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The small-molecule SMARt751 reverses Mycobacterium tuberculosis resistance to ethionamide in acute and chronic mouse models of tuberculosis.
Flipo M, Frita R, Bourotte M, Martínez-Martínez MS, Boesche M, Boyle GW, Derimanov G, Drewes G, Gamallo P, Ghidelli-Disse S, Gresham S, Jiménez E, de Mercado J, Pérez-Herrán E, Porras-De Francisco E, Rullas J, Casado P, Leroux F, Piveteau C, Kiass M, Mathys V, Soetaert K, Megalizzi V, Tanina A, Wintjens R, Antoine R, Brodin P, Delorme V, Moune M, Djaout K, Slupek S, Kemmer C, Gitzinger M, Ballell L, Mendoza-Losana A, Lociuro S, Deprez B, Barros-Aguirre D, Remuiñán MJ, Willand N, Baulard AR. Flipo M, et al. Among authors: baulard ar. Sci Transl Med. 2022 May 4;14(643):eaaz6280. doi: 10.1126/scitranslmed.aaz6280. Epub 2022 May 4. Sci Transl Med. 2022. PMID: 35507672
Synthetic EthR inhibitors boost antituberculous activity of ethionamide.
Willand N, Dirié B, Carette X, Bifani P, Singhal A, Desroses M, Leroux F, Willery E, Mathys V, Déprez-Poulain R, Delcroix G, Frénois F, Aumercier M, Locht C, Villeret V, Déprez B, Baulard AR. Willand N, et al. Among authors: baulard ar. Nat Med. 2009 May;15(5):537-44. doi: 10.1038/nm.1950. Epub 2009 May 3. Nat Med. 2009. PMID: 19412174
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors.
Flipo M, Desroses M, Lecat-Guillet N, Dirié B, Carette X, Leroux F, Piveteau C, Demirkaya F, Lens Z, Rucktooa P, Villeret V, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N. Flipo M, et al. Among authors: baulard ar. J Med Chem. 2011 Apr 28;54(8):2994-3010. doi: 10.1021/jm200076a. Epub 2011 Apr 1. J Med Chem. 2011. PMID: 21417236
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors.
Flipo M, Desroses M, Lecat-Guillet N, Villemagne B, Blondiaux N, Leroux F, Piveteau C, Mathys V, Flament MP, Siepmann J, Villeret V, Wohlkönig A, Wintjens R, Soror SH, Christophe T, Jeon HK, Locht C, Brodin P, Déprez B, Baulard AR, Willand N. Flipo M, et al. Among authors: baulard ar. J Med Chem. 2012 Jan 12;55(1):68-83. doi: 10.1021/jm200825u. Epub 2011 Dec 6. J Med Chem. 2012. PMID: 22098589
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands.
Carette X, Blondiaux N, Willery E, Hoos S, Lecat-Guillet N, Lens Z, Wohlkönig A, Wintjens R, Soror SH, Frénois F, Dirié B, Villeret V, England P, Lippens G, Deprez B, Locht C, Willand N, Baulard AR. Carette X, et al. Among authors: baulard ar. Nucleic Acids Res. 2012 Apr;40(7):3018-30. doi: 10.1093/nar/gkr1113. Epub 2011 Dec 9. Nucleic Acids Res. 2012. PMID: 22156370 Free PMC article.
Tuberculosis: the drug development pipeline at a glance.
Villemagne B, Crauste C, Flipo M, Baulard AR, Déprez B, Willand N. Villemagne B, et al. Among authors: baulard ar. Eur J Med Chem. 2012 May;51:1-16. doi: 10.1016/j.ejmech.2012.02.033. Epub 2012 Feb 25. Eur J Med Chem. 2012. PMID: 22421275 Review.
77 results