New Vistas in GPCR Research: the Dawn of an Exciting Drug Discovery Era?
Annual One-Day Meeting on Medicinal Chemistry of SRC & KVCV
Braine-L'Alleud, Belgium November 21, 2014
L01 - GPCR-ligand Structures through the Looking Glass: Computer-Aided Prediction of GPCR-Ligand Interactions
Dr Chris DE GRAAF
VU UNIVERSITY AMSTERDAM, Cambridge, United Kingdom Read more
Dr Chris DE GRAAF
Chris de Graaf performed his PhD research in the Division Molecular Toxicology at VU University Amsterdam on computational ligand binding mode and affinity predictions in cytochrome P450 enzymes (2002-2006, cum laude). He then joined the Structural Chemogenomics group (Dr. Rognan) at Université de Strasbourg as post-doctoral fellow and worked in collaboration with AstraZeneca Pharmaceuticals on the development and application of novel G protein-coupled receptor modeling techniques (2006-2008). In 2009 Chris de Graaf was appointed assistant professor in the Division Medicinal Chemistry at VU University Amsterdam. In this interdisciplinary research environment Dr. De Graaf and his team have developed several in silico modeling methods that steer synthetic medicinal chemistry and molecular pharmacology programs. Dr. De Graaf has recently been appointed vice chair of the COST Action CM1207 GLISTEN to oversee the planning, implementation and coordination of this European G Protein-Coupled Receptor research network.
L03 - Dual A2A-NR2B Antagonists: Potential for Unprecedented Activity in Parkinson’s Disease
His training background is in organic synthesis at the University of Namur (Belgium) in the laboratory of Professor Alain Krief. In 2000, Joel mercier moved to the PET research center at the University of Louvain-la-Neuve where he was involved in the radiolabeling development of various [18F]-fluorinated tracers. Since 2001, he is working in the medicinal chemistry Team at UCB Biopharma (Belgium) where he is currently associate director. Joel Mercier has over 10 years of experience working on and leading various CNS drug discovery projects (SV2 proteins, GPCRs, ion channels). In 2007, taking benefit of his experience in PET radiochemistry, he initiated the discovery of the first SV2A PET ligands. Since 2012, he is responsible of leading and coordinating all the PET ligand development activities within UCB Biopharma.
L05 - Developing Ligands to Validate the Role of Receptors for Long-chain Fatty Acids in the Treatment of Type II Diabetes
Prof. Graeme MILLIGAN
UNIVERSITY OF GLASGOW, Glasgow, United Kingdom Read more
Prof. Graeme MILLIGAN
1994-present: Professor of Molecular Pharmacology, University of Glasgow, Glasgow, Scotland, U.K.
2010-present: Dean of Research, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow, Scotland, U.K.
2012-present: Gardiner Professor of Biochemistry, University of Glasgow, Glasgow, Scotland, U.K.
My main research group centres on the function, structure and regulation of G protein-coupled receptors (GPCRs) and their interacting proteins. I have published more than 500 peer-reviewed articles on these topics. My research has been cited more than 20,000 times
1976-1979: University of Birmingham: Graduated with B.Sc. (Hons. 1st class) Biochemistry.
1979-1982: University of Nottingham: Graduated with Ph.D.
1982-1985: Fogarty International Visiting Fellow, National Institute of Mental Health
Bethesda, MD. U.S.A.
L06 - Positive Allosteric Modulators of mGlu2 Receptors for the Treatment of CNS Disorders
Dr Daniel OEHLRICH
JOHNSON & JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT, Beerse, Belgium Read more
Dr Daniel OEHLRICH
Daniel Oehlrich received his MChem in Chemistry from the University of Exeter, U.K., in 2001. He subsequently in 2004 received his Ph.D. from Warwick University, U.K., under the supervision of Prof. Michael Shipman, where he was successful in the total synthesis of Luminacin D, a natural anti-angiogenic molecule. He did postdoctoral studies at University of Manchester, U.K., where he worked for Prof. E. J. Thomas; the topic of the work was “The Target Synthesis of Novel Anti-Alzheimer Compounds”. He joined the department of medicinal chemistry of Johnson and Johnson in 2005, initially in Toledo, Spain, before transferring to Janssen Research and Development, Beerse, Belgium, in 2009. He is a senior scientist and project team leader in medicinal chemistry currently working on the synthesis of novel BACE1 inhibitors and previously researching positive allosteric modulators for mGlu2 and novel GSMs.
