The adhesion G protein-coupled receptors (aGPCRs) are an evolutionarily ancient family of receptors that play key roles in many different physiological processes. These receptors are notable for their exceptionally long ectodomains, which span several hundred to several thousand amino acids and contain various adhesion-related domains, as well as a GPCR autoproteolysis-inducing (GAIN) domain. The GAIN domain is conserved throughout almost the entire family and undergoes autoproteolysis to cleave the receptors into two noncovalently-associated protomers. Recent studies have revealed that the signaling activity of aGPCRs is largely determined by changes in the interactions among these protomers. We review recent advances in understanding aGPCR activation mechanisms and discuss the physiological roles and pharmacological properties of aGPCRs, with an eye toward the potential utility of these receptors as drug targets.

中文翻译：

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粘附G蛋白偶联受体作为药物靶标。

粘附G蛋白偶联受体（aGPCR）是一个古老的受体家族，在许多不同的生理过程中起着关键作用。这些受体以其异常长的胞外域而著名，该胞外域跨越数百至数千个氨基酸，并包含各种粘附相关的域以及GPCR自蛋白水解诱导（GAIN）域。GAIN结构域在几乎整个家族中都是保守的，并经过自身蛋白水解以将受体裂解为两个非共价结合的启动子。最近的研究表明，aGPCR的信号传导活性很大程度上取决于这些启动子之间相互作用的变化。我们回顾了了解aGPCR激活机制的最新进展，并讨论了aGPCR的生理作用和药理特性，