Review Article

Function and structure of bradykinin receptor 2 for drug discovery

Jin-kang Shen1, Hai-tao Zhang1,2
1 Hangzhou Institute of Innovative Medicine, Institute of Pharmacology and Toxicology, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
2 The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou 310009, China
Correspondence to: Hai-tao Zhang:,
DOI: 10.1038/s41401-022-00982-8
Received: 16 June 2022
Accepted: 11 August 2022
Advance online: 8 September 2022


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.
Keywords: type 2 bradykinin receptor; G protein-coupled receptor; functions; structures; drug discovery

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