Complexes of Trypanosoma cruzi sterol 14α-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.

@article{Hargrove2013ComplexesOT,
  title={Complexes of Trypanosoma cruzi sterol 14α-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.},
  author={Tatiana Y. Hargrove and Zdzislaw Wawrzak and Paul Alexander and Jason H. Chaplin and Martine Keenan and Susan A. Charman and Catherine J Perez and Michael R. Waterman and Eric Chatelain and Galina I Lepesheva},
  journal={The Journal of biological chemistry},
  year={2013},
  volume={288 44},
  pages={31602-15}
}
Chagas disease, caused by the eukaryotic (protozoan) parasite Trypanosoma cruzi, is an alarming emerging global health problem with no clinical drugs available to treat the chronic stage. Azole inhibitors of sterol 14α-demethylase (CYP51) were proven effective against Chagas, and antifungal drugs posaconazole and ravuconazole have entered clinical trials in Spain, Bolivia, and Argentina. Here we present the x-ray structures of T. cruzi CYP51 in complexes with two alternative drug candidates… CONTINUE READING
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