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酪氨酸酶抑制剂的药物设计。

Drug design of tyrosinase inhibitors.

机构信息

Department of Pharmacy, G. d'Annunzio University of Chieti-Pescara, Chieti, Italy.

Department of Pharmacy, G. d'Annunzio University of Chieti-Pescara, Chieti, Italy.

出版信息

Enzymes. 2024;56:111-134. doi: 10.1016/bs.enz.2024.06.001. Epub 2024 Jun 25.

Abstract

This copper-containing enzyme catalyzes the rate-limiting step for the melanin skin pigment bioproduction. Tyrosinase inhibitors can be exploited as skin whitening agents and food preservatives, opening new scenarios in food, cosmetics, agriculture and medicine. Despite the availability of natural inhibitors (hydroquinone, α-arbutin, kojic acid, retinoids, azelaic acid, resveratrol, caftaric acid, valonea tannin, chrysosplenetin and phenylethyl resorcinol), several synthetic compounds were proposed to overcome side effects and to improve the efficacy of natural agents. This chapter will gather the recent advances about synthetic tyrosinase inhibitors from the MedChem perspective, providing new suggestions for the scaffold-based design of innovative compounds.

摘要

这种含铜酶催化黑色素皮肤色素生物生产的限速步骤。酪氨酸酶抑制剂可用作皮肤美白剂和食品防腐剂,为食品、化妆品、农业和医药开辟了新的应用场景。尽管存在天然抑制剂(对苯二酚、α-熊果苷、曲酸、类视黄醇、壬二酸、白藜芦醇、咖啡鞣酸、缬草酸单宁、朝鲜蓟素和苯乙基间苯二酚),但仍提出了几种合成化合物来克服副作用并提高天然化合物的功效。本章将从 MedChem 的角度汇集最新的合成酪氨酸酶抑制剂进展,为基于支架的创新化合物设计提供新的建议。

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