RICT 2014

Ehrlich Prize Winner
Natural Antitumor Macrolides Acting on Tubulin: Synthesis and Functional Exploration

Prof. Karl-Heinz ALTMANN

SCS DMCCB & SWISS FEDERAL INSTITUTE OF TECHNOLOGY, Zürich, Switzerland
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Prof. Karl-Heinz ALTMANN

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Karl-Heinz Altmann has been a Professor of Pharmaceutical Sciences at the Swiss Federal Institute of Technology (ETH) in Zürich since July 2003. Professor Altmann studied chemistry at the University of Mainz, Germany and he holds a PhD degree in organic chemistry from the University of Basel, Switzerland. From 1990 to 1996 he was a research scientist and group leader at Ciba-Geigy Central Research in Basel. In 1997 he moved to Oncology Research of Novartis Pharma, until in 2000 he was appointed the Novartis Senior Chemistry Expert. From January to July 2003 he was the acting Global Head of Chemistry of the Novartis Institutes for BioMedical Research. Research in the Altmann group is centered on the chemical synthesis of pharmaceutically relevant natural products/natural product analogs and their biological evaluation, with a particular focus on leads for anticancer and antituberculosis drug discovery.

PDE10A Inhibitors as Potential Treatments for Schizophrenia

Dr Jose Manuel BARTOLOME

JANSSEN RESEARCH & DEVELOPMENT, Toledo, Spain
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Dr Jose Manuel BARTOLOME

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José Manuel is currently Principal Scientist at the Neuroscience Medicinal Chemistry Department of Janssen R & D. He is currently the Team Leader of a Med. Chem. Team focussed on neurology and psychiatry targets. Since 1998 Jose Manuel holds a Ph.D. degree from Autónoma University of Madrid for his work on the field of CCKA antagonists. In 1997, Jose Manuel joined Janssen R&D as a Scientist in the Medicinal Chemistry department. In 2002 he was promoted to Senior Scientist and then in 2008 to Principal Scientist within the Neuroscience Medicinal Chemistry department. In this period he has been involved in more than 15 Med. Chem. Programs contributing to the successful delivery of 5 clinical candidates. He is co-author of 20 peer-reviewed articles and of more than 20 communications to international conferences and co-inventor of 33 international patent applications.

Recent Advances in Predicting Cardiac Risk during Drug Development

Dr Arthur BROWN

CHANTEST, Cleveland, United States
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Dr Arthur BROWN

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Arthur M. “Buzz” Brown, MD, PhD, trained as a cardiologist and biophysicist, is founder and CEO of ChanTest Corporation. He has 30 + years of experience in ion channel structure, function and relationship to human disease and has established world-leading ion channel departments at UTMB, Baylor College of Medicine University and Case Western Reserve University. Dr. Brown received an M.D. from the University of Manitoba, Winnipeg, Canada, a Ph.D. in Physiology from the University of London and an M.A. from the University of Oxford. Dr. Brown holds 10 issued patents concerning application of ion channel pharmacology to therapeutics. He is Adjunct Professor of Physiology and Biophysics, School of Medicine, Case Western Reserve University, a collaborator with the FDA on cardiac safety issues and the recipient of the 2013 Distinguished Service Award from the Safety Pharmacology Society.

Excursions in Uncharted Structural Space

Prof. Erick M. CARREIRA

ETH ZÜRICH, Zürich, Switzerland
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Prof. Erick M. CARREIRA

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http://www.carreira.ethz.ch/