L04 - Biased Ligands, Allosteric Modulation: New Technological Approaches
Stephan Schann is in charge of research activities at Domain Therapeutics, a biopharmaceutical company focusing on GPCR drug discovery and early development. He is managing different projects from the gene to the optimized lead, such as the mGluR4 PAM program for Parkinson’s disease, partnered with Prexton Therapeutics, as well as the mGluR2 NAM or mGluR3 PAM programs for Alzheimer’s and Parkinson’s diseases respectively. He is also responsible for DTect-All™ and BioSens-All™, the two proprietary technological platforms used for drug discovery on challenging GPCRs. Before, Stephan spent six years at Faust Pharmaceuticals, a CNS clinical biopharmaceutical company, where he set up the medicinal chemistry activity. Prior to his position at Faust Pharmaceuticals, Stephan was team leader at EvotecOAI, Abingdon, UK from 2001 to 2003. Stephan received his PhD from University de Strasbourg, France in 2001 working on the synthesis of the first imidazoline I1-selective ligands.
L02 - Nanobodies to Study GPCR Transmembrane Signaling: From Structures to Function to Drugs
Jan Steyaert ir. Ph.D. is a full professor at the Vrije Universiteit Brussel (VUB). He teaches biochemistry and protein engineering for chemists, biologists and bio-engineers.
Jan Steyaert made his Ph.D. at the protein engineering department of Plant Genetic Systems (currently Bayer Crop science). After a postdoc in the International Livestock Research Institute (Nairobi, Kenya), he joined the laboratory of Structural Biology of Lode Wyns. Skilled in enzymology, structural biology and antibody technology. Experienced in steady state and pre-steady state kinetics, protein expression and purification, spectroscopic techniques, structural biology methods and phage display. He is co-founder of Ablynx (www.ablynx.com) and Agrosafve (www.agrosafve.com), two biotech spin-offs that valorize a unique family of single domain antibodies (nanobodies) derived from camels.
Last years, the Steyaert lab pioneered the use of nanobodies for chaperone-assisted X-ray crystallography (www.steyaertlab.eu), aiming at the highest hanging fruits of structural biology including membrane proteins, amyloidogenic proteins, and now also (transient) multiprotein complexes. The elucidation of the first GPCR structures in the agonist-bound active state demonstrate the power of Nanobodies to stabilize G protein coupled receptor conformational states including transmembrane signalling complexes. Recent work focusses on exploiting the conformational complexity of therapeutic targets for Nanobody-enabled drug discovery.
Jan Steyaert holds a Ph.D in Bioengineering Sciences from the VUB. He is currently Director of the Structural Biology Brussels lab (VUB) and Vice-Director and groupleader of the Structural Biology Research center of the Vlaams Instituut voor Biotechnologie (VIB).
OC03 - Identification of Modulators for SUCNR1 BY Screening of a SOSA Library with a Bioluminescent cAMP Assay
Mrs Julie GILISSEN
ULG, Liege, Belgium
OC01 - Discovery of Donecopride: Design of Dual 5-HT4R Agonists/AChE Inhibitors Multi-Target Directed Ligands for Alzheimer's Disease Treatment
Christophe Rochais received his Engineer Diploma in Chemistry from the Ecole Nationale Supérieure de Chimie de Mulhouse (ENSCMu) in 2002, and his PhD in the group or Prof. S. Rault from the University of Caen Basse-Normandie (2002-2005). After a post-doctoral fellowship that he completed in the Centre for Biomolecular Sciences of the University of Nottingham under the supervision of Pr Peter M. Fischer, he was appointed Lecturer in Organic Chemistry in the School of Pharmacy at the University of Caen Basse-Normandie in 2007 and in since January 2014 he assumed the position of Professor in Organic Chemistry. His research interests include medicinal chemistry program in the field of enzymatic inhibition and receptor modulation in order to develop pharmacological tools and bioactive compounds. Since 2012 he is leading an ANR JCJC program MALAD dedicated to the development of pleiotropic agents of interest in the treatment of Alzheimer's disease.
OC02 - Novel Histamine H1-Receptor Fluorescent Antagonists for the Study of Receptor-Ligand Interactions
Dr Leigh STODDART
UNIVERISITY OF NOTTINGHAM , Nottingham, United Kingdom Read more
Dr Leigh STODDART
Leigh Stoddart gained her PhD (2007) from the University of Glasgow, under the supervision of Professor Graeme Milligan. Her PhD focused on developing techniques to study the then newly deorphanised G protein-coupled receptors (GPCRs) for free fatty acid. In 2009, she took up a post-doctoral position with Professor Stephen Hill and Dr Stephen Briddon within the Cell Signalling Research Group at the University of Nottingham. Her main focus has been in the development of fluorescent small molecule agonists and antagonists for GPCRs, namely for the adenosine receptors and histamine H1 receptor, and their use to probe novel aspects of GPCR pharmacology.