Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin

被引:101
作者
Chini, B
Mouillac, B
Balestre, MN
TrumppKallmeyer, S
Hoflack, J
Hibert, M
Andriolo, M
Pupier, S
Jard, S
Barberis, C
机构
[1] CCIPE,INSERM,U401,F-34094 MONTPELLIER,FRANCE
[2] MARION MERRELL DOW RES INST,F-67009 STRASBOURG,FRANCE
关键词
oxytocin receptor; vasopressin; G protein coupled receptor; partial agonism; mutagenesis;
D O I
10.1016/S0014-5793(96)01135-0
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
We investigated the mechanisms that regulate the efficacy of agonists in the arginine-vasopressin (AVP)/oxytocin (OT) receptor system, In this paper, we present evidence that AVP, a full agonist of the vasopressin receptors, acts as a partial agonist on the oxytocin receptor, We also found that AVP becomes a full agonist when two aromatic residues of the oxytocin receptor are replaced by the residues present at equivalent positions in the vasopressin receptor subtypes, Our results indicate that these two residues modulate the response of the oxytocin receptor to the partial agonist AVP.
引用
收藏
页码:201 / 206
页数:6
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