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瘦素受体调节剂的治疗潜力。

Therapeutic potential of leptin receptor modulators.

机构信息

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, CS, Italy.

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Edificio Polifunzionale, 87036 Arcavacata di Rende, CS, Italy.

出版信息

Eur J Med Chem. 2014 May 6;78:97-105. doi: 10.1016/j.ejmech.2014.03.048. Epub 2014 Mar 16.

Abstract

Leptin, a pleiotropic molecule mainly produced by adipose tissue, was first discovered as a hormone controlling body weight and energy expenditure. In addition, leptin can modulate several processes in peripheral tissues such as immune response, fertility, hematopoiesis and carcinogenesis. The development of molecules that block or stimulate leptin receptor may therefore serve as a potent tool for studying the role of leptin in mammalian physiology and pathology, but it also may open new possibilities for therapy. This article presents an overview of current knowledge on leptin receptor modulators focusing on leptin mutein, leptin peptide modulators as well as small molecules with heterocyclic structure.

摘要

瘦素是一种主要由脂肪组织产生的多功能分子,最初被发现是一种控制体重和能量消耗的激素。此外,瘦素还可以调节外周组织中的多种过程,如免疫反应、生育能力、造血和癌变。因此,开发阻断或刺激瘦素受体的分子可能成为研究瘦素在哺乳动物生理学和病理学中作用的有力工具,但也可能为治疗开辟新的可能性。本文综述了目前关于瘦素受体调节剂的知识,重点介绍了瘦素突变体、瘦素肽调节剂以及具有杂环结构的小分子。

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