期刊
ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 58
卷 58, 期 -, 页码 429-449出版社
ANNUAL REVIEWS
DOI: 10.1146/annurev-pharmtox-010617-052933
关键词
therapeutic; agonist; antagonist; ligand; antibody; pharmaceutical
资金
- NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE [R21NS094136] Funding Source: NIH RePORTER
- NINDS NIH HHS [R21 NS094136, R01 NS072394] Funding Source: Medline
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.
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