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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.
Unique mechanism of action of the thiourea drug isoxyl on Mycobacterium tuberculosis.
Phetsuksiri B, Jackson M, Scherman H, McNeil M, Besra GS, Baulard AR, Slayden RA, DeBarber AE, Barry CE 3rd, Baird MS, Crick DC, Brennan PJ. Phetsuksiri B, et al. Among authors: baulard ar. J Biol Chem. 2003 Dec 26;278(52):53123-30. doi: 10.1074/jbc.M311209200. Epub 2003 Oct 14. J Biol Chem. 2003. PMID: 14559907 Free PMC article.
Insights into mechanisms of induction and ligands recognition in the transcriptional repressor EthR from Mycobacterium tuberculosis.
Frénois F, Baulard AR, Villeret V. Frénois F, et al. Among authors: baulard ar. Tuberculosis (Edinb). 2006 Mar;86(2):110-4. doi: 10.1016/j.tube.2005.07.005. Epub 2005 Oct 21. Tuberculosis (Edinb). 2006. PMID: 16243584 Review.
Two EthR crystal structures have been reported recently, either in a ligand-bound (Frenois F, Engohang-Ndong J, Locht C, Baulard AR, Villeret V. Mol Cell 2004; 16: 301-7) or in a presumed apo conformation (Dover LG, Corsino PE, Daniels IR, Cocklin SL, Tatituri V, Be …
Two EthR crystal structures have been reported recently, either in a ligand-bound (Frenois F, Engohang-Ndong J, Locht C, Baulard A …
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.
77 results