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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.
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.
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.
A Replicative In Vitro Assay for Drug Discovery against Leishmania donovani.
Tegazzini D, Díaz R, Aguilar F, Peña I, Presa JL, Yardley V, Martin JJ, Coteron JM, Croft SL, Cantizani J. Tegazzini D, et al. Among authors: martin jj. Antimicrob Agents Chemother. 2016 May 23;60(6):3524-32. doi: 10.1128/AAC.01781-15. Print 2016 Jun. Antimicrob Agents Chemother. 2016. PMID: 27021313 Free PMC article.
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