Article
CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs.
Molecular microbiology - 1 Aug 2016
Ng Caroline L, Siciliano Giulia, Lee Marcus C S, de Almeida Mariana J, Corey Victoria C, Bopp Selina E, Bertuccini Lucia, Wittlin Sergio, Kasdin Rachel G, Le Bihan Amélie, Clozel Martine, Winzeler Elizabeth A, Alano Pietro, Fidock David A
Abstract excerpt
Emerging resistance to first-line antimalarial combination therapies threatens malaria treatment and the global elimination campaign. Improved therapeutic strategies are required to protect existing drugs and enhance treatment efficacy. We report that the piperazine-containing compound ACT-451840 exhibits single-digit nanomolar inhibition of the Plasmodium falciparum asexual blood stages and transmissible...
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