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皮肤美白剂:酪氨酸酶抑制剂的药物化学视角

Skin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors.

作者信息

Pillaiyar Thanigaimalai, Manickam Manoj, Namasivayam Vigneshwaran

机构信息

a PharmaCenter Bonn , Pharmaceutical Institute, Pharmaceutical Chemistry I, University of Bonn , Bonn , Germany.

b College of Pharmacy and Institute of Drug Research and Development , Chungnam National University , Daejeon , Korea.

出版信息

J Enzyme Inhib Med Chem. 2017 Dec;32(1):403-425. doi: 10.1080/14756366.2016.1256882.

Abstract

Melanogenesis is a process to synthesize melanin, which is a primary responsible for the pigmentation of human skin, eye and hair. Although numerous enzymatic catalyzed and chemical reactions are involved in melanogenesis process, the enzymes such as tyrosinase and tyrosinase-related protein-1 (TRP-1) and TRP-2 played a major role in melanin synthesis. Specifically, tyrosinase is a key enzyme, which catalyzes a rate-limiting step of the melanin synthesis, and the downregulation of tyrosinase is the most prominent approach for the development of melanogenesis inhibitors. Therefore, numerous inhibitors that target tyrosinase have been developed in recent years. The review focuses on the recent discovery of tyrosinase inhibitors that are directly involved in the inhibition of tyrosinase catalytic activity and functionality from all sources, including laboratory synthetic methods, natural products, virtual screening and structure-based molecular docking studies.

摘要

黑色素生成是一个合成黑色素的过程,黑色素是人类皮肤、眼睛和头发色素沉着的主要原因。尽管黑色素生成过程涉及众多酶催化和化学反应,但诸如酪氨酸酶、酪氨酸酶相关蛋白-1(TRP-1)和TRP-2等酶在黑色素合成中起主要作用。具体而言,酪氨酸酶是一种关键酶,它催化黑色素合成的限速步骤,而酪氨酸酶的下调是开发黑色素生成抑制剂的最突出方法。因此,近年来已开发出许多靶向酪氨酸酶的抑制剂。本综述重点关注近年来直接参与抑制酪氨酸酶催化活性和功能的酪氨酸酶抑制剂的发现,这些抑制剂来源广泛,包括实验室合成方法、天然产物、虚拟筛选和基于结构的分子对接研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c057/6010116/483042ee2a45/IENZ_A_1256882_F0001_C.jpg

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