Joint Colloquium on G Protein-Coupled Receptors: Symposium II - GPCR Structural Biology and Drug Discovery
Tuesday May 11, 2021
Eastern Time (ET)
Tremendous scientific advancements over the last decade indicate that GPCR physiology and pharmacology are much more complex than originally thought and that it may be possible to exploit this complexity to treat a wide variety of diseases. The objective of this colloquium is to expose scientists to recent discoveries and multidisciplinary approaches used to study GPCRs and provide opportunities for establishing collaborations that bridge complementary interests.
The two-day event, held May 10-11 in the EB virtual platform, will feature speakers who have made exciting discoveries in GPCR research that range from molecular to systems biology, basic research to translational studies, and pharmacology to biochemistry to physiology.
Thanks to the generosity of our sponsors and support from ASPET, ASBMB, and APS, a ticket for the colloquium is being provided at no extra charge with your paid registration to Experimental Biology.
- Cambridge University
Molecular Basis for High-affinity Agonist Binding at the Beta1-adrenoceptor
Coupling of either a G protein or beta-arrestin to the beta1-adrenoceptor increases its affinity for agonists. We have determined structures of the beta1 receptor coupled either to arrestin or a G protein mimetic and compared them to structures of the receptor in an inactive state bound to the same ligands. This has defined the ligand-specific and coupler-specific allosteric effects of coupling at the intracellular surface of the receptor on the orthosteric binding pocket.
- University of North Carolina-Chapel Hill Medical School
New Technologies for Structure-guided GPCR Drug Discovery
- University of Pennsylvania
G Protein-Coupled Olfactory Receptors: Novel Insights into Responsiveness and Mechano-sensitivity
This talk aims to address two questions about G-protein coupled odorant receptors. (1) Why do some odorant receptors respond much broadly to odorants than others within the same subfamily (i.e., sharing high sequence homology)? (2) What is the physiological significance of intrinsic mechano-sensitivity of odorant receptors and olfactory sensory neurons?
- Duke University Medical Center
Molecular Mechanisms of Biased Signaling at the Angiotensin Receptor
The angiotensin II type 1 receptor (AT1R) is a premier model system for studies of biased agonism in GPCRs because small substitutions within the sequence of the angiotensin II octapeptide can lead to bias either towards Gq protein-mediated or β-arrestin-mediated signaling. Here we use X-ray crystallography and double electron-electron resonance spectroscopy to show that different classes of biased ligands have distinct, characteristic effects on the conformational heterogeneity of the AT1R.