Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin
Two aromatic residues regulate the response of the human oxytocin receptor to the partial agonist arginine vasopressin
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DOI：
10.1016/s0014-5793(96)01135-0
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发表时间：
1996-11-18
期刊：
影响因子：
3.5
通讯作者：
Barberis, C
中科院分区：
文献类型：
--
作者：
Chini, B;Mouillac, B;Barberis, C
我们研究了精氨酸-加压素（AVP）/催产素（OT）受体系统中激动剂的调节机制。在本文中，我们提供了证据，证明AVP是加压素受体的完全激动剂，对催产素受体起部分激动剂的作用，我们还发现，当催产素受体的两个芳香族残基被存在于催产素受体中相同位置的残基取代时，AVP成为完全激动剂。加压素受体亚型，我们的结果表明，这两个残基调节催产素受体的反应，部分激动剂AVP。
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.