Department of Molecular Medicine, The Herbert Wertheim UF Scripps Institute for Biomedical Innovation and Technology, Jupiter, FL 33458, U.S.A.
The Skaggs Graduate School of Chemical and Biological Sciences at Scripps Research, La Jolla, CA 92037, U.S.A.
Biochem Soc Trans. 2023 Aug 31;51(4):1533-1543. doi: 10.1042/BST20221316.
The cannabinoid receptors CB1 and CB2 mediate a variety of physiological processes and continue to be explored as desirable drug targets. Both receptors are activated by the endogenous endocannabinoids and the psychoactive components of marijuana. Over the years, many efforts have been made to make selective ligands; however, the high degree of homology between cannabinoid receptor subtypes introduces challenges in studying either receptor in isolation. Recent advancements in structure biology have resulted in a surge of high-resolution structures, enriching our knowledge and understanding of receptor structure and function. In this review, of recent cannabinoid receptor structures, key features of the inactive and active state CB1 and CB2 are presented. These structures will provide additional insight into the modulation and signaling mechanism of cannabinoid receptors CB1 and CB2 and aid in the development of future therapeutics.
大麻素受体 CB1 和 CB2 介导多种生理过程，并且继续作为理想的药物靶点进行探索。这两种受体都被内源性大麻素和大麻的精神活性成分激活。多年来，人们做出了许多努力来制造选择性配体；然而，大麻素受体亚型之间的高度同源性给单独研究任何一种受体都带来了挑战。结构生物学的最新进展产生了大量高分辨率结构，丰富了我们对受体结构和功能的认识。在这篇综述中，介绍了最近的大麻素受体结构，包括 CB1 和 CB2 的无活性和活性状态的关键特征。这些结构将为大麻素受体 CB1 和 CB2 的调节和信号转导机制提供更多的见解，并有助于开发未来的治疗方法。
