In silico studies of semi-synthetic benzo[a]phenazines as inhibitors of dihydrofolate reductase from Plasmodium falciparum

التفاصيل البيبلوغرافية
العنوان: In silico studies of semi-synthetic benzo[a]phenazines as inhibitors of dihydrofolate reductase from Plasmodium falciparum
المؤلفون: Tanos C. C. França, Raphael S. F. Silva, Joyce S. F. D. de Almeida
المصدر: Journal of Molecular Structure. 1237:130404
بيانات النشر: Elsevier BV, 2021.
سنة النشر: 2021
مصطلحات موضوعية: biology, ATP synthase, 010405 organic chemistry, Chemistry, In silico, Organic Chemistry, Active site, Plasmodium falciparum, 010402 general chemistry, biology.organism_classification, 01 natural sciences, 0104 chemical sciences, Analytical Chemistry, Semi synthetic, Inorganic Chemistry, Pyrimethamine, Biochemistry, parasitic diseases, Dihydrofolate reductase, biology.protein, medicine, Phosphofructokinase 2, Spectroscopy, medicine.drug
الوصف: An in silico study including molecular docking, molecular dynamics simulations and MM-PBSA calculations was performed to investigate if 7 benzo[a]phenazines previously evaluated against malaria parasites, would be able to bind to the DHFR domain of the bifunctional enzyme Dihydrofolate Reductase-Thymidylate Synthase of P. falciparum (PfDHFR-TS). The results showed that all ligands were able to form stable complexes inside the DHFR active site of PfDHFR-TS, similarly to the pyrimethamine analogue, and DHFR inhibitor, BT1. It was also shown that these ligands can be employed as precursors in the computer aided drug design of new antimalarial PfDHFR-TS inhibitors.
تدمد: 0022-2860
DOI: 10.1016/j.molstruc.2021.130404
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::53f2699b9022d7a20857694811f0ae07
https://doi.org/10.1016/j.molstruc.2021.130404
Rights: CLOSED
رقم الانضمام: edsair.doi...........53f2699b9022d7a20857694811f0ae07
قاعدة البيانات: OpenAIRE
الوصف
تدمد:00222860
DOI:10.1016/j.molstruc.2021.130404