Workshops and Seminars

1. Pre-Conference Symposia, Monday 19 March 2012

Lunch, morning and afternoon refreshements and documentation will be provided

New Directions in GPCR Small Molecule Drug Discovery
Symposium W

This multispeaker symposium will lead you through the challenges faced in GPCR drug discovery.  Topics covered will include:

• Biophysical Mapping of the Adenosine A2A Receptor
  Christopher J. Langmead, Head of Pharmacology, Heptares Therapeutics Ltd, UK
• In Silico Veritas: The Crude, the Best, and the Lucky in Computer-Aided Prediction of GPCR-Ligand Interactions
  Chris de Graaf, Assistant Professor, Medicinal Chemistry, VU University Amsterdam, The Netherlands
• Drug-Target Residence Time: An Overlooked Parameter in Drug Design and Discovery
  Laura H. Heitman, Department of Medicinal Chemistry, Leiden University / Amsterdam Centre for Drug Research, The Netherlands
• Molecular Properties Affecting Fast Dissociation from the D2 Receptor
  Gary Tresadern, Senior Scientist, Research Informatics Integrative Genomics, Janssen R&D, Spain
• Discovery of APD334, a Potent and Selective Sphingosine-1-Phosphate (S1P1) Receptor Agonist
  Robert M. Jones, Senior Director, Medicinal Chemistry, Arena Pharmaceuticals, USA

Workshop Chairman: Ad P. IJzerman, Division of Medicinal Chemistry, Leiden/AmsterdamCenter for Drug Research, The Netherlands
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Evening Seminar, Discussion and Dinners: Tuesday 20 March 2012

Registration 18.45 - Start 19.00 - End no later than 21.30.
Dinner, wine and refreshments will be included

Targeting GPCRs with Antibodies
Evening Seminar S

This interactive evening seminar will offer critical insights and discuss methods available for the development of antibody and antibody engineered product against GPCR targets.

Targeting GPCRs with Antibodies
Using antibody phage display and a proprietary Cell-Based Antibody Selection (CBAS™) technology, Affitech generated a panel of antagonistic antibodies against GPCR targets involved in cancer progression and inflammation. The generated antibodies effectively competed with ligand binding, were able to block ligand-induced signaling and cell migration, and demonstrated high cell killing activity via ADCC and/or CDC. Data showing applicability of the GPCR targeting antibodies for treatment of cancer, inflammatory and autoimmune diseases will be presented.
Sergej Kiprijanov, Vice President of Research and Preclinical Development, Affitech Research AS, Norway

A Functional Monoclonal Antibody Modulating mGlu7 Receptors
Immunisation with living cells that express recombinant mGlu/ receptors was used to generate a mGluR7-selective functional monoclonal antibody. MAB1/28 potently antagonises both, orthosteric and allosteric agonist-induced mGlu7 activities. Here we provide evidence for a bias agonist activity by MAB1/28 triggering a receptor internalisation pathway and MAPK activation, which is not utilised by small molecule orthosteric or allosteric agonists suggesting an additional possibility for modulating GPCR activities in disease or therapy.
Christoph Ullmer, Senior Principle Scientist, F. Hoffmann-La Roche, Ltd., Switzerland

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1. Post-Conference Symposia, Thursday 22 March 2012

Screening Methodologies for Drug Discovery targets
Symposium X

This is a full day multispeaker symposium addressing issues faced in screening for GPCRs targets.

• Label-Free Cellular Technologies for Primary Cell Analysis in Drug Discovery
  John Gatfield, Senior Lab Head Molecular Cell Biology, Actelion Pharmaceuticals Ltd, Switzerland
• Label-Free Technology to Unravel Molecular Mechanisms of Biased Signalling
  Andreas Bock, PhD Student, Department of Pharmacology and Toxicology, Institute of Pharmacy, University of Bonn, Germany
• A Beta-Arrestin Recruitment Assay in 1536-w Format to Identify Antagonists of a Chemokine Receptor
  Rochdi Bouhelal, Senior Scientist I, Center for Proteomic Chemistry, Novartis Institutes for Biomedical Research, Switzerland
• Application of Beta-Arrestin Screening Strategies to Aid Drug Discovery
  Xavier Leroy, Actelion Pharmaceuticals Ltd, Switzerland
• HDL-Like Discs for assaying GPCRs in Drug Discovery
  Cédric Fiez-Vandal, Postdoctoral Fellow, Novartis Pharma AG, Switzerland
• Allosteric Modulators of G Protein–Coupled Receptors: New Opportunities for Drug Discovery
  Maite de los Frailes, Director Molecular Discovery Technology, GSK, Spain
• Adenosine Receptor Heterodimers Signal Using Two Different G-Proteins
  Peter J. McCormick, Assistant Professor, University of Barcelona, Spain
• Interactive Round Table Discussion: Overcoming Challenges and the Use of Novel Technologies for GPCR Drug Discovery

Workshop Chairman: Rochdi Bouhelal, Senior Scientist I, Center for Proteomic Chemistry, Novartis Institutes for Biomedical Research, Switzerland