Ontology highlight
ABSTRACT:
SUBMITTER: Choi JY
PROVIDER: S-EPMC4027616 | biostudies-literature | 2014 Apr
REPOSITORIES: biostudies-literature
Choi Jun Yong JY Calvet Claudia M CM Vieira Debora F DF Gunatilleke Shamila S SS Cameron Michael D MD McKerrow James H JH Podust Larissa M LM Roush William R WR
ACS medicinal chemistry letters 20140122 4
Sterol 14α-demethylase (CYP51) is an important therapeutic target for fungal and parasitic infections due to its key role in the biosynthesis of ergosterol, an essential component of the cell membranes of these pathogenic organisms. We report the development of potent and selective d-tryptophan-derived inhibitors of T. cruzi CYP51. Structural information obtained from the cocrystal structure of CYP51 and (R)-2, which is >1000-fold more potent than its enantiomer (S)-1, was used to guide design o ...[more]