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Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Thomas M, Brand S, De Rycker M, Zuccotto F, Lukac I, Dodd PG, Ko EJ, Manthri S, McGonagle K, Osuna-Cabello M, Riley J, Pont C, Simeons F, Stojanovski L, Thomas J, Thompson S, Viayna E, Fiandor JM, Martin J, Wyatt PG, Miles TJ, Read KD, Marco M, Gilbert IH. Thomas M, et al. Among authors: martin j. J Med Chem. 2021 May 13;64(9):5905-5930. doi: 10.1021/acs.jmedchem.1c00047. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904304 Free PMC article.
Identifying inhibitors of the Leishmania inositol phosphorylceramide synthase with antiprotozoal activity using a yeast-based assay and ultra-high throughput screening platform.
Norcliffe JL, Mina JG, Alvarez E, Cantizani J, de Dios-Anton F, Colmenarejo G, Valle SG, Marco M, Fiandor JM, Martin JJ, Steel PG, Denny PW. Norcliffe JL, et al. Among authors: martin jj. Sci Rep. 2018 Mar 2;8(1):3938. doi: 10.1038/s41598-018-22063-9. Sci Rep. 2018. PMID: 29500420 Free PMC article.
Metabolic Clustering Analysis as a Strategy for Compound Selection in the Drug Discovery Pipeline for Leishmaniasis.
Armitage EG, Godzien J, Peña I, López-Gonzálvez Á, Angulo S, Gradillas A, Alonso-Herranz V, Martín J, Fiandor JM, Barrett MP, Gabarro R, Barbas C. Armitage EG, et al. Among authors: martin j. ACS Chem Biol. 2018 May 18;13(5):1361-1369. doi: 10.1021/acschembio.8b00204. Epub 2018 Apr 24. ACS Chem Biol. 2018. PMID: 29671577 Free article.
Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition.
Wyllie S, Brand S, Thomas M, De Rycker M, Chung CW, Pena I, Bingham RP, Bueren-Calabuig JA, Cantizani J, Cebrian D, Craggs PD, Ferguson L, Goswami P, Hobrath J, Howe J, Jeacock L, Ko EJ, Korczynska J, MacLean L, Manthri S, Martinez MS, Mata-Cantero L, Moniz S, Nühs A, Osuna-Cabello M, Pinto E, Riley J, Robinson S, Rowland P, Simeons FRC, Shishikura Y, Spinks D, Stojanovski L, Thomas J, Thompson S, Viayna Gaza E, Wall RJ, Zuccotto F, Horn D, Ferguson MAJ, Fairlamb AH, Fiandor JM, Martin J, Gray DW, Miles TJ, Gilbert IH, Read KD, Marco M, Wyatt PG. Wyllie S, et al. Among authors: martin j. Proc Natl Acad Sci U S A. 2019 May 7;116(19):9318-9323. doi: 10.1073/pnas.1820175116. Epub 2019 Apr 8. Proc Natl Acad Sci U S A. 2019. PMID: 30962368 Free PMC article.
Towards discovery of new leishmanicidal scaffolds able to inhibit Leishmania GSK-3.
Martínez de Iturrate P, Sebastián-Pérez V, Nácher-Vázquez M, Tremper CS, Smirlis D, Martín J, Martínez A, Campillo NE, Rivas L, Gil C. Martínez de Iturrate P, et al. Among authors: martin j. J Enzyme Inhib Med Chem. 2020 Dec;35(1):199-210. doi: 10.1080/14756366.2019.1693704. J Enzyme Inhib Med Chem. 2020. PMID: 31752556 Free PMC article.
The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani.
Wall RJ, Carvalho S, Milne R, Bueren-Calabuig JA, Moniz S, Cantizani-Perez J, MacLean L, Kessler A, Cotillo I, Sastry L, Manthri S, Patterson S, Zuccotto F, Thompson S, Martin J, Marco M, Miles TJ, De Rycker M, Thomas MG, Fairlamb AH, Gilbert IH, Wyllie S. Wall RJ, et al. Among authors: martin j. ACS Infect Dis. 2020 Mar 13;6(3):515-528. doi: 10.1021/acsinfecdis.9b00426. Epub 2020 Jan 30. ACS Infect Dis. 2020. PMID: 31967783 Free PMC article.
Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial.
Paradela LS, Wall RJ, Carvalho S, Chemi G, Corpas-Lopez V, Moynihan E, Bello D, Patterson S, Güther MLS, Fairlamb AH, Ferguson MAJ, Zuccotto F, Martin J, Gilbert IH, Wyllie S. Paradela LS, et al. Among authors: martin j. Cell Chem Biol. 2021 May 20;28(5):711-721.e8. doi: 10.1016/j.chembiol.2021.02.008. Epub 2021 Mar 9. Cell Chem Biol. 2021. PMID: 33691122 Free PMC article.
Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.
Thomas MG, McGonagle K, Rowland P, Robinson DA, Dodd PG, Camino-Díaz I, Campbell L, Cantizani J, Castañeda P, Conn D, Craggs PD, Edwards D, Ferguson L, Fosberry A, Frame L, Goswami P, Hu X, Korczynska J, MacLean L, Martin J, Mutter N, Osuna-Cabello M, Paterson C, Peña I, Pinto EG, Pont C, Riley J, Shishikura Y, Simeons FRC, Stojanovski L, Thomas J, Wrobel K, Young RJ, Zmuda F, Zuccotto F, Read KD, Gilbert IH, Marco M, Miles TJ, Manzano P, De Rycker M. Thomas MG, et al. Among authors: martin j. J Med Chem. 2023 Aug 10;66(15):10413-10431. doi: 10.1021/acs.jmedchem.3c00582. Epub 2023 Jul 28. J Med Chem. 2023. PMID: 37506194 Free PMC article.
Short-course combination treatment for experimental chronic Chagas disease.
González S, Wall RJ, Thomas J, Braillard S, Brunori G, Camino Díaz I, Cantizani J, Carvalho S, Castañeda Casado P, Chatelain E, Cotillo I, Fiandor JM, Francisco AF, Grimsditch D, Keenan M, Kelly JM, Kessler A, Luise C, Lyon JJ, MacLean L, Marco M, Martin JJ, Martinez Martinez MS, Paterson C, Read KD, Santos-Villarejo A, Zuccotto F, Wyllie S, Miles TJ, De Rycker M. González S, et al. Among authors: martin jj. Sci Transl Med. 2023 Dec 13;15(726):eadg8105. doi: 10.1126/scitranslmed.adg8105. Epub 2023 Dec 13. Sci Transl Med. 2023. PMID: 38091410 Free PMC article.
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