CHISHIKI

Drug Discovery

Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification

By Greg Osborne | Nov 26, 2019

About the Conference

Drug Discovery 2019

The European Laboratory Research & Innovation Group (ELRIG)

5 – 6 November 2019

ACC, Liverpool, UK

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Summary          

Greg Osborne, Principal Scientist, Molecular Pharmacology at Sosei Heptares, recently attended The European Laboratory Research & Innovation Group (ELRIG) conference named Drug Discovery 2019 at ACC in Liverpool, UK on November 6 and presented on “Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification”, at Hit Finding Strategies session.

 

Abstract

G protein-coupled receptors (GPCRs) are an important and long-standing family of drug targets. Despite many historical success stories, today there are still a significant number of GPCRs with compelling pre-clinical validation that remain highly challenging for drug discovery.

Over the last 10 years there has been great progress in the structural biology of GPCRs facilitating Structure-Based Drug Design (SBDD) approaches. Sosei Heptares uses its proprietary StaR® technology to thermostabilise GPCRs by mutagenesis into a chosen conformational state. These purified proteins can then be used for biophysical screening techniques and crystallisation to yield X-ray structures with multiple ligands.

This presentation will illustrate how at Sosei Heptares we use our StaR® approach for GPCR structure and hit identification. A series of short case studies will review how we have used the structural identification of orthosteric and allosteric binding sites for SBDD and highlight how this approach has provided differentiated series over empirical methods.

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