Meet Smartox at RCS Symposium on GPCR

Jun 10 2016

News

Meet Smartox at the 6th RCS / SCI symposium on GPCR in medchem, June 13-15 in Verona Italy and let’s discuss about the VenomScreen compound library.

Symposium website: http://www.maggichurchouseevents.co.uk/bmcs/gpcrs-2016.htm

Program

Day 1 – Monday 13th June

08:30	Registration and refreshments
	Session Chair: Fabrizio Micheli, Aptuit
09:20	Opening remarks Jonathan Goldman, CEO of Aptuit, and Adrian Hall, Co-chairman of the GPCRs Organising Committee
09:30	Plenary: The seventh millennium of GPCR drug discovery Fiona Marshall, Heptares Therapeutics, UK
10:20	Insights into chemistry and biology of GPCRs from molecular modelling Irina Tikhonova, Queen’s University Belfast, UK
10:55	Refreshments, exhibition and posters
11:25	Biased agonism @ FPR2 Olivier Corminboeuf, Actelion, Switzerland
12:00	TAAR1 agonists – a new approach for the treatment of psychiatric disorders Roger Norcross, Roche Pharma Research & Early Development, Switzerland
12:30	Binding of anticholinergics to the M3 receptor: explaining kinetics by mutagenesis and molecular dynamics simulations Christofer Tautermann, Boehringer Ingelheim, Germany
13:00	Lunch, exhibition and posters
	Session Chair: Simon Peace, GlaxoSmithKline
14:00	High-resolution structure of the human GPR40 receptor bound to allosteric agonist TAK-875 Gyorgy Snell, Takeda California, USA
14:40	Design, synthesis and pharmacological profile of the GPR40 receptor agonist MK-8666 Ravi Nargund, Merck, USA
15:10	Refreshments, exhibition and posters
15:40	Comparative GPCR structure and mutagenesis analyses in ligand modelling Kasper Harpsøe, University of Copenhagen, Denmark
16:25	Close
16:30	Coaches depart for visit to Vineyard (Cantina Sociale di Soave – Soave and Valpolicella) and evening meal
21:00	Coaches leave Vineyard for Verona city centre

Day 2 – Tuesday 14th June

	Session Chair: Adrian Hall, UCB
09:30	Recent computational trends in exploring G protein-coupled receptor (GPCR) ligand recognition pathways Stefano Moro, University of Padova, Italy
10:00	Discovery of small molecule modulators of the protease activated receptor-2 (PAR2) Roland Bürli, AstraZeneca and MedImmune, UK
10:30	Refreshments, exhibition and posters
11:00	Nutrient sensing GPCR FFAR1 (GPR40): allosteric agonist binding mode and physical properties influence agonist pharmacology Bruce Ellsworth, Bristol-Myers Squibb, USA
11:30	Roles of waters to predict binding affinity, selectivity and kinetics: a key component of high end GPCR SBDD Jonathan Mason, Heptares Therapeutics, UK
12:15	Lunch, exhibition and posters
	Session Chair: Caroline Low, Consultant
13:15	Design and synthesis of highly selective 5-HT2C receptor agonists as potential novel treatment for neuropsychiatric diseases Andreas Haupt, AbbVie, Germany
13:50	Dopamine D3/D2 antagonist PF-04363467 attenuates drug-seeking behaviour without concomitant D2 side effects Travis Wager, Pfizer, USA
14:25	Discovery of mGluR2 negative allosteric modulators for the treatment of neuropsychiatric disorders Michiel Van Gool, Janssen, Belgium
15:00	Refreshments, exhibition and posters
15:30	Acquired resistance to smoothened inhibitors in cancer patients Hayley Sharpe, Cambridge Institute for Medical Research, UK
16:05	Plenary: Are we there yet? How many unique GPCR structures needed? Vsevolod (Seva) Katritch, University of Southern California, USA
	Flash poster presentation session
16:55	Investigation of G-Protein-Coupled Receptor–VEGFR2 heteroreceptor complexes using Bioluminescence Resonance Energy Transfer (BRET) Diana Alcobia, University of Nottingham, UK
16:57	Quality tuning and pharmacological characterization of cell-free synthesized G-protein coupled receptors in customized membranes Frank Bernhard, Goethe Institute, Germany
16:59	Towards metabolically stable arylsulfonamide derivatives of (aryloxy)ethyl piperidines as potent and selective 5-HT7 receptor antagonists Vittorio Canale, Jagiellonian University Medical College, Poland
17:01	New small-molecule fluorescent probes for FPR optical visualization Agostino Cilibrizzi, Imperial College London, UK
17:03	Binding paths of peptide agonists and antagonists on a Class B GPCR mapped by genetically encoded chemical probes Irene Coin, University of Leipzig, Germany
17:05	Quantifying signalling bias: a simple approach to quantify functional selectivity and agonist bias Andrew Green, DiscoveRx, UK
17:07	The impact of modifying the structure of selected hexyl arylpiperazines on the activity for 5-HT1 / 5-HT7 receptors Jolanta Jaśkowska, Cracow University of Technology, Poland
17:09	A structure-based consensus scoring scheme for selecting class-A aminergic GPCR fragments Ádám Andor Kelemen, Hungarian Academy of Sciences, Hungary
17:11	Peptide ligand SAR of bradykinin 1 receptor explained by solid-state NMR Jiafei Mao, Goethe University Frankfurt, Germany
17:13	Design and synthesis of novel heterocyclic-based chemotypes as potent and selective CB2 ligands Noha Osman, German University in Cairo, Egypt
17:15	Fragment-based discovery of subtype selective adenosine receptor ligands from homology models Anirudh Ranganathan, Stockholm University (Scilifelab), Sweden
17:17	A virtual screening platform to identify selective ligands within GPCRs subfamilies Esther Sala, Intelligent Pharma SL, Spain
17:19	The application of NanoBRET for the characterisation of subtype selective dipeptide-linked fluorescent Propranolol derivatives for human β1 and β2 adrenoceptors Lea Santu, University of Nottingham, UK
17:21	Generating accessible and novel R-groups and scaffolds for GPCR projects Giovanna Tedesco, Cresset, UK
17:23	Specific anionic lipids interaction and allosteric modulation of GPCR Hsin-Yung Yen, University of Oxford, UK
17:25	Characterisation of the kinetics of binding of orexin antagonists at the OX1 receptor Richard Mould, Heptares Therapeutics Ltd, UK
17:27	Molecular dynamics of active state GLP-1R bound to either GLP-1 or oxyntomodulin Juan Carlos Mobarec, University of Essex, UK
17:30	Poster session
19:00	Conference dinner at Aptuit
Day 3 – Wednesday 15th June
	Session Chair: David Miller, Takeda Cambridge
09:00	What happens when you thermostabilise a GPCR? Bernadette Byrne, Imperial College London, UK
09:40	An integrated ligand and structure-based approach for the rational identification of novel dual acting A2A/NR2B antagonists: value of X-Ray crystallography for understanding an A2A activity cliff Zara Sands, UCB, Belgium
10:15	Refreshments, exhibition and posters
10:45	The Confo®body technology, a new platform to enable fragment screening on GPCRs Christel Menet, Confo Therapeutics, Belgium
11:20	LPARs – recent progress and medchem approach towards LPAR5 Werngard Czechtizky, Sanofi
12:00	Closing remarks David Miller, Co-chairman of the GPCRs Organising Committee, UK
12:05	Close

Meet Smartox at RCS Symposium on GPCR

Leave a Comment

Sign Up to our Newsletter