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Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening.
Faïon L, Djaout K, Frita R, Pintiala C, Cantrelle FX, Moune M, Vandeputte A, Bourbiaux K, Piveteau C, Herledan A, Biela A, Leroux F, Kremer L, Blaise M, Tanina A, Wintjens R, Hanoulle X, Déprez B, Willand N, Baulard AR, Flipo M. Faïon L, et al. Among authors: tanina a. Eur J Med Chem. 2020 Aug 15;200:112440. doi: 10.1016/j.ejmech.2020.112440. Epub 2020 May 18. Eur J Med Chem. 2020. PMID: 32505086 Free article.
A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2.
Prevet H, Moune M, Tanina A, Kemmer C, Herledan A, Frita R, Wohlkönig A, Bourotte M, Villemagne B, Leroux F, Gitzinger M, Baulard AR, Déprez B, Wintjens R, Willand N, Flipo M. Prevet H, et al. Among authors: tanina a. Eur J Med Chem. 2019 Apr 1;167:426-438. doi: 10.1016/j.ejmech.2019.02.023. Epub 2019 Feb 10. Eur J Med Chem. 2019. PMID: 30784877
A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR.
Tanina A, Wohlkönig A, Soror SH, Flipo M, Villemagne B, Prevet H, Déprez B, Moune M, Perée H, Meyer F, Baulard AR, Willand N, Wintjens R. Tanina A, et al. Biochim Biophys Acta Proteins Proteom. 2019 Mar;1867(3):248-258. doi: 10.1016/j.bbapap.2018.12.003. Epub 2018 Dec 13. Biochim Biophys Acta Proteins Proteom. 2019. PMID: 30553830 Free article.
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: tanina a. Sci Transl Med. 2022 May 4;14(643):eaaz6280. doi: 10.1126/scitranslmed.aaz6280. Epub 2022 May 4. Sci Transl Med. 2022. PMID: 35507672