Erick M. Carreira was born in Havana, Cuba in 1963. He obtained a B.S. degree in 1984 from the University of Illinois at Urbana­Champaign under the supervision of Scott E. Denmark and a Ph.D. degree in 1990 from Harvard University under the supervision of David A. Evans. After carrying out postdoctoral work with Peter Dervan at the California Institute of Technology through late 1992, he joined the faculty at the same institution as an assistant professor of chemistry and subsequently was promoted to the rank of associate professor of chemistry in the Spring of 1996, and full professor in Spring 1997. Since September 1998, he has been full professor of Organic Chemistry at the ETH Zürich. He is the recipient of the American Chemical Society Award in Pure Chemistry, Nobel Laureate Signature Award, Fresenius Award, a David and Lucile Packard Foundation Fellowship in Science, Alfred P. Sloan Fellowship, Camille and Henry Dreyfus Teacher Scholar Award, Merck Young Investigator Award, Eli Lilly Young Investigator Award, Pfizer Research Award, National Science Foundation CAREER Award, Arnold and Mabel Beckman Young Investigator Award, and a Camille and Henry Dreyfus New Faculty Award. He is also the recipient of the Associated Students of the California Institute of Technology Annual Award in Teaching and a Richard M. Badger Award in Teaching. His research program focuses on the asymmetric synthesis of biologically active, stereochemically complex, natural products. Target molecules are selected which pose unique challenges in asymmetric bond construction. A complex multistep synthesis endeavor provides a goal-oriented setting within which to engage in reaction innovation and design. Drawing from the areas of organometallic chemistry, coordination chemistry, and molecular recognition, Carreira's group is developing catalytic and stoichiometric reagents for asymmetric stereocontrol. Prof. Erick M. Carreira is a co-founder of SpiroChem AG, a swiss fine chemicals company active in the field of high-value-added building blocks and custom synthesis.

Novel Imidazoles as Selective TAAR1 Partial Agonists for the Treatment of Psychiatric Disorders

Dr Giuseppe CECERE

F. HOFFMANN-LA ROCHE, Basel, Switzerland
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Dr Giuseppe CECERE

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Current title and position: 2011-present-Senior Scientist, Medicinal Chemistry, F. Hoffmann-La Roche, Basel, Switzerland.
Research field: Design and synthesis of novel compounds (small molecules) for therapeutic use in the area of CNS.
Education: 2001-B.A. in chemistry at Naples University “Federico II”.2004-2008-PhD in organic chemistry at University of Cambridge (Jesus College) on “Total Synthesis of (–)-reidispongiolide A and C23-C36 Tail Analogues”. 2008-2010-Post-doctoral research fellow with Prof. David W.C. MacMillan at Princeton University on enantioselective organocatalysis (-amination of aldehydes).
Former professional experience: 2002-2004-Medicinal chemist at Merck/Rome working on HIV integrase inhibitors as antiviral agents.

Exploiting the Information Rich Output of SPR Biosensor Technology in Drug Discovery – From Target Evaluation to Fragment and Lead

Prof. Helena DANIELSON

UPPSALA UNIVERSITY, Uppsala, Sweden
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Prof. Helena DANIELSON

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Helena Danielson is Professor of Biochemistry at Uppsala University in Sweden since 2002 and Chief Scientific Officer of Beactica AB. She is a specialist in enzyme-based drug discovery and molecular recognition. Her education includes a Master of Science in Chemical Engineering at Lund University (1982) and, as a Fulbright scholar, a Master of Science in Biochemistry, University of Rochester, Rochester, NY, USA (1984), and a Ph. D. in Biochemistry at Stockholm University (1987). As a postdoc at Karolinska Institutet in Stockholm Helena Danielson started a research project on HIV protease as a drug target for AIDS, and has since expanded her research to other enzymes and diseases, more recently also with an interest in membrane receptors and neurological drug targets. Helena Danielson has focused on developing enzymology for drug discovery, and in particular biomolecular interaction analysis for detailed studies of enzyme-inhibitor interactions and other important recognition processes in the life science area. Helena Danielson co-founded Beactica AB in 2006. The company is a specialist drug discovery company that generates novel drug leads from low molecular weight fragments by integrating biomolecular interaction analysis with in silico molecular docking techniques.

