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dihydrofolate reductase

NOT Open Access | Regioisomerization of antimalarial drug WR99210 explains the inactivity of a commercial stock

October 21, 2020 - 09:24 -- NOT Open Access
Author(s): 
Remcho TP, Guggilapu SD, Cruz P, Nardone GA, Heffernan G, O'Connor RD, Bewley CA, Wellems TE, Lane KD
Reference: 
Antimicrob Agents Chemother. 2020 Oct 19:AAC.01385-20

WR99210, a former antimalarial drug candidate now widely used for the selection of Plasmodium transfectants, selectively targets the parasite dihydrofolate reductase thymidine synthase bifunctional enzyme (DHFR-TS) but not human DHFR, which is not fused with TS. Accordingly, WR99210 and plasmids expressing human dhfr have become valued tools for the genetic modification of parasites in the laboratory.

NOT Open Access | Discovery of traditional Chinese medicine derived compounds as wild type and mutant Plasmodium falciparum dihydrofolate reductase inhibitors: Induced fit docking and ADME studies

August 3, 2020 - 15:34 -- NOT Open Access
Author(s): 
Iwaloye O, Elekofehinti OO, Kikiowo B, Fadipe TM, Akinjiyan MO, Ariyo EO, Aiyeku OO, Adewumi NA
Reference: 
Curr Drug Discov Technol. 2020 Jul 29

In a bid to come up with effective compounds as inhibitors in antimalarial treatment, we built a library containing about 2,000 traditional Chinese medicine(TCM)-derived compounds retrieved from TCM Data-base@Taiwan. The active sites of both the wild type and mutant Plasmodium falciparum dihydrofolate reductase (pfDHFR) were explored using computational tools. pfDHFR, one of the prime drug targets in the prevention of malaria infection induced by the female anopheles mosquito has continued to coffer resistance to drugs (antifolates) due to mutation in some of the key amino acid residues crucial for its inhibition.

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