Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors

Laura Friggeri, Tatiana Y. Hargrove, Zdzislaw Wawrzak, F. Peter Guengerich, Galina I. Lepesheva^*

^*Corresponding author for this work

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Human sterol 14a-demethylase (CYP51) in complex with the functionally irreversible inhibitor (R)-N-(1-(3-chloro-4'-fluoro-[1,1'-biphenyl]-4-yl)-2-(1H-imidazol-1-yl)ethyl)-4-(5-(3-fluoro-5-(5-fluoropyrimidin-4-yl)phenyl)-1,3,4-oxadiazol-2-yl)benzamide
Friggeri, L. (Contributor), Hargrove, T. Y. (Contributor), Wawrzak, Z. (Contributor), Guengerich, F. P. (Contributor) & Lepesheva, G. I. (Contributor), Protein Data Bank (PDB), Nov 13 2019
DOI: 10.2210/pdb6Q2T/pdb, https://www.wwpdb.org/pdb?id=pdb_00006q2t
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