Synopsis
The key role of G-protein coupled receptors (GPCRs) in human disease underpins their importance to modern medicine.
We are pleased to announce that Actelion, Switzerland will support the fifth meeting in this series on GPCR drug discovery, which will combine cutting edge medicinal chemistry with innovative structural biology and novel drug design approaches.
- New technologies for GPCR research
- Lead generation approaches
- Case studies in GPCR drug development
- Allosteric modulation
- New ligands for peptide hormone receptors
- Structural biology and drug design
- First disclosures of clinical candidates
- Medicinal chemistry case studies from leading industrial scientists
Additional features
- Evening networking reception
- Poster sessions
- Conference dinner
- Trade exhibition opportunities
- Accommodation identified for direct booking
Programme
Day 1 - Monday 15 September
- 08:30
- Registration and refreshments
- 09:25
- Opening remarks
- 09:30
- Title to be confirmed
Bernadette Byrne, Imperial College London, UK
- 10:10
- Allosteric modulation of G protein-coupled receptors: alternative ways to train slippery serpent(ine)s
David Hall, GlaxoSmithKline, UK
- 10:50
- Refreshments and exhibition
- 11:20
- Discovery of TGR5 (GPBAR1) agonists
David Piotrowski, Pfizer, US
- 12:00
- Sylvain Célanire, Addex Therapeutics, Switzerland
- 12:40
- Lunch and exhibition
- 13:40
- CRTh2: can residence time help?
Rick Roberts, Almirall, Spain
- 14:20
- tmGluR5 antagonists: from discovery to clinical development
Fabrizio Gasparini, Novartis, Switzerland
- 15:00
- CB2 agonists as novel treatments for kidney diseases
Uwe Grether, F Hoffmann-La Roche Ltd, Switzerland
- 15:40
- Refreshments and exhibition
- 16:10
- Evolving stable GPCRs for drug screening and structural analysis
Andreas Plückthun, ETH Zurich, Switzerland
- 16:50
- The structural basis for ligand efficacy in the b1-Adrenoceptor
Chris Tate, MRC Laboratory of Molecular Biology, UK
- 17:40
- Close
Day 2
- 09:00
- Molecular basis for the unique dissociation kinetics of macitentan - a novel endothelin receptor antagonist
John Gatfield, Actelion, Switzerland
- 09:40
- Structure-based drug design with G protein-coupled receptors: the discovery of highly selective M1 agonists
Giles Brown, Heptares, UK
- 10:20
- Refreshments, exhibition and posters
- 10:50
- What lessons can we learn from 20 years of chemokine receptor drug discovery?
John Cumming, AstraZeneca, UK
- 11:30
- From structure-based chemogenomic reflection to in silico prediction of GPCR-ligand interactions
Chris de Graaf, University of Amsterdam, The Netherlands
- 12:10
- Lunch, exhibition and posters (Two workshops will run by Chemical Computing Group during this two-hour session)
- 14:10
- Neuroscience
To be confirmed, Janssen, Belgium
- 14:50
- Late breaker
- 15:20
- Late breaker
- 15:50
- Refreshments, exhibition and posters
- 16:20
- Novel GPR40 agonists for the treatment of type-2 diabetes
Chafiq Hamdouchi, Lilly, US
- 17:00
- The discovery of glucagon receptor antagonists for clinical development
Emma Parmee, Merck, US
- 17:40
- Close
- 1900
- Conference dinner
Day 3
- 09:00
- GPCRs: application of a multivalent approach
Dan Long, Theravance, US
- 09:40
- Identification of novel GPR81 agonist lead series for target biology evaluation
Ola Fjellström, AstraZeneca, Sweden
- 10:10
- Refreshments
- 10:40
- GPR81 agonists for the treatment of dyslipidaemia and atherosclerosis
Richard Davenport, Takeda, UK
- 11:05
- Structural insights in the molecular causes of congenital stationary night blindness
Ankita Singhal, Paul Scherrer Institute, Switzerland
- 11:30
- Crystal structures of the human adenosine A2A receptor: from agonist binding to the activation mechanism
Guillaume Lebon, CNRS, France
- 12:10
- Close
Accessibility Grants
SCI accessibility grants are available to support SCI members with disabilities, long term health conditions, those who require a carer, and members who are nursing parents to attend SCI events. Download an application form to apply for a grant.
Venue and Contact
Fees
GB£310 . . . . . . . . .SCI / RSC Member
GB£95. . . . . . . . . . SCI / RSC Student
GB£390. . . . . . . . . Non-Member
GB£130 . . . . . . . . .Non Member Student
Discounted rates will be offered to RSC and SCI student members and some bursaries will be available.
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Booking Process/Deadlines
Booking terms and conditions
CPD Info
SCI Members attending this meeting are able to claim CPD points.
Additional Info
Organising Committee
Adrian Hall, UCB (Co-chairman)
Simon Peace, GlaxoSmithKline (Co-chairman)
Xavier Leroy, Actelion
Caroline Low, Consultant
Jon Mason, Heptares
David Miller, Takeda
Exhibition and Sponsorship
Please contact the secretariat for details of exhibitor and sponsorship opportunities.