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The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors affords a new opportunity for drug repurposing.
Diaz-Gonzalez R, Kuhlmann FM, Galan-Rodriguez C, Madeira da Silva L, Saldivia M, Karver CE, Rodriguez A, Beverley SM, Navarro M, Pollastri MP. Diaz-Gonzalez R, et al. Among authors: pollastri mp. PLoS Negl Trop Dis. 2011 Aug;5(8):e1297. doi: 10.1371/journal.pntd.0001297. Epub 2011 Aug 23. PLoS Negl Trop Dis. 2011. PMID: 21886855 Free PMC article.
Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.
Seixas JD, Luengo-Arratta SA, Diaz R, Saldivia M, Rojas-Barros DI, Manzano P, Gonzalez S, Berlanga M, Smith TK, Navarro M, Pollastri MP. Seixas JD, et al. Among authors: pollastri mp. J Med Chem. 2014 Jun 12;57(11):4834-48. doi: 10.1021/jm500361r. Epub 2014 May 21. J Med Chem. 2014. PMID: 24805946 Free PMC article.
Identification and characterization of hundreds of potent and selective inhibitors of Trypanosoma brucei growth from a kinase-targeted library screening campaign.
Diaz R, Luengo-Arratta SA, Seixas JD, Amata E, Devine W, Cordon-Obras C, Rojas-Barros DI, Jimenez E, Ortega F, Crouch S, Colmenarejo G, Fiandor JM, Martin JJ, Berlanga M, Gonzalez S, Manzano P, Navarro M, Pollastri MP. Diaz R, et al. Among authors: pollastri mp. PLoS Negl Trop Dis. 2014 Oct 23;8(10):e3253. doi: 10.1371/journal.pntd.0003253. eCollection 2014 Oct. PLoS Negl Trop Dis. 2014. PMID: 25340575 Free PMC article.
Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?
Amata E, Xi H, Colmenarejo G, Gonzalez-Diaz R, Cordon-Obras C, Berlanga M, Manzano P, Erath J, Roncal NE, Lee PJ, Leed SE, Rodriguez A, Sciotti RJ, Navarro M, Pollastri MP. Amata E, et al. Among authors: pollastri mp. ACS Infect Dis. 2016 Mar 11;2(3):180-186. doi: 10.1021/acsinfecdis.5b00136. Epub 2016 Jan 17. ACS Infect Dis. 2016. PMID: 26998514 Free PMC article.
From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis.
Devine WG, Diaz-Gonzalez R, Ceballos-Perez G, Rojas D, Satoh T, Tear W, Ranade RM, Barros-Álvarez X, Hol WG, Buckner FS, Navarro M, Pollastri MP. Devine WG, et al. Among authors: pollastri mp. ACS Infect Dis. 2017 Mar 10;3(3):225-236. doi: 10.1021/acsinfecdis.6b00202. Epub 2017 Feb 8. ACS Infect Dis. 2017. PMID: 28110521 Free PMC article.
Anilinoquinoline based inhibitors of trypanosomatid proliferation.
Ferrins L, Sharma A, Thomas SM, Mehta N, Erath J, Tanghe S, Leed SE, Rodriguez A, Mensa-Wilmot K, Sciotti RJ, Gillingwater K, Pollastri MP. Ferrins L, et al. Among authors: pollastri mp. PLoS Negl Trop Dis. 2018 Nov 26;12(11):e0006834. doi: 10.1371/journal.pntd.0006834. eCollection 2018 Nov. PLoS Negl Trop Dis. 2018. PMID: 30475800 Free PMC article.
Evaluation of a class of isatinoids identified from a high-throughput screen of human kinase inhibitors as anti-Sleeping Sickness agents.
Klug DM, Diaz-Gonzalez R, Pérez-Moreno G, Ceballos-Pérez G, García-Hernández R, Gomez-Pérez V, Ruiz-Pérez LM, Rojas-Barros DI, Gamarro F, González-Pacanowska D, Martínez-Martínez MS, Manzano P, Ferrins L, Caffrey CR, Navarro M, Pollastri MP. Klug DM, et al. Among authors: pollastri mp. PLoS Negl Trop Dis. 2019 Feb 8;13(2):e0007129. doi: 10.1371/journal.pntd.0007129. eCollection 2019 Feb. PLoS Negl Trop Dis. 2019. PMID: 30735501 Free PMC article.
Hit-to-Lead Optimization of Benzoxazepinoindazoles As Human African Trypanosomiasis Therapeutics.
Klug DM, Tschiegg L, Diaz R, Rojas-Barros D, Perez-Moreno G, Ceballos G, García-Hernández R, Martinez-Martinez MS, Manzano P, Ruiz LM, Caffrey CR, Gamarro F, Pacanowska DG, Ferrins L, Navarro M, Pollastri MP. Klug DM, et al. Among authors: pollastri mp. J Med Chem. 2020 Mar 12;63(5):2527-2546. doi: 10.1021/acs.jmedchem.9b01506. Epub 2019 Nov 20. J Med Chem. 2020. PMID: 31670951 Free PMC article.
71 results