Chuang T T, Iacovelli L, Sallese M, De Blasi A
Receptor Systems Unit, GlaxoWellcome Research and Development, Stevenage, UK.
Trends Pharmacol Sci. 1996 Nov;17(11):416-21. doi: 10.1016/s0165-6147(96)10048-1.
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.
针对G蛋白偶联受体，已明确了两种快速脱敏模式：同源脱敏，主要涉及G蛋白偶联受体激酶和抑制蛋白；异源脱敏，主要涉及蛋白激酶A（PKA）和蛋白激酶C（PKC）。在这篇综述中，庄祖申及其同事讨论了相关证据，表明PKA和PKC可以改变G蛋白偶联受体激酶/抑制蛋白同源脱敏机制的功能状态，在信号转导中提供了一种新的相互作用水平。对G蛋白偶联受体激酶和抑制蛋白调节的研究证实，该机制的功能状态可能对细胞反应性产生重要影响，并且可能代表治疗策略的新靶点。
