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antiplasmodial compound

NOT Open Access | A novel antiplasmodial compound: integration of in silico and in vitro assays

February 10, 2021 - 09:51 -- NOT Open Access
Costa Júnior DB, Araújo JSC, Oliveira LM, Neri FSM, Moreira POL, Taranto AG, Fonseca AL, Varotti FP, Leite FHA
J Biomol Struct Dyn. 2021 Feb 8:1-13

Malaria is a disease caused by Plasmodium genus. which P. falciparum is responsible for the most severe form of the disease, cerebral malaria. In 2018, 405,000 people died of malaria. Antimalarial drugs have serious adverse effects and limited efficacy due to multidrug-resistant strains. One way to overcome these limitations is the use of computational approaches for prioritizing candidates to phenotypic assays and/or in vitro assays against validated targets. Plasmodium falciparum Enoyl-ACP reductase (PfENR) is noteworthy because it catalyzes the rate-limiting step of the biosynthetic pathway of fatty acid.

NOT Open Access | Resistance to some, but not other dimeric lindenane sesquiterpenoid esters is mediated by mutations in a Plasmodium falciparum esterase

September 29, 2020 - 13:08 -- NOT Open Access
Butler JH, Baptista RP, Valenciano AL, Zhou B, Kissinger JC, Tumwebaze PK, Rosenthal PJ, Cooper R, Yue JM, Cassera MB
ACS Infect Dis. 2020 Sep 24

Unique lindenane sesquiterpenoid dimers from Chloranthecae spp. were recently identified with promising in vitro antiplasmodial activity and potentially novel mechanisms of action. To gain mechanistic insights to this new class of natural products, in vitro selection of Plasmodium falciparum resistance to the most active antiplasmodial compound, chlorajaponilide C, was explored.

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