From the Jungle to the Synchrotron - Seven Millennia of Discovering Medicines Targeting G Protein-coupled Receptors

John Daly Lecture 2017 G protein-coupled receptors (GPCRs) are the largest family of related proteins in the human body and the site of action of around 300f prescription drugs. Drugs that target GPCRs derived from plants such as opioids, cannabinoids and alkaloids have been used as medicines for thousands of years without an understanding of their mechanism of action. Today advances in X-ray crystallography and biophysics are changing the face of GPCR drug discovery, enabling a precise understanding of the mechanisms of action of these drugs. GPCR x-ray structures are revealing an unexpected diversity in allosteric binding sites found on receptors and open up new opportunities for drug design. This lecture will provide an introduction to GPCRs, including some of the history of GPCR drug discovery finishing with an up-to-date description of the latest developments in our understanding of GPCR structures and their use in structure-based drug discovery. Dr. Marshall will deliver her lecture in memory of Dr. John Daly, a noted natural products chemist and pharmacologist in NIDDK.Air date: 5/17/2017 2:00:00 PM
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