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流感神经氨酸酶抑制剂的药效团模型——系统评价

Pharmacophore model of influenza neuraminidase inhibitors--a systematic review.

作者信息

Gong Jian-Zhi, Liu Yu, Xu Wen-Fang

机构信息

Institute of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong, PR China.

出版信息

Pharmazie. 2009 Oct;64(10):627-32.

Abstract

Recently, the worldwide spread of A/H5N1 avian influenza with high virulence has highlighted the potential threat of a human influenza pandemic. The viral surface glycoprotein, neuraminidase (NA), has been found to be a potential target to control influenza virus. With an understanding of the enzyme mechanism, the X-ray crystallographic structures of NA and its substrate or inhibitors, and progress in computational chemistry, the information about NA binding sites and pharmacophore models is derived from existing inhibitors and will serve as design guidelines of more potent agents against NA. This article gives a systematic review of the recent advances in this area.

摘要

最近,高致病性A/H5N1禽流感在全球范围内的传播凸显了人流感大流行的潜在威胁。病毒表面糖蛋白神经氨酸酶(NA)已被发现是控制流感病毒的一个潜在靶点。随着对该酶作用机制、NA及其底物或抑制剂的X射线晶体结构的了解,以及计算化学的进展,有关NA结合位点和药效团模型的信息来自现有的抑制剂,并将作为设计更有效抗NA药物的指导原则。本文对该领域的最新进展进行了系统综述。

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