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Items: 36

1.

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
2.

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs.

Salzano G, Wankar J, Ottani S, Villemagne B, Baulard AR, Willand N, Brodin P, Manet I, Gref R.

Int J Pharm. 2017 Oct 15;531(2):577-587. doi: 10.1016/j.ijpharm.2017.05.030. Epub 2017 May 15.

PMID:
28522424
3.

Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2.

Wohlkönig A, Remaut H, Moune M, Tanina A, Meyer F, Desroses M, Steyaert J, Willand N, Baulard AR, Wintjens R.

Biochem Biophys Res Commun. 2017 May 27;487(2):403-408. doi: 10.1016/j.bbrc.2017.04.074. Epub 2017 Apr 14.

PMID:
28416386
4.

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.

5.

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
6.

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.

7.

Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG.

Mori G, Chiarelli LR, Esposito M, Makarov V, Bellinzoni M, Hartkoorn RC, Degiacomi G, Boldrin F, Ekins S, de Jesus Lopes Ribeiro AL, Marino LB, Centárová I, Svetlíková Z, Blaško J, Kazakova E, Lepioshkin A, Barilone N, Zanoni G, Porta A, Fondi M, Fani R, Baulard AR, Mikušová K, Alzari PM, Manganelli R, de Carvalho LP, Riccardi G, Cole ST, Pasca MR.

Chem Biol. 2015 Jul 23;22(7):917-27. doi: 10.1016/j.chembiol.2015.05.016. Epub 2015 Jun 18.

8.

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
9.

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
10.

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
11.

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
12.

Tuberculosis: the drug development pipeline at a glance.

Villemagne B, Crauste C, Flipo M, Baulard AR, Déprez B, Willand N.

Eur J Med Chem. 2012 May;51:1-16. doi: 10.1016/j.ejmech.2012.02.033. Epub 2012 Feb 25. Review.

PMID:
22421275
13.

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.

Nucleic Acids Res. 2012 Apr;40(7):3018-30. doi: 10.1093/nar/gkr1113. Epub 2011 Dec 9.

14.

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
15.

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
16.

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
17.

Molecular mapping of lipoarabinomannans on mycobacteria.

Verbelen C, Christiaens N, Alsteens D, Dupres V, Baulard AR, Dufrêne YF.

Langmuir. 2009 Apr 21;25(8):4324-7. doi: 10.1021/la900302a.

PMID:
19278203
18.

Organization of the mycobacterial cell wall: a nanoscale view.

Alsteens D, Verbelen C, Dague E, Raze D, Baulard AR, Dufrêne YF.

Pflugers Arch. 2008 Apr;456(1):117-25. Epub 2007 Nov 28.

PMID:
18043940
19.

Direct measurement of hydrophobic forces on cell surfaces using AFM.

Alsteens D, Dague E, Rouxhet PG, Baulard AR, Dufrêne YF.

Langmuir. 2007 Nov 20;23(24):11977-9. Epub 2007 Oct 17.

PMID:
17941657
20.

Antibody response in pulmonary tuberculosis against recombinant 27kDa (MPT51, Rv3803c) protein of Mycobacterium tuberculosis.

Bethunaickan R, Baulard AR, Locht C, Raja A.

Scand J Infect Dis. 2007;39(10):867-74.

PMID:
17852894
21.

Chemical force microscopy of single live cells.

Dague E, Alsteens D, Latgé JP, Verbelen C, Raze D, Baulard AR, Dufrêne YF.

Nano Lett. 2007 Oct;7(10):3026-30. Epub 2007 Sep 13.

PMID:
17850167
22.

Ethambutol-induced alterations in Mycobacterium bovis BCG imaged by atomic force microscopy.

Verbelen C, Dupres V, Menozzi FD, Raze D, Baulard AR, Hols P, Dufrêne YF.

FEMS Microbiol Lett. 2006 Nov;264(2):192-7.

23.

Selective intracellular accumulation of the major metabolite issued from the activation of the prodrug ethionamide in mycobacteria.

Hanoulle X, Wieruszeski JM, Rousselot-Pailley P, Landrieu I, Locht C, Lippens G, Baulard AR.

J Antimicrob Chemother. 2006 Oct;58(4):768-72. Epub 2006 Aug 8.

PMID:
16895935
24.

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
25.

Monitoring of the ethionamide pro-drug activation in mycobacteria by (1)H high resolution magic angle spinning NMR.

Hanoulle X, Wieruszeski JM, Rousselot-Pailley P, Landrieu I, Baulard AR, Lippens G.

Biochem Biophys Res Commun. 2005 Jun 3;331(2):452-8.

PMID:
15850780
26.

[Doping in the peloton of antituberculosis drugs].

Baulard AR.

Med Sci (Paris). 2005 Apr;21(4):351-3. French. No abstract available.

27.

Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis.

Frénois F, Engohang-Ndong J, Locht C, Baulard AR, Villeret V.

Mol Cell. 2004 Oct 22;16(2):301-7.

28.

Cloning, expression, and purification of the 27 kDa (MPT51, Rv3803c) protein of Mycobacterium tuberculosis.

Ramalingam B, Baulard AR, Locht C, Narayanan PR, Raja A.

Protein Expr Purif. 2004 Jul;36(1):53-60.

PMID:
15177284
29.

Identification of a novel class of omega,E,E-farnesyl diphosphate synthase from Mycobacterium tuberculosis.

Dhiman RK, Schulbach MC, Mahapatra S, Baulard AR, Vissa V, Brennan PJ, Crick DC.

J Lipid Res. 2004 Jun;45(6):1140-7. Epub 2004 Apr 1.

30.

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.

31.

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.

J Biol Chem. 2003 Dec 26;278(52):53123-30. Epub 2003 Oct 14.

32.
33.

Ppm1, a novel polyprenol monophosphomannose synthase from Mycobacterium tuberculosis.

Gurcha SS, Baulard AR, Kremer L, Locht C, Moody DB, Muhlecker W, Costello CE, Crick DC, Brennan PJ, Besra GS.

Biochem J. 2002 Jul 15;365(Pt 2):441-50.

34.

Activation of the pro-drug ethionamide is regulated in mycobacteria.

Baulard AR, Betts JC, Engohang-Ndong J, Quan S, McAdam RA, Brennan PJ, Locht C, Besra GS.

J Biol Chem. 2000 Sep 8;275(36):28326-31.

35.

Thiolactomycin and related analogues as novel anti-mycobacterial agents targeting KasA and KasB condensing enzymes in Mycobacterium tuberculosis.

Kremer L, Douglas JD, Baulard AR, Morehouse C, Guy MR, Alland D, Dover LG, Lakey JH, Jacobs WR Jr, Brennan PJ, Minnikin DE, Besra GS.

J Biol Chem. 2000 Jun 2;275(22):16857-64.

36.

Antimycobacterial activities of isoxyl and new derivatives through the inhibition of mycolic acid synthesis.

Phetsuksiri B, Baulard AR, Cooper AM, Minnikin DE, Douglas JD, Besra GS, Brennan PJ.

Antimicrob Agents Chemother. 1999 May;43(5):1042-51.

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