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Cellular response to Trypanosoma cruzi infection induces secretion of defensin α-1, which damages the flagellum, neutralizes trypanosome motility, and inhibits infection.
Johnson CA, Rachakonda G, Kleshchenko YY, Nde PN, Madison MN, Pratap S, Cardenas TC, Taylor C, Lima MF, Villalta F. Johnson CA, et al. Among authors: rachakonda g. Infect Immun. 2013 Nov;81(11):4139-48. doi: 10.1128/IAI.01459-12. Epub 2013 Aug 26. Infect Immun. 2013. PMID: 23980110 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: rachakonda g. 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.
VFV as a New Effective CYP51 Structure-Derived Drug Candidate for Chagas Disease and Visceral Leishmaniasis.
Lepesheva GI, Hargrove TY, Rachakonda G, Wawrzak Z, Pomel S, Cojean S, Nde PN, Nes WD, Locuson CW, Calcutt MW, Waterman MR, Daniels JS, Loiseau PM, Villalta F. Lepesheva GI, et al. Among authors: rachakonda g. J Infect Dis. 2015 Nov 1;212(9):1439-48. doi: 10.1093/infdis/jiv228. Epub 2015 Apr 15. J Infect Dis. 2015. PMID: 25883390 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: rachakonda g. 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.
Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity.
Hargrove TY, Garvey EP, Hoekstra WJ, Yates CM, Wawrzak Z, Rachakonda G, Villalta F, Lepesheva GI. Hargrove TY, et al. Among authors: rachakonda g. Antimicrob Agents Chemother. 2017 Jun 27;61(7):e00570-17. doi: 10.1128/AAC.00570-17. Print 2017 Jul. Antimicrob Agents Chemother. 2017. PMID: 28461309 Free PMC article.
Sterol 14α-Demethylase Structure-Based Design of VNI (( R)- N-(1-(2,4-Dichlorophenyl)-2-(1 H-imidazol-1-yl)ethyl)-4-(5-phenyl-1,3,4-oxadiazol-2-yl)benzamide)) Derivatives To Target Fungal Infections: Synthesis, Biological Evaluation, and Crystallographic Analysis.
Friggeri L, Hargrove TY, Wawrzak Z, Blobaum AL, Rachakonda G, Lindsley CW, Villalta F, Nes WD, Botta M, Guengerich FP, Lepesheva GI. Friggeri L, et al. Among authors: rachakonda g. J Med Chem. 2018 Jul 12;61(13):5679-5691. doi: 10.1021/acs.jmedchem.8b00641. Epub 2018 Jun 25. J Med Chem. 2018. PMID: 29894182 Free PMC article.
36 results