Translational Biophysics: Using Biophysical Data in Medicinal Chemistry

Dr Matthias FRECH

MERCK, Darmstadt, Germany
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Dr Matthias FRECH

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Matthias is heading the department for Molecular Interaction and Biophysics (MIB) at Merck-Serono. Integrated into the “Small Molecule Platform”, the group is responsible for molecular interaction studies and protein crystallographic work, to generate insight into the mode of action by combining various biophysical methods. Fragment based lead discovery, thermodynamic signatures, interaction kinetics and protein structure are the current data packages which support the drug discovery process at Merck-Serono with biophysics. Prior to that position, he was responsible for a protein chemistry group working with different biophysical methods combined with the protein purification and analysis for structural studies and high throughput screening campaigns. Before joining Merck, he was working on protein kinases and their biochemical characterization a post doctoral fellow at the Friedrich Miescher Institute, part of the Novartis Research organisation,. As EMBO fellow he worked on nucleotide exchange factors and adaptor proteins in the p21ras signalling pathway at the CNRS Institute de Pharmacologie Moleculaire et Cellulaire in the technology park of Sophia Antipolis near Nice/ France. He accomplished his doctoral work in the department of Biophysics at the Max Plank Institute in Heidelberg focusing on molecular interaction studies of small p21ras like proteins.

Use of Peptides to Modulate Protein-Protein Interactions

Prof. Ernest GIRALT

INSTITUTE FOR RESEARCH IN BIOMEDICINE (IRB), Barcelona, Spain
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Prof. Ernest GIRALT

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Ernest Giralt is Professor of Organic Chemistry at the University of Barcelona in Spain and he is also Group Leader of a Research Group in the Institute for Research in Biomedicine (IRB Barcelona) where is the Head of the Chemistry and Molecular Pharmacology Programme. He is one of the founding members of the European Peptide Society. He has received several awards, among others the Dimitrios Theodoropoulos Award from the European Peptide Society in 2010 and recently the National Research Award (2011) from the Ministerio de Ciencia e Innovación (Spain). His major interests lie in the field of peptide synthesis and structure determination, in particular using NMR to the study of complex molecular recognition processes, with emphasis on the design of specific ligands for interaction with protein surfaces, related to possible therapeutic uses. This includes studies concerning new drug delivery systems, amyloid protein aggregation inhibitors and antitumor peptides of marine origin.

Discovery and Optimisation of a Novel Series of EZH2 Inhibitors, Challenges and Clinical Perspectives

Dr Jean-Christophe HARMANGE

CONSTELLATION PHARMACEUTICALS, Cambridge, United States
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Dr Jean-Christophe HARMANGE

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Jean-Christophe Harmange, Pharm.D., Ph.D., is an Executive Director at Constellation Pharmaceuticals. His current responsibilities include providing leadership for Drug Discovery in the areas of automation, assay development and screening, structural biology and medicinal chemistry. Prior to Constellation Pharmaceuticals, Dr. Harmange was a Director at Amgen where he led medicinal chemistry teams responsible for delivering AMG 208 and AMG 337. Prior to Amgen, Dr. Harmange occupied different positions at Eisai (Andover, MA) and at Servier (Suresnes, France). Dr. Harmange holds a Pharm. D. and a Ph.D. in organic chemistry from Paris XII University and was a postdoctoral fellow in the Laboratory of Pr. Yoshito Kishi at Harvard University.

Molecular Basis of Ligand Dissociation from GPCRs – a Molecular Dynamics and Mutagenesis Study on the Adenosine A_2A Receptor

Prof. Laura HEITMAN

UNIVERSITY OF LEIDEN, Leiden, The Netherlands
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Prof. Laura HEITMAN

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Laura H. Heitman, PhD. studied Biopharmaceutical Sciences at the University of Leiden, The Netherlands. Traineeships were performed at Medicinal Chemistry of the Leiden University, NL and at Pharmaceutical and Biological Chemistry of the School of Pharmacy in London, UK. In October 2004, she started as a PhD student on the project “Allosteric modulation of ‘reproductive’ GPCRs” at the Division of Medicinal Chemistry of Leiden University. In January 2009 she was appointed ‘tenure track’ assistant professor of molecular pharmacology in this division. Her research interests are mainly focused on understanding and improving drug-receptor interactions, and more specifically, receptor residence time and allosteric modulation of GPCRs. Laura recently obtained several grants, all allowing her to study new concepts for drug action that are so close to her heart.

