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[α-黑素细胞刺激素。从实验室到临床]

[Alpha-melanocyte-stimulating hormone. From bench to bedside].

作者信息

Böhm M, Luger T A

机构信息

Klinik und Poliklinik für Hautkrankheiten-Allgemeine Dermatologie und Venerologie, Universitätsklinikum Münster, Von-Esmarch-Str. 58, 48149, Münster, Germany.

出版信息

Hautarzt. 2010 Jun;61(6):497-504. doi: 10.1007/s00105-009-1891-1.

Abstract

Alpha-melanocyte-stimulating hormone (alpha-MSH) is a tridecapeptide that is produced by the skin itself from the precursor proopiomelanocortin. It crucially mediates ultraviolet light-induced tanning after binding to melanocortin-1 receptors (MC-1R) expressed on the surface of epidermal melanocytes. The potent pigment-inducing and also cytoprotective actions of alpha-MSH are the rationale for the performance of first phase II clinical trials with Nle4-D-Phe7-alpha-MSH (NDP-alpha-MSH), a subcutaneously administered synthetic and superpotent alpha-MSH analogue, in patients with photodermatoses such as erythropoietic protoporphyria. Since alpha-MSH has shown promising anti-inflammatory and antifibrotic properties in numerous preclinical studies, it will be most interesting to evaluate these effects in further clinical pilot studies with NDP-alpha-MSH. In addition to alpha-MSH analogues, truncated tripeptides such as KDPT which do not bind to MC-1R but have sustained anti-inflammatory properties are currently emerging as another novel therapeutic strategy in dermatology.

摘要

α-黑素细胞刺激素(α-MSH)是一种十三肽,由皮肤自身从前体阿黑皮素原产生。它在与表皮黑素细胞表面表达的黑素皮质素-1受体(MC-1R)结合后,对紫外线诱导的晒黑起着关键的介导作用。α-MSH强大的色素诱导作用以及细胞保护作用,是在患有光皮肤病(如红细胞生成性原卟啉症)的患者中开展Nle4-D-Phe7-α-MSH(NDP-α-MSH,一种皮下注射的合成且强效的α-MSH类似物)的一期临床试验的依据。由于α-MSH在众多临床前研究中已显示出有前景的抗炎和抗纤维化特性,在进一步使用NDP-α-MSH进行的临床前期研究中评估这些作用将非常有趣。除了α-MSH类似物外,截短的三肽如KDPT,它们不与MC-1R结合但具有持续的抗炎特性,目前正作为皮肤病学中的另一种新型治疗策略出现。

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