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Pharmacology

2009

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Full-Text Articles in Cell Biology

Identification Of A Conserved Cluster In The Rh Domain Of Grk Critical For Activation By Gpcrs, Faiza Baameur Dec 2009

Identification Of A Conserved Cluster In The Rh Domain Of Grk Critical For Activation By Gpcrs, Faiza Baameur

UT GSBS Dissertations and Theses (Open Access)

One of the most critical aspects of G Protein Coupled Receptors (GPCRs) regulation is their rapid and acute desensitization following agonist stimulation. Phosphorylation of these receptors by GPCR kinases (GRK) is a major mechanism of desensitization. Considerable evidence from studies of rhodopsin kinase and GRK2 suggests there is an allosteric docking site for the receptor distinct from the GRK catalytic site. While the agonist-activated GPCR appears crucial for GRK activation, the molecular details of this interaction remain unclear. Recent studies suggested an important role for the N- and C-termini and domains in the small lobe of the kinase domain in ...