.
In 2011, she obtained a Young Researcher ANR Grant for the project PLUS, to use protein chemical shits for the fast generation of protein-ligand 3D structures.
Isabelle Krimm is a research scientist at the France’s national scientific research centre (CNRS) since 2002. She received a Ph.D. in structural biology from the University of Lyon in 2000 and won the Young Researcher Award of Lyon the same year.
From 2000-2002, Isabelle studied lamin proteins by heteronuclear NMR at the Commissariat à l’Energie Atomique (CEA) in Saclay. In 2002, she became researcher at the Institute of Analytical Sciences where she was involved in the determination of protein 3D structures by NMR.
Subsequently, Isabelle started working on new projects related to the analysis of protein-ligand interactions, with a particular interest for fragment-based approaches for drug discovery, and created an NMR screening platform as well as her own fragment library.
In 2011, she obtained a Young Researcher ANR Grant for the project PLUS, to use protein chemical shits for the fast generation of protein-ligand 3D structures.
Inhibiting Chromatin Assembly by Targeting Histone Chaperones (KL07)
Dr Françoise OCHSENBEIN
CEA SACLAY
Gif-sur-Yvette, France
Gif-sur-Yvette, France
Group leader at CEA Saclay, and Institut of Integrative Biology of the Cell (I2BC).
Our team characterizes the structure of complexes involved in maintaining genome integrity, develop new methods for the prediction of their conformations and design inhibitory compounds capable of disrupting these interactions.
SELECTED FINANCED PROJECTS (as coordinator)
2007 -Young researcher ANR project BREAKABOUND (histone chaperone structure function and inhibition)
2013 - Collaborative ANR Project CHAPINHIB (design chaperone inhibitors)
SELECTED PUBLICATIONS (2012-2015) out of 31 publications and 4 patents
1. Jiao, Y., Seeger, K, et al. and Ochsenbein, F. (2012). Surprising complexity of the Asf1 histone chaperone-Rad53 kinase interaction. Proc Natl Acad Sci USA, Feb 21;109(8):2866-71.
2. Richet N, Liu D, et al. Ochsenbein F. (2015) Structural insight into how the human helicase subunit MCM2 may act as a histone chaperone together with ASF1 at the replication fork, Nucleic Acids Research 18;43(3):1905-17
3. Ochsenbein F, Morelli X, Verma C, (2015) Editorial of Protein-Protein Interaction Analysis and Modulation, Prog Biophys Mol Biol. Oct;119(1):1.
Our team characterizes the structure of complexes involved in maintaining genome integrity, develop new methods for the prediction of their conformations and design inhibitory compounds capable of disrupting these interactions.
SELECTED FINANCED PROJECTS (as coordinator)
2007 -Young researcher ANR project BREAKABOUND (histone chaperone structure function and inhibition)
2013 - Collaborative ANR Project CHAPINHIB (design chaperone inhibitors)
SELECTED PUBLICATIONS (2012-2015) out of 31 publications and 4 patents
1. Jiao, Y., Seeger, K, et al. and Ochsenbein, F. (2012). Surprising complexity of the Asf1 histone chaperone-Rad53 kinase interaction. Proc Natl Acad Sci USA, Feb 21;109(8):2866-71.
2. Richet N, Liu D, et al. Ochsenbein F. (2015) Structural insight into how the human helicase subunit MCM2 may act as a histone chaperone together with ASF1 at the replication fork, Nucleic Acids Research 18;43(3):1905-17
3. Ochsenbein F, Morelli X, Verma C, (2015) Editorial of Protein-Protein Interaction Analysis and Modulation, Prog Biophys Mol Biol. Oct;119(1):1.