A clinical drug library screen identifies astemizole as an antimalarial agent
CR Chong, X Chen, L Shi, JO Liu… - Nature chemical …, 2006 - nature.com
CR Chong, X Chen, L Shi, JO Liu, DJ Sullivan Jr
Nature chemical biology, 2006•nature.comThe 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.
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.
Abstract
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.
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