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Review Article

异源三聚体G蛋白α-亚基-结构，肽衍生抑制剂和机制

卷 29, 期 42, 2022

发表于: 01 April, 2022

页: [6359 - 6378] 页: 20

弟呕挨: 10.2174/0929867329666220308112424

价格: $65

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摘要

G蛋白偶联受体是人体内最大的蛋白质家族，是最重要的一类药物靶标。它们接收细胞外信号并将其转导到细胞质中。鸟嘌呤核苷酸结合Gα蛋白是GPCR诱导细胞内效应的主要中继。超过 800 种不同的 GPCR 与属于 4 个家族（Gαi、Gαs、Gαq 和 Gα12/13）的 16 种 Gα 蛋白相互作用。直接抑制Gα蛋白亚基而不是调节GPCR亚型已被提出作为治疗复杂疾病（包括炎症和癌症）的新策略。本文介绍了G蛋白的结构和功能，并描述了肽和肽衍生Gα蛋白抑制剂的研究进展。它们已成为不可或缺的药理工具，其中一些显示出作为未来药物的巨大潜力。

关键词: 环肽，FR900359，异源三聚体G蛋白，Gα蛋白，G蛋白偶联受体，肽，YM-254890，抑制剂。

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