GPCRs in Medicinal Chemistry

G-protein-coupled receptors (GPCRs) play a crucial role in transmitting chemical signals from hormones and neurotransmitters across cell membranes and converting them into cellular responses. These drive processes as diverse as cell development and proliferation, neuromodulation, metabolic disorders, inflammation, and viral infection.  As such, they are involved in many diseases and continue to represent the target of a large proportion of all modern medicinal drugs. This meeting follows the success of the first symposium held in Verona (September 2006) and is the perfect opportunity to discuss the latest ideas and developments in drug discovery with leading academic and industrial scientists.

 Organisers:  RSC Biological and Medicinal Chemistry Sector, SCI Fine Chemicals Panel and the Swedish Academy of Pharmaceutical Sciences

PROGRAMME

Monday 8 September 

Structural basis for positive versus negative efficacy of ligands in 7TM receptors - medicinal                      chemistry meets molecular pharmacology                       
Thue Schwartz (7TM Pharma and University of Copenhagen, Denmark) 

Structure and dynamics of the human β₂ adrenoceptor
Brian Kobilka (Stanford University, USA)

A journey from agonists to inverse agonists of the histamine H3 receptor                       
Frédéric Denonne (UCB, Belgium)

Challenges in the optimisation of dual histamine H1/H3 antagonists                       
Simon Hodgson (GlaxoSmithKline, UK)

The discovery of MK-0974, an orally active calcitonin gene-related  peptide (CGRP) receptor antagonist for the treatment of migraine                       
Theresa Williams (Merck, USA)

SOM230:  From drug discovery to superior tumor therapy                                   
Ian Lewis (Novartis, Switzerland)

Discovery of new, drug-like V1a antagonists: 
Lead optimisation as a journey through physico-chemical property space                       
Thomas Ryckmans (Pfizer, UK)

Tuesday 9 September 

Activation and allosteric modulation of metabotropic glutamate and GABA receptors                       
Jean-Philippe Pin (Montpellier, France)

Allosteric modulation of GPCRs                       
Jean-Philippe Rocher (Addex Pharmaceuticals, Switzerland)

 A 'fast' track to atypicality - The discovery of JNJ37822681 for the treatment of schizophrenia                        Gregor Macdonald (Johnson & Johnson, Belgium)

 An industrialized discovery engine that provides a wealth of novel chemistries for GPCR targets and validates their clinical relevance                       
Uli Hacksell (Acadia Pharmaceuticals, USA)

Discovery and pharmacological evaluation of agonists of the orphan receptor GDIR (GPR119)            
Graeme Semple (Arena Pharmaceuticals, USA)

The discovery of orally-bioavailable Ghrelin receptor agonists for the treatment of
functional bowel disorders                       
Jason Witherington (GlaxoSmithKline, UK)

 Orally available, peripherally restricted CB1 agonists as novel analgesics                      
Mirek Tomaszewski (AstraZeneca, Canada)

The discovery of novel CB1 receptor antagonists                       
Phil Cowley (Organon, Schering Plough Corporation, UK )

Wednesday 10 September

Predicting off-target effects and polypharmacology                       
Brian Shoichet (UCSF, California, USA)

Chemical tractability of the GPCR protein family                       
Udo Bauer (AstraZeneca Mölndal, Sweden)

Development of 5-HT6 receptor antagonists                          
Peter Brandt (Biovitrum, Sweden)

Discovery of novel adenosine A2A receptor antagonists for the treatment of Parkinson’s disease                        Andy Stamford (Schering-Plough, USA)

The programme also includes a poster session and the deadline for submission of abstracts is 9 June.

Full details can be found in the pdf of the meeting circular.  Please click here to open a copy.