This review is provided in recognition of the extensive contributions of Dr. Robert J. Lefkowitz to the G protein-coupled receptor (GPCR) field and to celebrate his 75th birthday. Since one of the authors trained with Bob in the 80s, we provide a history of work done in the Lefkowitz lab during the 80s that focused on dissecting the mechanisms that regulate GPCR signaling, with a particular emphasis on the GPCR kinases (GRKs). In addition, we highlight structure/function characteristics of GRK interaction with GPCRs as well as a review of two recent reports that provide a molecular model for GRK-GPCR interaction. Finally, we offer our perspective on some future studies that we believe will drive this field.

本文是对Robert J. Lefkowitz博士对G蛋白偶联受体（GPCR）领域的广泛贡献并庆祝其75岁生日所做出的广泛贡献的认可。自从其中一位作者在80年代接受Bob的培训以来，我们提供了80年代Lefkowitz实验室中完成的工作历史，该工作专注于剖析调节GPCR信号传导的机制，尤其着重于GPCR激酶（GRKs）。此外，我们重点介绍了GRK与GPCR相互作用的结构/功能特征，以及对最近两个提供GRK-GPCR相互作用分子模型的报告的综述。最后，我们对未来的一些研究提出了自己的看法，我们相信这些研究将推动这一领域的发展。