当前位置: X-MOL 学术Mol. Cell. Endocrinol. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Molecular chaperones and G protein-coupled receptor maturation and pharmacology.
Molecular and Cellular Endocrinology ( IF 4.1 ) Pub Date : 2020-05-07 , DOI: 10.1016/j.mce.2020.110862
Ya-Xiong Tao 1
Affiliation  

G protein-coupled receptors (GPCRs) are highly conserved versatile signaling molecules located at the plasma membrane that respond to diverse extracellular signals. They regulate almost all physiological processes in the vertebrates. About 35% of current drugs target these receptors. Mutations in these genes have been identified as causes of numerous diseases. The seven transmembrane domain structure of GPCRs implies that the folding of these transmembrane proteins is extremely complicated and difficult. Indeed, many wild type GPCRs are not folded optimally. The most common defect in genetic diseases caused by GPCR mutations is misfolding and failure to reach the plasma membrane where it functions. General molecular chaperones aid the folding of all proteins, including GPCRs, by preventing aggregation, promoting folding and disaggregating small aggregates. Some GPCRs need additional receptor-specific chaperones to assist their folding. Many of these receptor-specific chaperones interact with additional receptors and alter receptor pharmacology, expanding the understanding of these chaperone proteins.

中文翻译:

分子伴侣和G蛋白偶联受体的成熟和药理作用。

G蛋白偶联受体(GPCR)是位于质膜上的高度保守的通用信号分子,可响应多种细胞外信号。它们调节脊椎动物中几乎所有的生理过程。目前约35%的药物靶向这些受体。这些基因的突变已被确定为多种疾病的原因。GPCR的七个跨膜结构域结构意味着这些跨膜蛋白的折叠极其复杂和困难。实际上,许多野生型GPCR并不是最优折叠的。由GPCR突变引起的遗传疾病中最常见的缺陷是折叠错误和无法到达其起作用的质膜。通用分子伴侣可以防止聚集,从而有助于折叠所有蛋白质(包括GPCR),促进折叠和分解小骨料。一些GPCR需要其他受体特异性伴侣来协助其折叠。这些受体特异性伴侣蛋白中的许多与其他受体相互作用并改变受体药理学,从而扩展了对这些伴侣蛋白的理解。
更新日期:2020-05-07
down
wechat
bug