Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that regulates the cardiovascular system as a vasodepressor. Dysfunction of B2R is also closely related to cancers and hereditary angioedema (HAE). Although several B2R agonists and antagonists have been developed, icatibant is the only B2R antagonist clinically used for treating HAE. The recently determined structures of B2R have provided molecular insights into the functions and regulation of B2R, which shed light on structure-based drug design for the treatment of B2R-related diseases. In this review, we summarize the structure and function of B2R in relation to drug discovery and discuss future research directions to elucidate the remaining unknown functions of B2R dimerization.

2 型缓激肽受体 (B2R) 是一种重要的 G 蛋白偶联受体 (GPCR)，可作为血管抑制剂调节心血管系统。 B2R功能障碍还与癌症和遗传性血管性水肿（HAE）密切相关。尽管已经开发了几种B2R激动剂和拮抗剂，但艾替班特是临床上唯一用于治疗HAE的B2R拮抗剂。最近确定的 B2R 结构为 B2R 的功能和调节提供了分子见解，这为治疗 B2R 相关疾病的基于结构的药物设计提供了线索。在这篇综述中，我们总结了 B2R 与药物发现相关的结构和功能，并讨论了未来的研究方向，以阐明 B2R 二聚化剩余的未知功能。