Dissecting signaling and functions of adhesion G protein-coupled receptors
Dissecting signaling and functions of adhesion G protein-coupled receptors
复制标题
DOI：
10.1111/j.1749-6632.2012.06820.x
复制
发表时间：
2012-01-01
期刊：
影响因子：
--
通讯作者：
Langenhan, Tobias
中科院分区：
文献类型：
--
作者：
Arac, Demet;Aust, Gabriela;Langenhan, Tobias
G蛋白偶联受体（GPCR）包括人类基因组中的受体的扩展超家族。粘附G类蛋白偶联受体（adhesion-GPCR）形成第二大类GPCR。尽管在各种器官系统中促进细胞和基质接触的丰度、大小、分子结构和功能，但粘附-GPCR是迄今为止了解最少的GPCR类别。粘附-GPCR具有独特的分子结构，具有含有各种粘附结构域的延伸的N-末端。此外，许多粘附-GPCR在含有GPCR蛋白水解位点（GPS）的保守GPCR自蛋白水解诱导（GAIN）结构域处被自蛋白水解切割成N-末端片段（NTF、NT、α-亚基）和C-末端片段（CTF、CT、β-亚基）。这两个特征将粘附-GPCR与其他GPCR类别区分开来。尽管近年来在免疫、神经科学、发育和肿瘤生物学等不同领域中对粘附-GPCR的积极研究已经加强，但粘附-GPCR的一般生物学和药理学性质并不为人所知，并且它们尚未用于生物医学目的。2012年9月6日至8日在维尔茨堡大学生理学研究所举行的“第六届国际粘附-GPCR研讨会”聚集了目前积极从事粘附-GPCR研究的大多数研究人员，包括来自欧洲、美国和亚洲实验室的科学家。会议的特点是对驱动粘附-GPCR信号转导的分子事件的新生机制理解，评估其功能的新模型，以及它们参与人类疾病的证据。
G protein-coupled receptors (GPCRs) comprise an expanded superfamily of receptors in the human genome. Adhesion class G protein-coupled receptors (adhesion-GPCRs) form the second largest class of GPCRs. Despite the abundance, size, molecular structure, and functions in facilitating cell and matrix contacts in a variety of organ systems, adhesion-GPCRs are by far the most poorly understood GPCR class. Adhesion-GPCRs possess a unique molecular structure, with extended N-termini containing various adhesion domains. In addition, many adhesion-GPCRs are autoproteolytically cleaved into an N-terminal fragment (NTF, NT, alpha-subunit) and C-terminal fragment (CTF, CT, beta-subunit) at a conserved GPCR autoproteolysis-inducing (GAIN) domain that contains a GPCR proteolysis site (GPS). These two features distinguish adhesion-GPCRs from other GPCR classes. Though active research on adhesion-GPCRs in diverse areas, such as immunity, neuroscience, and development and tumor biology has been intensified in the recent years, the general biological and pharmacological properties of adhesion-GPCRs are not well known, and they have not yet been used for biomedical purposes. The "6th International Adhesion-GPCR Workshop," held at the Institute of Physiology of the University of Wurzburg on September 6-8, 2012, assembled a majority of the investigators currently actively pursuing research on adhesion-GPCRs, including scientists from laboratories in Europe, the United States, and Asia. The meeting featured the nascent mechanistic understanding of the molecular events driving the signal transduction of adhesion-GPCRs, novel models to evaluate their functions, and evidence for their involvement in human disease.