Vsevolod Gurevich to Speak on Designer Arrestins at GPCR Conference, May 22-23, 2014, Cambridge, MA
Dr. Vsevolod Gurevich will speak at the GPCR Structure, Function and Drug Discovery Conference, to be held May 22-23, 2014 in Cambridge, MA.
- (1888PressRelease) February 12, 2014 - Dr. Gurevich, a Professor of Pharmacology at Vanderbilt University, will present about "Designer Arrestins: Creating Receptor Specificity and Signaling Bias," will discuss how arrestins are versatile signaling receptors. They preferentially bind active phosphorylated GPCRs, block further G protein activation, orchestrate receptor trafficking, and redirect signaling to alternative pathways.
Professor Gurevich will share how targeted reengineering of arrestins yielded mutants with special functional characteristics. These included: "enhanced" forms that tightly bind unphosphorylated active GPCRs and compensate for defective receptor phosphorylation, and variants of inherently promiscuous non-visual arrestins with high preference for particular GPCRs.
Manipulation of elements engaged by MAP kinases also yielded arrestins that bind all kinases in JNK pathway but do not promote JNK activation, thereby acting as dominant-negative silent scaffolds that recruit these kinases away from productive scaffolds and suppress JNK activity in the cell.
Selective modification of arrestin binding to other partners enables channeling of signaling in desired direction, which is critical for treatment of most genetic and acquired disorders. Thus, reengineered signaling proteins are novel molecular tools with virtually unlimited therapeutic potential.
For more information about the conference, please visit www.gtcbio.com/gpcr.
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