MOLECULAR-CLONING OF THE CANINE ANGIOTENSIN-II RECEPTOR - AN AT1-LIKE RECEPTOR WITH REDUCED AFFINITY FOR DUP753

被引：31

作者：

BURNS, L

CLARK, KL

BRADLEY, J

ROBERTSON, MJ

CLARK, AJL

机构：

[1] UNIV LONDON ST BARTHOLOMEWS HOSP & MED COLL,DEPT CHEM ENDOCRINOL,LONDON EC1A 7BE,ENGLAND

[2] GLAXO GRP RES LTD,DEPT CARDIOVASC & RESP PHARMACOL,WARE SG12 0DP,HERTS,ENGLAND

来源：

FEBS LETTERS | 1994年 / 343卷 / 02期

关键词：

ANGIOTENSIN RECEPTOR; NONPEPTIDE ANTAGONISTS; CDNA CLONING; DOG AORTA; VASCULAR CONTRACTILITY; COS CELL;

D O I：

10.1016/0014-5793(94)80307-2

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：

Canine aortic strip studies revealed insensitivity of angiotensin II (AII)-induced aortic contraction to inhibition by the non-peptide antagonist DuP753 (pK(B) = 6.7 +/- 0.1). In order to determine the origin of this phenomenon we cloned the canine homologue of the AT(1) AII receptor. Expression of this cDNA in COS-7 cells indicated a low affinity of DuP753 for the cloned receptor (K-D = 92 nM). The predicted amino acid sequence is highly homologous to other mammalian AT(1) receptors; sequence comparisons suggest the pharmacological difference may be the result of a threonine residue in position 163 in the IVth transmembrane domain.

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页码：146 / 150

页数：5

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