The Design and Optimisation of Selective Protein Kinase C Theta Inhibitors for the Treatment of Autoimmune Diseases

Dr Juan-Miguel JIMENEZ

VERTEX PHARMACEUTICALS, Abingdon, United Kingdom
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Dr Juan-Miguel JIMENEZ

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Juan-Miguel Jimenez, Senior Director, Head of Chemistry UK, Vertex Pharmaceuticals Europe. Juan-Miguel received his Ph.D. degree in Organic Chemistry in 1993 under the supervision of Profs. Joan Bosch and Maria Luisa Bennasar in the Faculty of Pharmacy (University of Barcelona). In 1994-1995 he joined Paul Wender’s Group at Stanford University (USA), as a Fulbrigth Postdoctoral Fellow. He joined Almirall Prodesfarma in 1997 as Senior Organic Chemist and was appointed Head of Section in 2002. During the time at Almirall he participated in several projects in the area of inflammation. In 2003 he joined Vertex Pharmaceuticals (UK) as senior Project Leader and subsequently appointed Head of Chemistry in 2013 where he is currently working. He has developed leadership responsibilities for Kinase projects within several therapeutic areas, including cancer, immunology and CNS.

Cell Identity Loss in Cancer: a Source of New Biomarkers and Therapeutic Targets

Dr Saadi KHOCHBIN

JOSEPH FOURIER UNIVERSITY, Grenoble, France
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Dr Saadi KHOCHBIN

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Saadi Khochbin, Ph D, is the head of a research team and of a department at the INSERM/Grenoble University Research Centre U823. The discovery of class II histone-deacetylases (HDACs) in higher eukaryotes and the identification and functional characterization of the first cytoplasmic HDAC (HDAC6), exemplify his past contribution. His recent work on the molecular basis of haploid male genome reprogramming is now shedding light on the obscure process of male genome reorganization, and is leading to unexpected applications in cancer biology. As a consequence, a new approach to cancer has been initiated, exploring the multiple potentials of ectopic gene activations in all cancers, discovering novel oncogenic mechanisms and powerful markers, as well as pointing to unexpected new therapeutic targets.

The Lab Oddity Prevails - Discovery of pan-CDK Inhibitor BAY 1000394 (Roniciclib) for the Treatment of Cancer

Dr Ulrich LÜCKING

BAYER HEALTHCARE, Basel, Switzerland
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Dr Ulrich LÜCKING

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Ulrich Lücking is a Senior Research Scientist at Bayer Pharma AG in Berlin. He started his industrial career at the former Schering AG in 2001, working across multiple therapeutic areas, mainly in lead optimization, to successfully deliver multiple clinical candidates. His efforts were instrumental in the discovery of clinical candidates in the CDK inhibitor programs and in the Androgen Receptor Suppressor Program. Prior to joining industry, he studied chemistry at the University of Hannover (Germany). As an Erasmus student and later for his diploma work, he spent time in the laboratory of Prof. Steven V. Ley at Cambridge University (UK). In 1999 he completed his Ph.D. under the direction of Prof. Andreas Pfaltz at the Max Planck Institute für Kohlenforschung, Mülheim an der Ruhr (Germany), and then carried out postdoctoral work in the laboratories of Prof. Julius Rebek at the Scripps Research

Targeting BAX for Cancer Therapy: from Computer Screen to Mouse

Dr Luciana MARINELLI

UNIVERSITY OF NAPOLI, Napoli, Italy
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Dr Luciana MARINELLI

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Luciana Marinelli is a Medicinal Chemistry team leader in the Department of Pharmacy at the University of Naples “Federico II” (Italy). She obtained her PhD in Medicinal Chemistry in 2002 following research undertaken within the laboratories of Prof. Horst Kessler at the Insitut fur Organische Chemie und Biochemie, Technische Universitat Muenchen (Germany) working on targeting intergin receptors. Her research interests are especially in Computational Chemistry, from methodology development to its applications in Medicinal Chemistry and Biology. Her research interest focused on the discovery and development of novel anticancer drugs. She has experience leading projects with a range of antitumor molecular targets such as Integrins, Kinases, G-Quadruplex DNA, and GPCRs. She is the recipient of the 2010 FARMAINDUSTRIA AWARD of the Medicinal Chemistry Division of Italian Chemical Society. She is currently Professor of Medicinal Chemistry at the University of Naples “Federico II”, (Naples, Italy).

