Tt. Chuang et al., G-PROTEIN-COUPLED RECEPTORS - HETEROLOGOUS REGULATION OF HOMOLOGOUS DESENSITIZATION AND ITS IMPLICATIONS, Trends in pharmacological sciences, 17(11), 1996, pp. 416-421
Two patterns of rapid desensitization have been characterized for G pr
otein-coupled receptors: homologous desensitizaton, which mainly invol
ves 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 evidenc
e to show that PKA and PKC can modify the functional state of the G pr
otein-coupled receptor kinases/arrestin homologous desensitization mac
hinery, providing a navel level of cross-talk in signal transduction.
Studies on regulation of G protein-coupled receptor kinases and arrest
ins confirm that the functional state of this machinery may have impor
tant consequences for cellular responsiveness and may represent new ta
rgets for therapeutic strategies.