Cholesterol in Class C GPCRs: Role, Relevance, and Localization.
Cholesterol in Class C GPCRs: Role, Relevance, and Localization.
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DOI：
10.3390/membranes13030301
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发表时间：
2023-03-03
期刊：
影响因子：
4.2
通讯作者：
Moradi M
中科院分区：
文献类型：
--
作者：
Isu UH;Badiee SA;Khodadadi E;Moradi M
G蛋白偶联受体（GPCR）是细胞表面受体的最大超家族之一，是在几乎每个器官系统中发挥关键作用的七螺旋整合膜蛋白。G蛋白偶联受体在富含胆固醇的膜中起作用，GPCR跨膜结构域附近的胆固醇水平不平衡影响许多GPCR的结构和/或功能，这种现象与几种疾病有关。胆固醇的这些作用可能通过改变脂质环境的机械性质而导致间接变化，或通过结合蛋白质上的特定位点而导致直接变化。有许多关于胆固醇如何调节A类GPCR的研究和综述;然而，这一研究领域尚未探索C类GPCR，其特征在于大的细胞外区域并且通常形成组成型二聚体。本文综述了C类GPCR识别胆固醇所涉及的特定相互作用位点、功能和结构动力学。我们总结了最近的数据，从一些典型的家庭成员来解释膜胆固醇对C类GPCR的结构特征和功能的影响，并推测其相应的治疗潜力。
G-protein coupled receptors (GPCRs), one of the largest superfamilies of cell-surface receptors, are heptahelical integral membrane proteins that play critical roles in virtually every organ system. G-protein-coupled receptors operate in membranes rich in cholesterol, with an imbalance in cholesterol level within the vicinity of GPCR transmembrane domains affecting the structure and/or function of many GPCRs, a phenomenon that has been linked to several diseases. These effects of cholesterol could result in indirect changes by altering the mechanical properties of the lipid environment or direct changes by binding to specific sites on the protein. There are a number of studies and reviews on how cholesterol modulates class A GPCRs; however, this area of study is yet to be explored for class C GPCRs, which are characterized by a large extracellular region and often form constitutive dimers. This review highlights specific sites of interaction, functions, and structural dynamics involved in the cholesterol recognition of the class C GPCRs. We summarize recent data from some typical family members to explain the effects of membrane cholesterol on the structural features and functions of class C GPCRs and speculate on their corresponding therapeutic potential.
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