Polar Units and Dipolar Interactions Modulating, Conformation, Lipophilicity, and other Physicochemical Properties

Prof. Klaus MÜLLER

F. HOFFMANN-LA ROCHE, Switzerland
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Prof. Klaus MÜLLER

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Klaus Müller is Extraordinary Professor at the University of Basel. Prior to his retirement in 2009 he occupied leading positions at F. Hoffmann-La Roche AG, among them as Head of ‚Pharma New Technologies‘ and of ‚Science and Technology Relations‘ for the development of innovative technologies and scientific collaborations with external groups. He was Secretary-General and Board Member of the Roche Research Foundation until its conclusion in 2008 and since then manages the Roche Postdoc Fellowship Program. Educated as Organic Chemist at ETH Zurich, he got his PhD in 1970, undertook a 1-year postdoctoral stay in the US in physical-organic chemistry, and was then Lecturer at Harvard University, before returning to ETHZ in late 1974. He habilitated in 1977 and remained there as junior staff member before joining Roche in 1982 to develop computer-assisted molecular modeling and implementing structural biology and bioinformatics, areas where he has been active until now.

Specific Antidotes for Dabigatran: Structure-Guided Affinity Optimisation and Functional Characterisation

Dr Herbert NAR

BOEHRINGER INGELHEIM, Biberach, Germany
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Dr Herbert NAR

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Herbert Nar graduated from the Technical University Munich in Chemistry and obtained his Ph.D. from the same institute with structural studies on blue copper electron transfer proteins. In his postdoctoral work with Robert Huber at the Max-Planck-Institute für Biochemie, he determined the 3D structures of proteins involved in pterin biosynthesis and studied their enzymatic mechanisms. He joined Boehringer Ingelheim in 1995 to establish a protein crystallography laboratory. In 2000, he took over responsibility for the Structural Research Group that comprises units for protein expression and purification, biophysics of ligand binding, and NMR and protein crystallography.

High-Throughput Chemical Microarray SPR: The Biophysical Tool for Fragment Based Screening in Drug Discovery

Dr Thomas NEUMANN

GRAFFINITY PHARMACEUTICALS, Illkirch, France
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Dr Thomas NEUMANN

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Dr Thomas Neumann received his PhD in 2001 for his work on novel SPR based biosensors at the Max-Planck Institute for Polymer Research, Mainz, Germany. After having held a postdoctoral position at the Imperial College, London, UK, he joined Graffinity Pharmaceuticals in 2003. As a Senior Scientist he contributed to the technical development of the SPR platform before he was appointed Head of Screening and oversaw most of the >100 SPR screening campaigns conducted at Graffinity. With more than 13 years of experience in SPR related techniques he currently heads the operations in Heidelberg as Graffinity’s Managing Director

Discovery of TAK-632: Pan-RAF Inhibitor with Potent Antitumor Activity against BRAF and NRAS Mutant Melanomas

Dr Masanori OKANIWA

TAKEDA PHARMACEUTICAL COMPANY, Kanagawa, Japan
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Dr Masanori OKANIWA

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Masanori Okaniwa is a Principal Scientist at the Pharmaceutical Research Division of Takeda Pharmaceutical Company Limited, in Kanagawa, Japan. He is a medicinal chemist with 14 years of experience, leading several oncology drug discovery teams at Takeda. He earned his M.Sc. degree from Kyoto University for the study of organometallic reaction and received his Ph.D. degree from Kyoto Pharmaceutical University with a thesis regarding medicinal chemistry work to improve oral absorption of kinase inhibitors. He is currently a visiting post-doctoral scientist, exploring potential novel cancer therapeutic approaches in the Department of Cellular and Molecular Pharmacology, University of California, San Francisco.

