MMV008138 是一种物种选择性抗疟剂,靶向 MEP 途径中的 IspD 酶,对恶性疟原虫 Dd2 虫株作用的 IC50 值为 250 nM。
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MMV008138 is a species-selective antimalarial agent which targets the enzyme 2- C-methyl-d-erythritol 4-phosphate cytidylyltransferase (IspD) in the MEP pathway, with an IC50 of 250 nM for P. falciparum Dd2 strain[1][2]. IC50: 250 nM (P. falciparum Dd2 strain)[1]
[1]. Ghavami M, et al. Biological Studies and Target Engagement of the 2- C-Methyl-d-Erythritol 4-Phosphate Cytidylyltransferase (IspD)-Targeting Antimalarial Agent (1 R,3 S)-MMV008138 and Analogs. ACS Infect Dis. 2018 Apr 13;4(4):549-559. [2]. Yao ZK, et al. Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure-activity studies. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1515-9.
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