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Items: 24

1.

Advances in preclinical approaches to Chagas disease drug discovery.

Villalta F, Rachakonda G.

Expert Opin Drug Discov. 2019 Nov;14(11):1161-1174. doi: 10.1080/17460441.2019.1652593. Epub 2019 Aug 14.

PMID:
31411084
2.

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.

ACS Infect Dis. 2019 Mar 8;5(3):365-371. doi: 10.1021/acsinfecdis.8b00253. Epub 2019 Jan 23.

PMID:
30625275
3.

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.

J Med Chem. 2018 Dec 13;61(23):10910-10921. doi: 10.1021/acs.jmedchem.8b01671. Epub 2018 Nov 30.

PMID:
30451500
4.

Phospho-proteomic analysis of primary human colon epithelial cells during the early Trypanosoma cruzi infection phase.

Suman S, Rachakonda G, Mandape SN, Sakhare SS, Villalta F, Pratap S, Lima MF, Nde PN.

PLoS Negl Trop Dis. 2018 Sep 17;12(9):e0006792. doi: 10.1371/journal.pntd.0006792. eCollection 2018 Sep.

5.

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.

J Med Chem. 2018 Jul 12;61(13):5679-5691. doi: 10.1021/acs.jmedchem.8b00641. Epub 2018 Jun 25.

6.

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.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00570-17. doi: 10.1128/AAC.00570-17. Print 2017 Jul.

7.

Epitope Capsid-Incorporation: New Effective Approach for Vaccine Development for Chagas Disease.

Matthews QL, Farrow AL, Rachakonda G, Gu L, Nde P, Krendelchtchikov A, Pratap S, Sakhare SS, Sabbaj S, Lima MF, Villalta F.

Pathog Immun. 2016 Fall-Winter;1(2):214-233.

8.

Role of TGF-β-induced Claudin-4 expression through c-Jun signaling in non-small cell lung cancer.

Rachakonda G, Vu T, Jin L, Samanta D, Datta PK.

Cell Signal. 2016 Oct;28(10):1537-44. doi: 10.1016/j.cellsig.2016.07.006. Epub 2016 Jul 15.

PMID:
27424491
9.

Early Regulation of Profibrotic Genes in Primary Human Cardiac Myocytes by Trypanosoma cruzi.

Udoko AN, Johnson CA, Dykan A, Rachakonda G, Villalta F, Mandape SN, Lima MF, Pratap S, Nde PN.

PLoS Negl Trop Dis. 2016 Jan 15;10(1):e0003747. doi: 10.1371/journal.pntd.0003747. eCollection 2016 Jan.

10.

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.

Antimicrob Agents Chemother. 2015 Dec 7;60(2):1058-66. doi: 10.1128/AAC.02287-15. Print 2016 Feb.

11.

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.

J Infect Dis. 2015 Nov 1;212(9):1439-48. doi: 10.1093/infdis/jiv228. Epub 2015 Apr 15.

12.

Immunization with Hexon modified adenoviral vectors integrated with gp83 epitope provides protection against Trypanosoma cruzi infection.

Farrow AL, Rachakonda G, Gu L, Krendelchtchikova V, Nde PN, Pratap S, Lima MF, Villalta F, Matthews QL.

PLoS Negl Trop Dis. 2014 Aug 21;8(8):e3089. doi: 10.1371/journal.pntd.0003089. eCollection 2014 Aug.

13.

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.

J Med Chem. 2014 Aug 14;57(15):6704-17. doi: 10.1021/jm500739f. Epub 2014 Jul 29.

14.

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.

Infect Immun. 2013 Nov;81(11):4139-48. doi: 10.1128/IAI.01459-12. Epub 2013 Aug 26.

15.

The novel antiangiogenic VJ115 inhibits the NADH oxidase ENOX1 and cytoskeleton-remodeling proteins.