Chemical Probes for Epigenetics

Dr Dafydd OWEN

PFIZER, Cambridge, United States
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Dr Dafydd OWEN

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Dafydd Owen has fifteen years of experience as a medicinal chemist in the design and synthesis of drug-like molecules for Pfizer at its Sandwich UK and Cambridge MA research sites. He is currently an Associate Research Fellow within Pfizer Worldwide Medicinal Chemistry where he leads a leads an outward looking, academically collaborative group for Pfizer, researching chemical probes for epigenetic targets. He obtained his first degree at Imperial College in 1994 before moving to the University of Cambridge to gain a PhD under the supervision of Professor Steve Ley in 1997. Having won a research fellowship for postdoctoral work, he spent 1998 with Professor Leo Paquette at Ohio State University. During his research career has delivered over fifty invited lectures and is also an author on over thirty research papers and patents. He has made contributions to three compounds currently in Pfizer’s Phase I/II portfolio. In 2009 he was the recipient of a Pfizer Worldwide R&D People Leader Award. In the same year he was selected as an ACS Organic Division Young Industrial Investigator, receiving his award at the 2009 Fall ACS National Meeting in Washington DC.

Design and Applications of Protein Epitope Mimetics

Prof. John ROBINSON

UNIVERSITY OF ZÜRICH, Zürich, Switzerland
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Prof. John ROBINSON

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John Robinson studied chemistry at University College, London, where he was awarded the B.Sc. degree in 1974. He completed his Ph.D. at Cambridge University in 1977, under the supervision of Professor A. R. Battersby. With a Royal Society Postdoctoral Fellowship, he subsequently carried out postdoctoral work in the Biochemistry Institute of the University of Karlsruhe, before joining the Chemistry Department of Southampton University, UK in 1979 as a lecturer. In 1987, he became senior lecturer, and moved to Zurich as Full Professor of Organic Chemistry in 1989.

Pseudo-Natural Product Synthesis and Drug Applications

Prof. Hiroaki SUGA

UNIVERSITY OF TOKYO, Tokyo, Japan
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Prof. Hiroaki SUGA

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Professor, Department of Chemistry, Graduate School of Science, The University of Tokyo Research Fields: Chemical Biology and Biotechnology Ph.D. at MIT (1994), Post-doctoral Fellow at MGH (1994-1997), Assistant Professor at SUNY Buffalo (1997-2002), Associate Professor at SUNY Buffalo (2002-2003), Associate Professor at RCAST The University of Tokyo (2003-2005), Professor at RCAST (2005-2010), Professor at the present position (2010-present), PeptiDream Inc. Tokyo Founder and Board Member (2006-present)

2-Clips Peptides: A Novel Class of Biopharmaceuticals

Prof. Peter TIMMERMAN

PEPSCAN THERAPEUTICS, Lelystad, The Netherlands
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Prof. Peter TIMMERMAN

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Peter Timmerman, PhD. Chief Scientific Officer (CSO) at Pepscan Therapeutics Peter Timmerman studied Organic and Analytical Chemistry at the ‘Vrije Universiteit’ of Amsterdam (1984-1989). He obtained a PhD-degree in Supramolecular Chemistry (summa cum laude) from the University of Twente with David N. Reinhoudt (1994). He was Assistant Professor in Supramolecular Chemistry at the University of Twente from 1995-2001, whereafter he joined Pepscan Therapeutics in 2001. He is the inventor of Pepscan’s proprietary and broadly applicable ‘2-CLIPS’ technology for conformationally constraining peptides. The technology is a.o. applied to the mapping of conformational and discontinuous antibody binding sites. Lately, Bicycle Therapeutics was granted a non-exclusive license on the CLIPS-technology for development of therapeutic 2-CLIPS peptides. Timmerman also led the development of a therapeutic peptide-based anti-VEGF-vaccine that is currently in Phase-IIa clinical testing. Since March 2007 he holds a Special Chair in ‘Protein Mimetic Chemistry’ at the Faculty of Science of the University of Amsterdam. Timmerman is co-author of >80 peer-reviewed scientific papers and >10 patents.

Genotoxicity Screening can guide Lead Optimisation and Reduce Late Stage Attrition

Prof. Richard WALMSLEY

UNIVERSITY OF MANCHESTER, Manchester, United Kingdom
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Prof. Richard WALMSLEY

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RMW is Founder and CSO of Gentronix Ltd (established 1999) and Professor of Genetics at University of Manchester. Educated at the University of Kent, 1975-1981: B.Sc. Microbiology; Ph.D. Genetics Professional experience: Research fellow at University of Chicago; Lecturer, Senior lecturer UMIST/University of Manchester. Primary research field: genetic toxicology. The laboratory has produced a number of accurate genotoxicity tests, which can be deployed either in early high throughput screening or during later stage hazard assessment. The human cell GreenScreen HC and BlueScreen HC GADD45a reporter assays have now been used to generate data from over 12000 compounds.

Strategies to Target Protein-Protein Interactions: from Discovery to Clinical Development

Prof. Shaomeng WANG

UNIVERSITY OF MICHIGAN, Michigan, United States
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Prof. Shaomeng WANG

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Dr. Wang received his B.S. in Chemistry from Peking University in 1986 and his Ph.D. in Chemistry from Case Western Reserve University in 1992. Dr. Wang did his postdoctoral training in drug design at the National Cancer Institute, NIH between1992-1996. Dr. Wang was Assistant Professor at Georgetown University from 1996-2000 and Associate Professor from 2000-2001. Dr. Wang joined the faculty at the University of Michigan Medical School as a tenured Associate Professor in 2001 and was promoted to Professor in 2006. Dr. Wang was named the Warner-Lambert/Parke-Davis Professor in Medicine in 2007. Dr. Wang serves as the Co-Director of the Molecular Therapeutics Program at the University of Michigan Comprehensive Cancer Center and is the Director of the Cancer Drug Discovery Program at the University of Michigan. Dr. Wang is the Editor-in-Chief for Journal of Medicinal Chemistry, a premier international journal in medicinal chemistry and drug discovery by the American Chemical Society and serves on the editorial board for several international journals. Dr. Wang has published more than 200 papers in peer-reviewed scientific journals and 100+ meeting abstracts, and is an inventor on more than 40 patents and patent applications. In addition to his academic role, Dr Wang is a co-founder of Ascenta Therapeutics and Ascentage Pharma, which were established to develop innovative anticancer medicines with technologies licensed mainly from the University of Michigan.

Identification of Cell-penetrating Compounds and their Use for Intracellular Delivery of Cathepsin D Inhibitors

Prof. Muriel AMBLARD

CNRS-UNIVERSTY OF MONTPELLIER I, Montpellier, France
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Prof. Muriel AMBLARD

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Muriel Amblard obtained her PhD in Organic Chemistry at the University of Montpellier under the supervision of Prof Jean Martinez in 1991. She joined the group of Dr Paul Anderson at Merck Sharp & Dohm in West point (Pennsylvania, USA) as a post-doctoral fellow. In 1996, she obtained a position at the Laboratory of Amino Acid Peptide and Protein in Montpellier as a CR CNRS researcher. She became a CNRS senior researcher (DR2 CNRS) and a team leader at the Institute of Biomolecules Max Mousseron in 2007. Her research interests are mainly at the interface of chemistry, biology and analysis. She developed a number of potent receptor agonists and antagonists of several peptide hormones. Related to medicinal chemistry programs, she designed and synthesized small molecules as multifunctional platforms. Her recent work on the design and development of constrained β-amino acid and dipeptide mimic oligomers allowed to identify highly predictable and stable helical molecular architectures. Some of them were used as intracellular penetrating compounds and were successfully applied for delivery of Cathepsin D inhibitor. A part of her research program is devoted to the development of peptide-based biopolymers by new approaches relying on bottom up polymerisation of peptide-activated monomer.

