Monk Kelly R, Hamann Jörg, Langenhan Tobias, Nijmeijer Saskia, Schöneberg Torsten, Liebscher Ines
Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.).
Department of Developmental Biology, Washington University School of Medicine, St. Louis, Missouri (K.R.M.); Department of Experimental Immunology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands (J.H.); Department of Neurophysiology, Institute of Physiology, University of Würzburg, Würzburg, Germany (T.L.); Department of Medicinal Chemistry/Amsterdam Institute for Molecules, Medicines and Systems, VU University, Amsterdam, The Netherlands (S.N.); and Institute of Biochemistry, Molecular Biochemistry, Medical Faculty, University of Leipzig, Leipzig, Germany (T.S., I.L.)
Mol Pharmacol. 2015 Sep;88(3):617-23. doi: 10.1124/mol.115.098749. Epub 2015 May 8.
The adhesion family of G protein-coupled receptors (aGPCRs) comprises 33 members in humans. aGPCRs are characterized by their enormous size and complex modular structures. While the physiologic importance of many aGPCRs has been clearly demonstrated in recent years, the underlying molecular functions have only recently begun to be elucidated. In this minireview, we present an overview of our current knowledge on aGPCR activation and signal transduction with a focus on the latest findings regarding the interplay between ligand binding, mechanical force, and the tethered agonistic Stachel sequence, as well as implications on translational approaches that may derive from understanding aGPCR pharmacology.
G蛋白偶联受体粘附家族（aGPCRs）在人类中包含33个成员。aGPCRs的特点是其巨大的规模和复杂的模块化结构。虽然近年来许多aGPCRs的生理重要性已得到明确证明，但其潜在的分子功能直到最近才开始被阐明。在这篇小型综述中，我们概述了目前关于aGPCR激活和信号转导的知识，重点关注配体结合、机械力和拴系激动性Stachel序列之间相互作用的最新发现，以及对可能源于理解aGPCR药理学的转化方法的影响。
