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Trends Pharmacol Sci. 1996 Nov;17(11):416-21.

G protein-coupled receptors: heterologous regulation of homologous desensitization and its implications.

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  • 1Receptor Systems Unit, GlaxoWellcome Research and Development, Stevenage, UK.


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.

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