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Dimerization of Chemokine Receptors and its Novel Roles in Drug Discovery

机译:趋化因子受体的二聚体及其在药物发现中的新作用

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G-protein-coupled receptors (GPCRs) comprise the largest family of integral membrane proteins and mediate most of the transmembrane signal transduction. Approximately 50 % of all marketed drugs target GPCRs, which makes this protein family the most important drug targets. Chemokine receptors belong to GPCRs, which were perceived as monomers decades ago. However, recently there are growing evidences indicating that most of GPCRs can form dimers or higher order oligomers. Some chemokine receptors are also found existing as homodimers or heterodimers. A large number of studies have suggested that homodimers or heterodimers may exhibit specific functions, which are different from their monomeric counterparts. Meanwhile, the appearance of dimers with new signaling properties gives new chance in the search for novel drug targets. In this review, we will mainly summarize the current knowledge of the dimerization of chemmokine receptors and its potential roles in drug discovery.
机译:G蛋白偶联受体(GPCR)包含最大的整合膜蛋白家族,并介导大多数跨膜信号转导。所有上市药物中约有50%靶向GPCR,这使得该蛋白家族成为最重要的药物靶向。趋化因子受体属于GPCR,几十年前被认为是单体。但是,最近有越来越多的证据表明大多数GPCR可以形成二聚体或更高阶的寡聚体。还发现一些趋化因子受体以同二聚体或异二聚体存在。大量研究表明,同二聚体或异二聚体可能表现出特定的功能,这与它们的单体对应物不同。同时,具有新信号特性的二聚体的出现为寻找新的药物靶标提供了新的机会。在这篇综述中,我们将主要总结趋化因子受体二聚体的当前知识及其在药物发现中的潜在作用。

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