5th RSC/SCI Symposium on GPCRs in Medicinal Chemistry

5th RSC/SCI Symposium on GPCRs in Medicinal Chemistry
15 - 17 September 2014, Basel, Switzerland


The key role of G protein-coupled receptors (GPCRs) in human disease underpins their importance to modern medicine.

This meeting combineed cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches. This meeting was sponsored by Actelion, Switzerland.

Themes of the meeting

  • New technologies for GPCR research
  • Lead generation approaches
  • Case studies in GPCR drug development
  • Allosteric modulation
  • New ligands for peptide hormone receptors


Bernadette Byrne
Imperial College London
Exploring GPCR structure and function

David Hall
Allosteric modulation of G protein-coupled receptors: alternative ways to train slippery serpent(ine)s

David Piotrowski
Discovery of TGR5 (GPBAR1) agonists

Sylvain Célanire
Addex Therapeutics
Progress towards novel metabotropic glutamate receptor 4 (mGlu4) positive allosteric modulators for CNS disorders

Rick Roberts
CRTh2: can residence time help?

Fabrizio Gasparini
mGluR5 antagonists: from discovery to clinical development

Uwe Grether
F Hoffmann-La Roche Ltd
CB2 agonists as novel treatments for kidney diseases

Andreas Plückthun
ETH Zurich
Evolving stable GPCRs for drug screening and structural analysis

Chris Tate
MRC Laboratory of Molecular Biology
The structural basis for ligand efficacy in the b-Adrenoceptor 1

John Gatfield
Molecular basis for the unique dissociation kinetics of macitentan - a novel endothelin receptor antagonist

Giles Brown
Structure-based drug design with G protein-coupled receptors: the discovery of highly selective M1 agonists

John Cumming
What lessons can we learn from 20 years of chemokine receptor drug discovery?

Chris de Graaf
VU University Amsterdam
From structure-based chemogenomic reflection to in silico prediction of GPCR-ligand interactions

Susana Conde
Identification of new selective, orally active mGluR5 positive allosteric modulators (PAM): lead generation SAR and effects in animal models of schizophrenia

Chafiq Hamdouchi
Novel GPR40 agonists for the treatment of type-2 diabetes

Emma Parmee
The discovery of glucagon receptor antagonists for clinical development

Dan Long
GPCRs: application of a multivalent approach

Ola Fjellström
Identification of novel GPR81 agonist lead series for target biology evaluation

Richard Davenport
GPR81 agonists for the treatment of dyslipidaemia and atherosclerosis

Ankita Singhal
Paul Scherrer Institute
Structural insights in the molecular causes of congenital stationary night blindness

Guillaume Lebon
Crystal structures of the human adenosine A receptor: from agonist binding to the activation 2A mechanism