由美国国立癌症研究所（NCI）开发治疗项目推动的基于天然产物的抗HIV药物研发。

Natural product-based anti-HIV drug discovery and development facilitated by the NCI developmental therapeutics program.

作者信息

Yang S S, Cragg G M, Newman D J, Bader J P

机构信息

Developmental Therapeutics Program, National Cancer Institute, Bethesda, Maryland 20892, USA.

出版信息

J Nat Prod. 2001 Feb;64(2):265-77. doi: 10.1021/np0003995.

DOI:10.1021/np0003995

PMID:11430019

Abstract

During the decade 1987-1996, the Developmental Therapeutics Program (DTP) of the National Cancer Institute (NCI) provided infrastructure support for both intramural and extramural anti-HIV (human immunodeficiency virus) drug discovery research and development. This retrospective review describes some of the anti-HIV lead discovery and development that took place under DTP auspices or which was substantially facilitated by resources made available through the DTP. Examples highlighted include leads identified through the initial screening of pure natural product derived compounds and those derived from bioassay-guided fractionation of crude natural product extracts, and these are classified according to the mechanism of action targeting the critical steps within the replication cycle of HIV.

摘要

在1987年至1996年的十年间，美国国立癌症研究所（NCI）的发展治疗学项目（DTP）为内部和外部的抗HIV（人类免疫缺陷病毒）药物发现研究与开发提供了基础设施支持。本回顾性综述描述了一些在DTP支持下进行的抗HIV先导化合物的发现与开发，或者是通过DTP提供的资源而得到极大推动的相关研究。重点突出的例子包括通过对纯天然产物衍生化合物的初步筛选以及对天然产物粗提物进行生物测定导向分馏所确定的先导化合物，并且这些先导化合物根据针对HIV复制周期关键步骤的作用机制进行分类。