Other search tools

About this data

The publication data currently available has been vetted by Vanderbilt faculty, staff, administrators and trainees. The data itself is retrieved directly from NCBI's PubMed and is automatically updated on a weekly basis to ensure accuracy and completeness.

If you have any questions or comments, please contact us.

Results: 1 to 10 of 30

Publication Record

Connections

A new chemotype with promise against Trypanosoma cruzi.
Wang X, Cal M, Kaiser M, Buckner FS, Lepesheva GI, Sanford AG, Wallick AI, Davis PH, Vennerstrom JL
(2020) Bioorg Med Chem Lett 30: 126778
MeSH Terms: Animals, Chagas Disease, Humans, Structure-Activity Relationship, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Successful Aspects of the Coadministration of Sterol 14α-Demethylase Inhibitor VFV and Benznidazole in Experimental Mouse Models of Chagas Disease Caused by the Drug-Resistant Strain of Trypanosoma cruzi.
Guedes-da-Silva FH, Batista DDGJ, Da Silva CF, Pavão BP, Batista MM, Moreira OC, Souza LRQ, Britto C, Rachakonda G, Villalta F, Lepesheva GI, Soeiro MNC
(2019) ACS Infect Dis 5: 365-371
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Disease Models, Animal, Drug Synergism, Drug Therapy, Combination, Humans, Male, Mice, Nitroimidazoles, Protozoan Proteins, Sterol 14-Demethylase, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.
Friggeri L, Hargrove TY, Rachakonda G, Blobaum AL, Fisher P, de Oliveira GM, da Silva CF, Soeiro MNC, Nes WD, Lindsley CW, Villalta F, Guengerich FP, Lepesheva GI
(2018) J Med Chem 61: 10910-10921
MeSH Terms: 14-alpha Demethylase Inhibitors, Antiprotozoal Agents, Chagas Disease, Drug Design, Drug Stability, Humans, Microsomes, Models, Molecular, Protein Conformation, Sterol 14-Demethylase, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Binding of a physiological substrate causes large-scale conformational reorganization in cytochrome P450 51.
Hargrove TY, Wawrzak Z, Fisher PM, Child SA, Nes WD, Guengerich FP, Waterman MR, Lepesheva GI
(2018) J Biol Chem 293: 19344-19353
MeSH Terms: Biocatalysis, Electron Transport, Enzyme Stability, Heme, Models, Molecular, Protein Binding, Protein Conformation, Sterol 14-Demethylase, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
CYP51 as drug targets for fungi and protozoan parasites: past, present and future.
Lepesheva GI, Friggeri L, Waterman MR
(2018) Parasitology 145: 1820-1836
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Antifungal Agents, Cytochrome P450 Family 51, Fungemia, Fungi, Humans, Models, Molecular, Parasites, Protein Binding, Substrate Specificity, Trypanosoma brucei brucei, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Antitrypanosomal Activity of Sterol 14α-Demethylase (CYP51) Inhibitors VNI and VFV in the Swiss Mouse Models of Chagas Disease Induced by the Trypanosoma cruzi Y Strain.
Guedes-da-Silva FH, Batista DG, Da Silva CF, De Araújo JS, Pavão BP, Simões-Silva MR, Batista MM, Demarque KC, Moreira OC, Britto C, Lepesheva GI, Soeiro MN
(2017) Antimicrob Agents Chemother 61:
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Cyclophosphamide, Cytochrome P-450 Enzyme System, Disease Models, Animal, Drug Administration Schedule, Female, Gene Expression, Humans, Imidazoles, Immunosuppressive Agents, Male, Mice, Models, Molecular, Nitroimidazoles, Oxadiazoles, Parasite Load, Recurrence, Survival Analysis, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
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
(2016) Antimicrob Agents Chemother 60: 1058-66
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Crystallography, X-Ray, Disease Models, Animal, Female, Heme, Mice, Models, Molecular, Protein Conformation, Pyridines, Sterol 14-Demethylase, Tetrazoles, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Different Therapeutic Outcomes of Benznidazole and VNI Treatments in Different Genders in Mouse Experimental Models of Trypanosoma cruzi Infection.
Guedes-da-Silva FH, Batista DG, da Silva CF, Meuser MB, Simões-Silva MR, de Araújo JS, Ferreira CG, Moreira OC, Britto C, Lepesheva GI, Soeiro Mde N
(2015) Antimicrob Agents Chemother 59: 7564-70
MeSH Terms: 14-alpha Demethylase Inhibitors, Animals, Chagas Disease, Cytochrome P-450 Enzyme System, Disease Models, Animal, Drug Administration Schedule, Drug Evaluation, Preclinical, Female, Gene Expression, Imidazoles, Immunosuppressive Agents, Male, Mice, Nitroimidazoles, Oxadiazoles, Parasitemia, Sex Factors, Treatment Outcome, Trypanocidal Agents, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
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
(2015) J Infect Dis 212: 1439-48
MeSH Terms: Animals, Antiprotozoal Agents, Benzamides, Biotransformation, Chagas Disease, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Enzyme System, Disease Models, Animal, Female, Humans, Imidazoles, Inhibitory Concentration 50, Leishmaniasis, Visceral, Mice, Mice, Inbred BALB C, Microsomes, Liver, Molecular Structure, Oxadiazoles, Rats, Structure-Activity Relationship, Tissue Distribution, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
Papadopoulou MV, Bloomer WD, Lepesheva GI, Rosenzweig HS, Kaiser M, Aguilera-Venegas B, Wilkinson SR, Chatelain E, Ioset JR
(2015) J Med Chem 58: 1307-19
MeSH Terms: Amides, Animals, Cell Line, Chagas Disease, Dose-Response Relationship, Drug, Methanol, Mice, Mice, Inbred BALB C, Molecular Structure, Parasitic Sensitivity Tests, Rats, Structure-Activity Relationship, Triazoles, Trypanocidal Agents, Trypanosoma brucei rhodesiense, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms