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

Two patterns of rapid desensitization have been characterized for G protein-coupled receptn:d: homologous desensitizeton, which mainly involves G protein-coupled receptor kineses and arrestins, and heterologous desensitization, which mainly involves protein kinases A IPKA) and C (PKC). In this review, Tsu T&en 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 far cellular responsiveness and may represent new targets for therapeutic strategies.