CLONING AND PHARMACOLOGICAL CHARACTERIZATION OF A HUMAN BRADYKININ (BK-2) RECEPTOR

被引：451

作者：

HESS, JF ^{[1
]}

BORKOWSKI, JA ^{[1
]}

YOUNG, GS ^{[1
]}

STRADER, CD ^{[1
]}

RANSOM, RW ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,DEPT NEW LEAD PHARMACOL,W POINT,PA 19486

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1992年 / 184卷 / 01期

关键词：

D O I：

10.1016/0006-291X(92)91187-U

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A human BK-2 bradykinin receptor was cloned from the lung fibroblast cell line CCD-16Lu. The cDNA clone encodes a 364 amino acid protein that has the characteristics of a seven transmembrane domain G-protein coupled receptor. The predicted amino acid sequence of the human BK-2 receptor is 81% identical to the smooth muscle rat BK-2 receptor (1). Transfection of the human BK-2 receptor cDNA into COS-7 cells results in the expression of high levels of specific BK binding sites. Saturation binding analysis indicates that the human BK-2 receptor expressed in COS-7 cells binds BK with a KD of 0.13 nM. Pharmacological characterization of the expressed BK receptor is consistent with the cDNA encoding a receptor of the BK-2 subtype. The BK-2 receptor antagonist Hoe 140 (2), D-Arg0[Hyp3, Thi5, D-Tic7, Oic8]BK has a high affinity (IC50=65 pM) for the cloned human receptor. The tissue distribution of the human BK-2 receptor was analyzed by competitive PCR with human tissue cDNA and is similar to that determined for the BK-2 receptor in the rat. © 1992.

引用

页码：260 / 268

页数：9