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Crystal structures of Trypanosoma brucei sterol 14alpha-demethylase and implications for selective treatment of human infections.
Lepesheva GI, Park HW, Hargrove TY, Vanhollebeke B, Wawrzak Z, Harp JM, Sundaramoorthy M, Nes WD, Pays E, Chaudhuri M, Villalta F, Waterman MR. Lepesheva GI, et al. Among authors: wawrzak z. J Biol Chem. 2010 Jan 15;285(3):1773-80. doi: 10.1074/jbc.M109.067470. Epub 2009 Nov 18. J Biol Chem. 2010. PMID: 19923211 Free PMC article.
Complexes of Trypanosoma cruzi sterol 14α-demethylase (CYP51) with two pyridine-based drug candidates for Chagas disease: structural basis for pathogen selectivity.
Hargrove TY, Wawrzak Z, Alexander PW, Chaplin JH, Keenan M, Charman SA, Perez CJ, Waterman MR, Chatelain E, Lepesheva GI. Hargrove TY, et al. Among authors: wawrzak z. J Biol Chem. 2013 Nov 1;288(44):31602-15. doi: 10.1074/jbc.M113.497990. Epub 2013 Sep 18. J Biol Chem. 2013. PMID: 24047900 Free PMC article.
Structural basis for rational design of inhibitors targeting Trypanosoma cruzi sterol 14α-demethylase: two regions of the enzyme molecule potentiate its inhibition.
Friggeri L, Hargrove TY, Rachakonda G, Williams AD, Wawrzak Z, Di Santo R, De Vita D, Waterman MR, Tortorella S, Villalta F, Lepesheva GI. Friggeri L, et al. Among authors: wawrzak z. J Med Chem. 2014 Aug 14;57(15):6704-17. doi: 10.1021/jm500739f. Epub 2014 Jul 29. J Med Chem. 2014. PMID: 25033013 Free PMC article.
Clinical Candidate VT-1161's Antiparasitic Effect In Vitro, Activity in a Murine Model of Chagas Disease, and Structural Characterization in Complex with the Target Enzyme CYP51 from Trypanosoma cruzi.
Hoekstra WJ, Hargrove TY, Wawrzak Z, da Gama Jaen Batista D, da Silva CF, Nefertiti AS, Rachakonda G, Schotzinger RJ, Villalta F, Soeiro Mde N, Lepesheva GI. Hoekstra WJ, et al. Among authors: wawrzak z. Antimicrob Agents Chemother. 2015 Dec 7;60(2):1058-66. doi: 10.1128/AAC.02287-15. Print 2016 Feb. Antimicrob Agents Chemother. 2015. PMID: 26643331 Free PMC article.
Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis.
Hargrove TY, Friggeri L, Wawrzak Z, Qi A, Hoekstra WJ, Schotzinger RJ, York JD, Guengerich FP, Lepesheva GI. Hargrove TY, et al. Among authors: wawrzak z. J Biol Chem. 2017 Apr 21;292(16):6728-6743. doi: 10.1074/jbc.M117.778308. Epub 2017 Mar 3. J Biol Chem. 2017. PMID: 28258218 Free PMC article.
102 results