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Items: 1 to 20 of 101

1.

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.

ACS Chem Biol. 2017 May 19;12(5):1390-1396. doi: 10.1021/acschembio.7b00091. Epub 2017 Apr 5.

2.

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis.

Flipo M, Willand N, Lecat-Guillet N, Hounsou C, Desroses M, Leroux F, Lens Z, Villeret V, Wohlkönig A, Wintjens R, Christophe T, Kyoung Jeon H, Locht C, Brodin P, Baulard AR, Déprez B.

J Med Chem. 2012 Jul 26;55(14):6391-402. doi: 10.1021/jm300377g. Epub 2012 Jul 17.

PMID:
22738293
3.

A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters.

Nikiforov PO, Surade S, Blaszczyk M, Delorme V, Brodin P, Baulard AR, Blundell TL, Abell C.

Org Biomol Chem. 2016 Feb 21;14(7):2318-26. doi: 10.1039/c5ob02630j. Epub 2016 Jan 25.

4.

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.

J Med Chem. 2012 Jan 12;55(1):68-83. doi: 10.1021/jm200825u. Epub 2011 Dec 6.

PMID:
22098589
5.

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.

Nat Med. 2009 May;15(5):537-44. doi: 10.1038/nm.1950. Epub 2009 May 3.

PMID:
19412174
6.

EthR, a repressor of the TetR/CamR family implicated in ethionamide resistance in mycobacteria, octamerizes cooperatively on its operator.

Engohang-Ndong J, Baillat D, Aumercier M, Bellefontaine F, Besra GS, Locht C, Baulard AR.

Mol Microbiol. 2004 Jan;51(1):175-88.

7.

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.

J Med Chem. 2011 Apr 28;54(8):2994-3010. doi: 10.1021/jm200076a. Epub 2011 Apr 1.

PMID:
21417236
8.

New active leads for tuberculosis booster drugs by structure-based drug discovery.

Tatum NJ, Liebeschuetz JW, Cole JC, Frita R, Herledan A, Baulard AR, Willand N, Pohl E.

Org Biomol Chem. 2017 Dec 13;15(48):10245-10255. doi: 10.1039/c7ob00910k.

PMID:
29182187
9.

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.

J Med Chem. 2014 Jun 12;57(11):4876-88. doi: 10.1021/jm500422b. Epub 2014 May 28.

PMID:
24818704
10.

Insights into mechanisms of induction and ligands recognition in the transcriptional repressor EthR from Mycobacterium tuberculosis.

Frénois F, Baulard AR, Villeret V.

Tuberculosis (Edinb). 2006 Mar;86(2):110-4. Epub 2005 Oct 21. Review.

PMID:
16243584
11.

Phenylethyl butyrate enhances the potency of second-line drugs against clinical isolates of Mycobacterium tuberculosis.

Grau T, Selchow P, Tigges M, Burri R, Gitzinger M, Böttger EC, Fussenegger M, Sander P.

Antimicrob Agents Chemother. 2012 Feb;56(2):1142-5. doi: 10.1128/AAC.05649-11. Epub 2011 Nov 21.

12.

Crystal structure of the TetR/CamR family repressor Mycobacterium tuberculosis EthR implicated in ethionamide resistance.

Dover LG, Corsino PE, Daniels IR, Cocklin SL, Tatituri V, Besra GS, Fütterer K.

J Mol Biol. 2004 Jul 23;340(5):1095-105.

PMID:
15236969
13.

Analogues of ethionamide, a drug used for multidrug-resistant tuberculosis, exhibit potent inhibition of tyrosinase.

Choi J, Park SJ, Jee JG.

Eur J Med Chem. 2015 Dec 1;106:157-66. doi: 10.1016/j.ejmech.2015.10.033. Epub 2015 Oct 19.

PMID:
26544630
14.

Structural and docking studies of potent ethionamide boosters.

Tatum NJ, Villemagne B, Willand N, Deprez B, Liebeschuetz JW, Baulard AR, Pohl E.

Acta Crystallogr C. 2013 Nov;69(Pt 11):1243-50. doi: 10.1107/S0108270113028126. Epub 2013 Oct 24.

PMID:
24192167
15.

The Mycobacterium tuberculosis transcriptional repressor EthR is negatively regulated by Serine/Threonine phosphorylation.

Leiba J, Carrère-Kremer S, Blondiaux N, Dimala MM, Wohlkönig A, Baulard A, Kremer L, Molle V.

Biochem Biophys Res Commun. 2014 Apr 18;446(4):1132-8. doi: 10.1016/j.bbrc.2014.03.074. Epub 2014 Mar 22.

PMID:
24667600
16.

Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands.

Crauste C, Willand N, Villemagne B, Flipo M, Willery E, Carette X, Dimala MM, Drucbert AS, Danze PM, Deprez B, Baulard AR.

Anal Biochem. 2014 May 1;452:54-66. doi: 10.1016/j.ab.2014.02.011. Epub 2014 Feb 20.

PMID:
24561027
17.

Genotypic Analysis of Genes Associated with Independent Resistance and Cross-Resistance to Isoniazid and Ethionamide in Mycobacterium tuberculosis Clinical Isolates.

Rueda J, Realpe T, Mejia GI, Zapata E, Rozo JC, Ferro BE, Robledo J.

Antimicrob Agents Chemother. 2015 Dec;59(12):7805-10. doi: 10.1128/AAC.01028-15. Epub 2015 Sep 14.

18.

Metabolism of the antituberculosis drug ethionamide.

Vale N, Gomes P, Santos HA.

Curr Drug Metab. 2013 Jan;14(1):151-8. Review.

PMID:
23215813
19.

Preparation and biological evaluation of ethionamide-mesoporous silicon nanoparticles against Mycobacterium tuberculosis.

Vale N, Correia A, Silva S, Figueiredo P, Mäkilä E, Salonen J, Hirvonen J, Pedrosa J, Santos HA, Fraga A.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):403-405. doi: 10.1016/j.bmcl.2016.12.060. Epub 2016 Dec 26.

PMID:
28057421
20.

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.

Science. 2017 Mar 17;355(6330):1206-1211. doi: 10.1126/science.aag1006. Epub 2017 Mar 16.

PMID:
28302858

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