Venkateswaran A, Friedman DB, Walsh AJ, Skala MC, Sasi S, Rachakonda G, Crooks PA, Freeman ML, Sekhar KR.

Invest New Drugs. 2013 Jun;31(3):535-44. doi: 10.1007/s10637-012-9884-9. Epub 2012 Oct 9.

16.

The novel chemical entity YTR107 inhibits recruitment of nucleophosmin to sites of DNA damage, suppressing repair of DNA double-strand breaks and enhancing radiosensitization.

Sekhar KR, Reddy YT, Reddy PN, Crooks PA, Venkateswaran A, McDonald WH, Geng L, Sasi S, Van Der Waal RP, Roti JL, Salleng KJ, Rachakonda G, Freeman ML.

Clin Cancer Res. 2011 Oct 15;17(20):6490-9. doi: 10.1158/1078-0432.CCR-11-1054. Epub 2011 Aug 30.

17.

NRF2 deficiency reduces life span of mice administered thoracic irradiation.

Travis EL, Rachakonda G, Zhou X, Korhonen K, Sekhar KR, Biswas S, Freeman ML.

Free Radic Biol Med. 2011 Sep 15;51(6):1175-83. doi: 10.1016/j.freeradbiomed.2011.05.038. Epub 2011 Jun 12.

18.

Increased cell migration and plasticity in Nrf2-deficient cancer cell lines.

Rachakonda G, Sekhar KR, Jowhar D, Samson PC, Wikswo JP, Beauchamp RD, Datta PK, Freeman ML.

Oncogene. 2010 Jun 24;29(25):3703-14. doi: 10.1038/onc.2010.118. Epub 2010 May 3.

19.

Cysteine-based regulation of the CUL3 adaptor protein Keap1.

Sekhar KR, Rachakonda G, Freeman ML.

Toxicol Appl Pharmacol. 2010 Apr 1;244(1):21-6. doi: 10.1016/j.taap.2009.06.016. Epub 2009 Jun 26. Review.

20.

Indolyl-quinuclidinols inhibit ENOX activity and endothelial cell morphogenesis while enhancing radiation-mediated control of tumor vasculature.

Geng L, Rachakonda G, Morré DJ, Morré DM, Crooks PA, Sonar VN, Roti JL, Rogers BE, Greco S, Ye F, Salleng KJ, Sasi S, Freeman ML, Sekhar KR.

FASEB J. 2009 Sep;23(9):2986-95. doi: 10.1096/fj.09-130005. Epub 2009 Apr 24.

21.

Smad7 induces hepatic metastasis in colorectal cancer.

Halder SK, Rachakonda G, Deane NG, Datta PK.

Br J Cancer. 2008 Sep 16;99(6):957-65. doi: 10.1038/sj.bjc.6604562.

22.

Genetic diversity of noroviruses and sapoviruses in children with acute sporadic gastroenteritis in New Delhi, India.

Rachakonda G, Choudekar A, Parveen S, Bhatnagar S, Patwari A, Broor S.

J Clin Virol. 2008 Sep;43(1):42-8. doi: 10.1016/j.jcv.2008.05.006. Epub 2008 Jul 7.

PMID:
18602864
23.

Covalent modification at Cys151 dissociates the electrophile sensor Keap1 from the ubiquitin ligase CUL3.

Rachakonda G, Xiong Y, Sekhar KR, Stamer SL, Liebler DC, Freeman ML.

Chem Res Toxicol. 2008 Mar;21(3):705-10. doi: 10.1021/tx700302s. Epub 2008 Feb 6.

PMID:
18251510
24.

Activating transcription factor 3 is a novel repressor of the nuclear factor erythroid-derived 2-related factor 2 (Nrf2)-regulated stress pathway.

Brown SL, Sekhar KR, Rachakonda G, Sasi S, Freeman ML.

Cancer Res. 2008 Jan 15;68(2):364-8. doi: 10.1158/0008-5472.CAN-07-2170.

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