Robert J. Lefkowitz

TL;DR: Results indicate that tyrosine residues have a function in the conformational stability of α2-adrenoceptors and may be directly involved with ligand binding to the receptor.

TL;DR: The role of the autonomic nervous system in the pathophysiology of heart failure has been studied for decades, but within the past few years have adrenergic receptors and their alterations occupied center stage.

TL;DR: This work has developed a mixed culture system to study the mechanism of GPCR-mediated HB-EGF shedding in COS-7 cells, and demonstrates that EGFR-dependent activation of the ERK cascade after a2AAR stimulation requires Gbg subunits upstream and dynamin-dependent endocytosis downstream of HBEGF Shedding and EGFR activation, whereas Src kinase activity is required both for the release of HB-egF and for HB- EGF

TL;DR: Following photolysis up to 90% of the ..cap alpha../sub 2/-adrenoceptors could be irreversibly labeled with (/sup 3/H)SKF 102229.

TL;DR: Methodological criteria crucial for valid comparison of receptor occupancy and adenylate cyclase activity are delineated and the possible molecular mechanisms of receptor-cyclase coupling which might give rise to the coupling curves observed are discussed.