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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity.
Villemagne B, Machelart A, Tran NC, Flipo M, Moune M, Leroux F, Piveteau C, Wohlkönig A, Wintjens R, Li X, Gref R, Brodin P, Deprez B, Baulard AR, Willand N. Villemagne B, et al. Among authors: baulard ar. ACS Infect Dis. 2020 Mar 13;6(3):366-378. doi: 10.1021/acsinfecdis.9b00277. Epub 2020 Mar 2. ACS Infect Dis. 2020. PMID: 32011115
Tuberculosis: the drug development pipeline at a glance.
Villemagne B, Crauste C, Flipo M, Baulard AR, Déprez B, Willand N. Villemagne B, et al. 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.
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches.
Villemagne B, Flipo M, Blondiaux N, Crauste C, Malaquin S, Leroux F, Piveteau C, Villeret V, Brodin P, Villoutreix BO, Sperandio O, Soror SH, Wohlkönig A, Wintjens R, Deprez B, Baulard AR, Willand N. Villemagne B, et al. Among authors: baulard ar. J Med Chem. 2014 Jun 12;57(11):4876-88. doi: 10.1021/jm500422b. Epub 2014 May 28. J Med Chem. 2014. PMID: 24818704
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420.
Blondiaux N, Moune M, Desroses M, Frita R, Flipo M, Mathys V, Soetaert K, Kiass M, Delorme V, Djaout K, Trebosc V, Kemmer C, Wintjens R, Wohlkönig A, Antoine R, Huot L, Hot D, Coscolla M, Feldmann J, Gagneux S, Locht C, Brodin P, Gitzinger M, Déprez B, Willand N, Baulard AR. Blondiaux N, et al. Among authors: baulard ar. Science. 2017 Mar 17;355(6330):1206-1211. doi: 10.1126/science.aag1006. Epub 2017 Mar 16. Science. 2017. PMID: 28302858
Phenotypic assays for Mycobacterium tuberculosis infection.
Song OR, Deboosere N, Delorme V, Queval CJ, Deloison G, Werkmeister E, Lafont F, Baulard A, Iantomasi R, Brodin P. Song OR, et al. Among authors: baulard a. Cytometry A. 2017 Oct;91(10):983-994. doi: 10.1002/cyto.a.23129. Epub 2017 May 19. Cytometry A. 2017. PMID: 28544095 Free article.
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays.
Nikiforov PO, Blaszczyk M, Surade S, Boshoff HI, Sajid A, Delorme V, Deboosere N, Brodin P, Baulard AR, Barry CE 3rd, Blundell TL, Abell C. Nikiforov PO, et al. Among authors: baulard ar. ACS Chem Biol. 2017 May 19;12(5):1390-1396. doi: 10.1021/acschembio.7b00091. Epub 2017 Apr 5. ACS Chem Biol. 2017. PMID: 28314097 Free PMC article.
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: baulard ar. 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.
78 results