A clinical drug library screen identifies astemizole as an antimalarial agent
A clinical drug library screen identifies astemizole as an antimalarial agent
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DOI：
10.1038/nchembio806
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发表时间：
2006-08-01
影响因子：
14.8
通讯作者：
Sullivan, David J., Jr.
中科院分区：
文献类型：
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作者：
Chong, Curtis R.;Chen, Xiaochun;Sullivan, David J., Jr.
新药开发的高成本和漫长的时间线是为被忽视的疾病创造疗法的主要障碍。为了加速药物发现，我们创建了一个包含2，687种现有药物的库，并筛选了人类疟疾寄生虫恶性疟原虫的抑制剂。抗组胺药阿司咪唑及其主要的人体代谢产物是氯喹敏感和多重耐药寄生虫的有前途的新抑制剂，它们在两种小鼠疟疾模型中显示出疗效。
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.