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Harnessing cryo-EM to investigate GPCR structure and discover new medicines

This webinar is brought to you by the Science/AAAS Custom Publishing Office

Harnessing cryo-EM to investigate GPCR structure and discover new medicines

27 May 2020

12:00 p.m. ET

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G protein–coupled receptors (GPCRs) are an important family of drug targets—about one-third of all U.S. Food and Drug Administration-approved drugs target the 800 GPCR family members. Despite many success stories, there are still a significant number of GPCR-targeting drugs that never leave the preclinical testing stage. Rational drug design at both orthosteric and allosteric binding sites hold the key for exploiting GPCR targets in full. Over the last 10 years, substantial progress has been made in the structural biology of GPCRs, facilitated by structure-based drug design (SBDD) approaches. Recent progress in the field of cryo-electron microscopy (cryo-EM) has enabled researchers to consistently image proteins at resolutions in the 2.5-Å range, leading to greater biological insights into ligand recognition and GPCR activation. Together, these advances point to GPCR SBDD becoming the new normal for delivering first-in-class and best-in-class drugs.

This webinar will be presented by Matthew Belousoff from the Monash Institute of Pharmaceutical Sciences and Stacey Southall from Sosei Heptares, who will share their use of cryo-EM and how it fits into both the discovery and pharmaceutical side of GPCR research.

During this webinar, the speakers will:

  • Describe the activation of receptor complexes and the presence of multiple dynamic states
  • Discuss the advantages of Sosei Heptares’ StaR (Stabilized Receptor) technology for cryo-EM structures
  • Showcase incorporating single-particle analysis into industrial SBDD workflows
  • Receive and answer questions during the live broadcast.

This webinar will last for approximately 60 minutes.

Speaker bios

Matthew Belousoff, Ph.D.

Monash University
Clayton, Australia

Dr. Belousoff began his structural biological career in 2008 as a post-doctoral fellow, in the lab of Prof. Ada Yonath, doing X-ray crystallography on the bacterial ribosome. After returning to Australia in 2011, he has been using single particle cryo-EM as a tool for the development of new ribosomal interfering antibiotics. In early 2019 he joined the lab of Prof. Patrick Sexton at Monash Institute of Pharmaceutical Sceinces. In collaboration with Prof. Rado Danev (University of Tokyo) he helped solve over 40 GPCR structures by single particle cryo-EM, ranging from small molecule to peptide agonist structures.

Stacey Southall, Ph.D.

Sosei Heptares
Cambridge, UK

Dr. Southall studied at University of Sheffield and University of Cambridge where she developed a passion for understanding protein structure. She followed her studies with postdoctoral fellowships at UEA, the Institute of Cancer Research, and EMBL where she developed this into a desire to use protein structure information to combat disease. Stacey joined Sosei Heptares 5 years ago and leads a team focused on using biophysical and structural data to drive drug discovery for GPCRs.

Jackie Oberst, Ph.D.

Washington, DC

Dr. Oberst did her undergraduate training at the University of Maryland, College Park, and her Ph.D. in Tumor Biology at Georgetown University, Washington D.C. She combined her interests in science and writing by pursuing an M.A. in Journalism from the Philip Merrill College of Journalism at the University of Maryland, College Park. Dr. Oberst joined Science/AAAS in 2016 as the Assistant Editor for Custom Publishing. Before then she worked at Nature magazine, the Howard Hughes Medical Institute, The Endocrine Society, and the National Institutes of Mental Health.

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