Silicon-containing Tetrahydrocyclopenta[c]acridine Derivatives as CDKs Inhibitors: Design, Organometallic Synthesis, Metabolic Stability and Optimisation

Prof. Philippe BELMONT

UNIVERSITY PARIS DESCARTES, Paris, France
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Prof. Philippe BELMONT

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Philippe Belmont was born in Paris in 1970. He grew up in the French Caribbean where he started a BS degree in Biology and Biochemistry. In 1990 he moved to the University Joseph Fourier (Grenoble, France), where in 1996 he obtained a PhD in Bioorganic Chemistry (Advisor: Dr M. Demeunynck/Pr J Lhomme). Then, he moved successively as a post-doctoral fellow at Case Western Reserve University (Professor A. J. Pearson, Cleveland, USA) and to the Collège de France (Pr J.-M. Lehn/Dr J.-P. Vigneron, Paris, France). In 2000 he joined the group of Pr M. A. Ciufolini as a CR CNRS researcher (ICBMS Intitute, UMR CNRS 5246, Lyon, France). He obtained in 2004 the habilitation diploma and started then an autonomous career. In 2009, Philippe Belmont was awarded the CNRS bronze medal and then joined the Institut Curie (UMR CNRS 176) with an ATIP fellowship to lead an independent research group. In 2011 he succeeded in becoming a CNRS senior researcher (DR2 CNRS), but chose the same year an appointment as a full Professor of organic chemistry at the University Paris Descartes, School of Pharmacy (UMR CNRS 8638). His field of interest and expertise are in organometallic chemistry (Au, Ag, Co, Rh) devoted to the original access to various heterocyclic structures in view of studying their biological properties, in particular against tumors (e.g. kinases inhibition).

Innovative Fluorescent-Based Approaches to GPCR Screening and Functional Architecture Studies

Prof. Dominique BONNET

UNIVERSITY OF STRASBOURG, Illkirch, France
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Prof. Dominique BONNET

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Dominique Bonnet is currently senior researcher at the French National Centre for Scientific Research (CNRS), within the Laboratoire d’Innovation Thérapeutique (UMR 7200) at the University of Strasbourg. His research interests are mainly focused on developing chemical tools and generic methods to accelerate the discovery of GPCR probes and drug candidates. Prior to join the CNRS in 2004, he got a Ph.D in Organic Chemistry in October 2000 from Lille 2 University, in the field of chemical ligation to facilitate the access to biomolecules for immunotherapeutic applications. Afterwards, he moved to the University of Southampton (UK) as a research assistant on a project aiming at synthesizing original heterocyclic scaffolds for combinatorial chemistry. From 2001 to 2003, he worked as a project leader in chemistry at Sedac-Therapeutics in Lille. He is also co-founder of Immune Targeting System Ltd, a London biotechnology company, developing fully synthetic vaccines against mutative viruses.

Combining Organic Synthesis, Software Development and Biochemistry for the Design and Discovery of Prolyl oligopeptidase Inhibitors

Prof. Nicolas MOITESSIER

MCGILL UNIVERSITY, Montreal, Canada
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Prof. Nicolas MOITESSIER

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Nicolas Moitessier is an Associate Professor at McGill University, Montréal, Canada. Nic Moitessier received his undergraduate training and his PhD from Université Henri Poincaré-Nancy I (France) with a major focus of carbohydrate chemistry and computer aided drug design. In 1998, he moved to Montréal where his interests involved the docking study and the asymmetric synthesis of conformationally constrained enzyme inhibitors. In 2001, he moved back to Nancy to start an academic career (Chargé de Recherche, CNRS) then back to Montréal in 2003 (Assistant Professor, McGill University). In 2009, He was promoted to Associate Professor. His current research interests integrates computational chemistry and organic/medicinal chemistry, spanning from software development and computational chemistry to sugar chemistry and asymmetric synthesis. In 2008, he received the first Reginald Fessenden Professorship in innovation for the development of the Forecaster platform in drug discovery now distributed by Molecular Forecaster, a company he co-founded in 2010. In 2009, he was awarded the AstraZeneca Award in Chemistry.