A clinical drug library screen identifies astemizole as an antimalarial agent

被引：221

作者：

Chong, Curtis R.

Chen, Xiaochun

Shi, Lirong

O Liu, Jun

Sullivan, David J., Jr. ^{[1
]}

机构：

[1] Johns Hopkins Univ, Sch Med, Johns Hopkins Clin Compound Screening Initiat, Baltimore, MD 21205 USA

[2] Johns Hopkins Univ, Sch Med, Dept Pharmacol & Mol Sci, Baltimore, MD 21205 USA

[3] Johns Hopkins Univ, Sch Med, Med Sci Training Program, Baltimore, MD 21205 USA

[4] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Malaria Res Inst, W Harry Feinstone Dept Mol Microbiol & Immunol, Baltimore, MD 21205 USA

[5] Johns Hopkins Univ, Sch Med, Dept Neurosci, Baltimore, MD 21205 USA

来源：

NATURE CHEMICAL BIOLOGY | 2006年 / 2卷 / 08期

关键词：

D O I：

10.1038/nchembio806

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The high cost and protracted time line of new drug discovery are major roadblocks to creating therapies for neglected diseases. To accelerate drug discovery we created a library of 2,687 existing drugs and screened for inhibitors of the human malaria parasite Plasmodium falciparum. The antihistamine astemizole and its principal human metabolite are promising new inhibitors of chloroquine-sensitive and multidrug-resistant parasites, and they show efficacy in two mouse models of malaria.

引用

页码：415 / 416

页数：2

共 10 条

[1] Toward a pharmacophore for drugs inducing the long QT syndrome:: Insights from a CoMFA study of HERG K+ channel blockers [J].