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Items: 26

1.

A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation.

Pastor A, Machelart A, Li X, Willand N, Baulard A, Brodin P, Gref R, Desmaële D.

Org Biomol Chem. 2019 May 28;17(20):5129-5137. doi: 10.1039/c9ob00680j. Epub 2019 May 10.

PMID:
31073555
2.

Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis.

Machelart A, Salzano G, Li X, Demars A, Debrie AS, Menendez-Miranda M, Pancani E, Jouny S, Hoffmann E, Deboosere N, Belhaouane I, Rouanet C, Simar S, Talahari S, Giannini V, Villemagne B, Flipo M, Brosch R, Nesslany F, Deprez B, Muraille E, Locht C, Baulard AR, Willand N, Majlessi L, Gref R, Brodin P.

ACS Nano. 2019 Apr 23;13(4):3992-4007. doi: 10.1021/acsnano.8b07902. Epub 2019 Mar 8.

PMID:
30822386
3.

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.

Eur J Med Chem. 2019 Apr 1;167:426-438. doi: 10.1016/j.ejmech.2019.02.023. Epub 2019 Feb 10.

PMID:
30784877
4.

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.

Biochim Biophys Acta Proteins Proteom. 2019 Mar;1867(3):248-258. doi: 10.1016/j.bbapap.2018.12.003. Epub 2018 Dec 13.

PMID:
30553830
5.

Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis.

Prieri M, Frita R, Probst N, Sournia-Saquet A, Bourotte M, Déprez B, Baulard AR, Willand N.

Eur J Med Chem. 2018 Nov 5;159:35-46. doi: 10.1016/j.ejmech.2018.09.038. Epub 2018 Sep 20.

PMID:
30268015
6.

Publisher Correction: Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles.

Costa-Gouveia J, Pancani E, Jouny S, Machelart A, Delorme V, Salzano G, Iantomasi R, Piveteau C, Queval CJ, Song OR, Flipo M, Deprez B, Saint-André JP, Hureaux J, Majlessi L, Willand N, Baulard A, Brodin P, Gref R.

Sci Rep. 2018 May 10;8(1):7596. doi: 10.1038/s41598-018-25177-2.

7.

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
8.

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles.

Costa-Gouveia J, Pancani E, Jouny S, Machelart A, Delorme V, Salzano G, Iantomasi R, Piveteau C, Queval CJ, Song OR, Flipo M, Deprez B, Saint-André JP, Hureaux J, Majlessi L, Willand N, Baulard A, Brodin P, Gref R.

Sci Rep. 2017 Jul 14;7(1):5390. doi: 10.1038/s41598-017-05453-3. Erratum in: Sci Rep. 2018 May 10;8(1):7596.

9.

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
10.

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
11.

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
12.

Towards explaining the health impacts of residential energy efficiency interventions - A realist review. Part 1: Pathways.

Willand N, Ridley I, Maller C.

Soc Sci Med. 2015 May;133:191-201. doi: 10.1016/j.socscimed.2015.02.005. Epub 2015 Feb 11. Review.

PMID:
25687402
13.

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
14.

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
15.

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
16.

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
17.

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
18.

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.

19.

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
20.

Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation.

Deprez-Poulain R, Cousaert N, Toto P, Willand N, Deprez B.

Eur J Med Chem. 2011 Sep;46(9):3867-76. doi: 10.1016/j.ejmech.2011.05.056. Epub 2011 May 30.

PMID:
21683484
21.

MALDI imaging techniques dedicated to drug-distribution studies.

Bonnel D, Legouffe R, Willand N, Baulard A, Hamm G, Deprez B, Stauber J.

Bioanalysis. 2011 Jun;3(12):1399-406. doi: 10.4155/bio.11.88.

PMID:
21679033
22.

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
23.

Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator.

Willand N, Desroses M, Toto P, Dirié B, Lens Z, Villeret V, Rucktooa P, Locht C, Baulard A, Deprez B.

ACS Chem Biol. 2010 Nov 19;5(11):1007-13. doi: 10.1021/cb100177g.

PMID:
20704273
24.

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
25.

Natural compounds: leads or ideas? Bioinspired molecules for drug discovery.

Beghyn T, Deprez-Poulain R, Willand N, Folleas B, Deprez B.

Chem Biol Drug Des. 2008 Jul;72(1):3-15. doi: 10.1111/j.1747-0285.2008.00673.x. Epub 2008 Jun 11.

PMID:
18554253
26.

[Neuraminidase inhibitors and risk of H5N1 influenza].

Gras-Masse H, Willand N.

Ann Pharm Fr. 2007 Jan;65(1):50-7. Review. French.

PMID:
17299351

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