Honey, we need to talk about the membrane progestin receptors
Honey, we need to talk about the membrane progestin receptors
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DOI：
10.1016/j.steroids.2007.12.004
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发表时间：
2008-10-01
期刊：
影响因子：
2.7
通讯作者：
Gellersen, Birgit
中科院分区：
文献类型：
--
作者：
Fernandes, Maria Sofia;Brosens, Jan J.;Gellersen, Birgit
最近发现的三个密切相关的细胞表面受体，结合孕酮和介导的各种细胞质信号级联反应的行动已被宣布为一个重大突破。原因是显而易见的。孕激素是所有主要生殖事件的重要调节剂，孕激素和抗孕激素广泛用于治疗许多不同的妇科和产科疾病。据报道，新的膜促甲状腺激素受体（mPR α、β、γ）类似于G蛋白偶联受体并起G蛋白偶联受体的作用，因此是有希望的药物靶标。然而，我们的研究未能证实mPR在细胞表面表达，它们介导快速孕酮信号传导事件，甚至它们是真正的孕酮结合部分。虽然这些令人震惊的相反结果的原因尚不清楚，但对现有数据的批判性审查可能有助于揭示有争议的mPR。是时候谈谈了(C)2007年爱思唯尔公司All rights reserved.
The recent discovery of three closely related cell surface receptors that bind to progesterone and mediate its actions on various cytoplasmic signalling cascades has been heralded as a major break-through. The reason for this is all too obvious. Progesterone is an essential regulator of all major reproductive events and progestins and antiprogestins are widely used in the treatment of many different gynaecological and obstetrical disorders. The novel membrane progestin receptors (mPR alpha, beta, gamma) reportedly resemble and function as G-protein-coupled receptors and therefore are promising pharmaceutical targets. However, our studies failed to corroborate that mPRs are expressed on the cell surface, that they mediate rapid progesterone signalling events, and even that they are bona fide progestin binding moieties. While the reason for these startling opposing results remains unclear, a critical review of existing data may help to shed some light onto the controversial mPRs. Time has come to talk. (C) 2007 Elsevier Inc. All rights reserved.