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Gonadotropin-releasing hormone antagonists.
Current Opinion in Pharmacology ( IF 4 ) Pub Date : 2003-12-03 , DOI: 10.1016/j.coph.2003.06.009
Karen L Herbst 1
Affiliation  

Hypothalamic gonadotropin-releasing hormone (GnRH) is a decapeptide that stimulates pituitary synthesis and secretion of gonadotropins and, therefore, gonadal hormones. GnRH antagonists, of which thousands have been formulated, inhibit the hormone from binding to its receptor, inducing a pharmacological hypophysectomy. Peptide derivations of GnRH and non-peptide compounds are both in clinical trials or approved for assisted reproduction. As these compounds reach the market, the use of antagonists might expand to treatment of other hormonally dependent diseases, hormonal male contraception and growth inhibition of extra-pituitary cancer cells expressing GnRH receptors.

中文翻译:

促性腺激素释放激素拮抗剂。

下丘脑促性腺激素释放激素(GnRH)是一种十肽,可刺激垂体合成和促性腺激素的分泌,从而刺激性腺激素。已经配制了成千上万种GnRH拮抗剂,抑制该激素与其受体的结合,从而导致药理性垂体切除术。GnRH和非肽化合物的肽衍生物都在临床试验中或已批准用于辅助生殖。随着这些化合物投放市场,拮抗剂的使用可能会扩展到其他荷尔蒙依赖性疾病的治疗,荷尔蒙男性避孕以及表达GnRH受体的垂体外癌细胞的生长抑制。
更新日期:2019-11-01
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