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WR99210

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.

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