The four adenosine receptors (ARs), A₁, A_2A, A_2B, and A₃, constitute a subfamily of G protein-coupled receptors (GPCRs) with exceptional foundations for structure-based ligand design. The vast amount of mutagenesis data, accumulated in the literature since the 1990s, has been recently supplemented with structural information, currently consisting of several inactive and active structures of the A_2A and inactive conformations of the A₁ ARs. We provide the first integrated view of the pharmacological, biochemical, and structural data available for this receptor family, by mapping onto the relevant crystal structures all site-directed mutagenesis data, curated and deposited at the GPCR database (available through http://www.gpcrdb.org). This analysis provides novel insights into ligand binding, allosteric modulation, and signaling of the AR family.

四个腺苷受体（ARs）A ₁，A _2A，A _2B和A ₃构成了G蛋白偶联受体（GPCR）的一个亚家族，具有基于结构的配体设计的特殊基础。自1990年代以来在文献中积累的大量诱变数据，最近已得到结构信息的补充，该信息目前由A _2A的几种非活性和活性结构以及A _1的非活性构象组成AR。通过将所有定点诱变数据映射到相关的晶体结构上，并整理并保存在GPCR数据库中（可通过http：// www获得），我们提供了可用于该受体家族的药理，生化和结构数据的第一个综合视图。 .gpcrdb.org）。这项分析为AR家族的配体结合，变构调节和信号传导提供了新颖的见解。