CHISHIKI

Drug Discovery

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

By Mathew Leveridge et al. | Jan 28, 2020

About the Conference

SLAS(Society for Laboratory Automation and Screening(SLAS) 2020

25-29th Januray 2020

San Diego, CA

Conference Website

 

Summary         

Mathew Leveridge, Senior Scientist, Pharmacology, attended the SLAS (Society for Laboratory Automation and Screening) 2020 conference in San Diego on 25-29th Jan to present on Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification.

 

Poster 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 poster will illustrate how at Sosei Heptares we use our StaR® approach for GPCR structure and hit identification.

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