Application of Sosei Heptares GPCR StaR® platform for Structure Based Drug Design & Hit Identification
By Mathew Leveridge, Greg Osborne, Chris de Graaf, Kirstie Bennett, Stacey Southall, Matt Barnes | Jan 28, 2020
About the Conference
SLAS(Society for Laboratory Automation and Screening(SLAS) 2020
25-29th Januray 2020
San Diego, CA
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.
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.