GPCR expression in tissues and cells: Are the optimal receptors being used as drug targets?
GPCR expression in tissues and cells: Are the optimal receptors being used as drug targets?
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DOI：
10.1111/j.1476-5381.2011.01434.x
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发表时间：
2012-03-01
影响因子：
7.3
通讯作者：
Wilderman, A.
中科院分区：
文献类型：
--
作者：
Insel, P. A.;Snead, A.;Wilderman, A.
G蛋白偶联受体[GPCR，也称为7-跨膜（7-TM）受体]是人类和其他物种中最大的膜受体家族，此外，也是目前最多的药物靶点。在这篇文章中，我们回顾了定义GPCR表达的方法和表明单个细胞表达>100种不同GPCR的数据。这些受体定量表达的研究结果使我们得出结论，最佳GPCR目前可能不用作治疗靶点。我们认为，对单个细胞中GPCR表达的研究可能会揭示有关细胞生理学和治疗方法的新见解。因此，定义和表征最高表达的GPCR的发现在鉴定针对广泛的临床疾病的新药靶点和新疗法方面具有重要的潜力。
G-protein-coupled receptors [GPCRs, also known as 7-transmembrane (7-TM) receptors] comprise the largest family of membrane receptors in humans and other species and, in addition, represent the greatest number of current drug targets. In this article, we review methods to define GPCR expression and data indicating that individual cells express >100 different GPCRs. Results from studies that have quantified expression of these receptors lead us to conclude that the optimal GPCRs may not be currently used as therapeutic targets. We propose that studies of GPCR expression in individual cells will likely reveal new insights regarding cellular physiology and therapeutic approaches. Findings that define and characterize the most highly expressed GPCRs thus have important potential in terms of identifying new drug targets and novel therapies directed at a wide range of clinical disorders.