G protein-coupled receptors: heterologous regulation of homologous desensitization and its implications.
Two patterns of rapid desensitization have been characterized for G protein-coupled receptors: homologous desensitization, which mainly involves G protein-coupled receptor kinases and arrestins, and heterologous desensitization, which mainly involves protein kinases A (PKA) and C (PKC). In this review, Tsu Tshen Chuang and colleagues discuss evidence to show that PKA and PKC can modify the functional state of the G protein-coupled receptor kinases/arrestin homologous desensitization machinery, providing a novel level of cross-talk in signal transduction. Studies on regulation of G protein-coupled receptor kinases and arrestins confirm that the functional state of this machinery may have important consequences for cellular responsiveness and may represent new targets for therapeutic strategies.
Chuang
T T
TT
Receptor Systems Unit, GlaxoWellcome Research and Development, Stevenage, UK.
Iacovelli
L
L
Sallese
M
M
De Blasi
A
A
D000818:Animals; D019204:GTP-Binding Proteins / Q000378:metabolism*; D006801:Humans; D010766:Phosphorylation; D011956:Receptors, Cell Surface / Q000378:metabolism*; D012680:Sensitivity and Specificity
D011956:Receptors, Cell Surface; D019204:GTP-Binding Proteins