Shahbazi Fred, Grandi Victoria, Banerjee Abhinandan, Trant John F
Department of Chemistry and Biochemistry, University of Windsor, Windsor, ON N9B 3P4, Canada.
Department of Chemistry and Biochemistry, University of Windsor, Windsor, ON N9B 3P4, Canada.
iScience. 2020 Jul 24;23(7):101301. doi: 10.1016/j.isci.2020.101301. Epub 2020 Jun 20.
Like most modern molecular biology and natural product chemistry, understanding cannabinoid pharmacology centers around molecular interactions, in this case, between the cannabinoids and their putative targets, the G-protein coupled receptors (GPCRs) cannabinoid receptor 1 (CB) and cannabinoid receptor 2 (CB). Understanding the complex structure and interplay between the partners in this molecular dance is required to understand the mechanism of action of synthetic, endogenous, and phytochemical cannabinoids. This review, with 91 references, surveys our understanding of the structural biology of the cannabinoids and their target receptors including both a critical comparison of the extant crystal structures and the computationally derived homology models, as well as an in-depth discussion about the binding modes of the major cannabinoids. The aim is to assist in situating structural biochemists, synthetic chemists, and molecular biologists who are new to the field of cannabis research.
与大多数现代分子生物学和天然产物化学一样，理解大麻素药理学围绕分子相互作用展开，在这种情况下，是大麻素与其假定靶点——G蛋白偶联受体（GPCR）大麻素受体1（CB1）和大麻素受体2（CB2）之间的相互作用。要理解合成大麻素、内源性大麻素和植物化学大麻素的作用机制，就需要了解这场分子舞蹈中各参与者之间复杂的结构和相互作用。这篇综述有91篇参考文献，概述了我们对大麻素及其靶受体结构生物学的理解，包括对现有晶体结构和计算得出的同源模型的批判性比较，以及对主要大麻素结合模式的深入讨论。目的是帮助初涉大麻研究领域的结构生物化学家、合成化学家及分子生物学家了解相关情况。
