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Hybrid Inhibitors of Malarial Dihydrofolate Reductase with Dual Binding Modes That Can Forestall Resistance

[Image: see text] The S108N mutation of dihydrofolate reductase (DHFR) renders Plasmodium falciparum malaria parasites resistant to pyrimethamine through steric clash with the rigid side chain of the inhibitor. Inhibitors with flexible side chains can avoid this clash and retain effectiveness agains...

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Publicado en:ACS Med Chem Lett
Autores principales: Tarnchompoo, Bongkoch, Chitnumsub, Penchit, Jaruwat, Aritsara, Shaw, Philip J., Vanichtanankul, Jarunee, Poen, Sinothai, Rattanajak, Roonglawan, Wongsombat, Chayaphat, Tonsomboon, Aunchalee, Decharuangsilp, Sasithorn, Anukunwithaya, Tosapol, Arwon, Uthai, Kamchonwongpaisan, Sumalee, Yuthavong, Yongyuth
Formato: Artigo
Lenguaje:Inglês
Publicado: American Chemical Society 2018
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC6295868/
https://ncbi.nlm.nih.gov/pubmed/30613332
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00389
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