| Literature DB >> 24440298 |
Hitesh Sharma1, Mark J Landau2, Todd J Sullivan3, Vidya P Kumar1, Markus K Dahlgren3, William L Jorgensen3, Karen S Anderson4.
Abstract
The parasite Toxoplasma gondii can lead to toxoplasmosis in those who are immunocompromised. To combat the infection, the enzyme responsible for nucleotide synthesis thymidylate synthase-dihydrofolate reductase (TS-DHFR) is a suitable drug target. We have used virtual screening to determine novel allosteric inhibitors at the interface between the two TS domains. Selected compounds from virtual screening inhibited TS activity. Thus, these results show that allosteric inhibition by small drug-like molecules can occur in T. gondii TS-DHFR and pave the way for new and potent species-specific inhibitors.Entities:
Keywords: Dihydrofolate reductase; Thymidylate synthase; Toxoplasma gondii; Virtual screening
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Year: 2013 PMID: 24440298 PMCID: PMC3946055 DOI: 10.1016/j.bmcl.2013.12.039
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823