The solution structure of Bacillus anthracis dihydrofolate reductase yields insight into the analysis of structure-activity relationships for novel inhibitors.

@article{Beierlein2009TheSS,
  title={The solution structure of Bacillus anthracis dihydrofolate reductase yields insight into the analysis of structure-activity relationships for novel inhibitors.},
  author={Jennifer M Beierlein and Lalit Deshmukh and Kathleen M. Frey and Olga Pavlovna Vinogradova and Amy C. Anderson},
  journal={Biochemistry},
  year={2009},
  volume={48 19},
  pages={4100-8}
}
There is a significant need for new therapeutics to treat infections caused by the biodefense agent Bacillus anthracis. In pursuit of drug discovery against this organism, we have developed novel propargyl-linked inhibitors that target the essential enzyme dihydrofolate reductase (DHFR) from B. anthracis. Previously, we reported an initial series of these inhibitors and a high-resolution crystal structure of the ternary complex of the enzyme bound to its cofactor and one of the most potent… CONTINUE READING
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