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Items: 1 to 50 of 76

1.

Implementation of chlorhexidine gluconate bathing to reduce HAIs.

DePrez B, Schreeder C, Davidson S.

Nurs Manage. 2019 Nov;50(11):13-17. doi: 10.1097/01.NUMA.0000602824.95678.0a.

PMID:
31688541
2.

The use or generation of biomedical data and existing medicines to discover and establish new treatments for patients with rare diseases - recommendations of the IRDiRC Data Mining and Repurposing Task Force.

Southall NT, Natarajan M, Lau LPL, Jonker AH, Deprez B, Guilliams T, Hunter L, Rademaker CM, Hivert V, Ardigò D; IRDiRC Data Mining and Repurposing Task Force.

Orphanet J Rare Dis. 2019 Oct 15;14(1):225. doi: 10.1186/s13023-019-1193-3.

3.

High-Throughput DNA Plasmid Multiplexing and Transfection Using Acoustic Nanodispensing Technology.

Colin B, Rocq N, Deprez B, Couturier C.

J Vis Exp. 2019 Aug 8;(150). doi: 10.3791/59570.

PMID:
31449254
4.

Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening.

Leroux F, Bosc D, Beghyn T, Hermant P, Warenghem S, Landry V, Pottiez V, Guillaume V, Charton J, Herledan A, Urata S, Liang W, Sheng L, Tang WJ, Deprez B, Deprez-Poulain R.

Eur J Med Chem. 2019 Oct 1;179:557-566. doi: 10.1016/j.ejmech.2019.06.057. Epub 2019 Jun 24.

PMID:
31276900
5.

BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr348 phosphorylation.

Sartori M, Mendes T, Desai S, Lasorsa A, Herledan A, Malmanche N, Mäkinen P, Marttinen M, Malki I, Chapuis J, Flaig A, Vreulx AC, Ciancia M, Amouyel P, Leroux F, Déprez B, Cantrelle FX, Maréchal D, Pradier L, Hiltunen M, Landrieu I, Kilinc D, Herault Y, Laporte J, Lambert JC.

Acta Neuropathol. 2019 Oct;138(4):631-652. doi: 10.1007/s00401-019-02017-9. Epub 2019 May 7.

6.

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
7.

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
8.

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
9.

High-Throughput DNA Plasmid Transfection Using Acoustic Droplet Ejection Technology.

Colin B, Deprez B, Couturier C.

SLAS Discov. 2019 Apr;24(4):492-500. doi: 10.1177/2472555218803064. Epub 2018 Oct 5.

PMID:
30290128
10.

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
11.

Development and implementation of a cell-based assay to discover agonists of the nuclear receptor REV-ERBα.

Hering Y, Berthier A, Duez H, Lefebvre P, Deprez B, Gribbon P, Wolf M, Reinshagen J, Halley F, Hannemann J, Böger R, Staels B, Gul S.

J Biol Methods. 2018 Jun 25;5(3):e94. doi: 10.14440/jbm.2018.244. eCollection 2018.

12.

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.

13.

Ensemble cryoEM elucidates the mechanism of insulin capture and degradation by human insulin degrading enzyme.

Zhang Z, Liang WG, Bailey LJ, Tan YZ, Wei H, Wang A, Farcasanu M, Woods VA, McCord LA, Lee D, Shang W, Deprez-Poulain R, Deprez B, Liu DR, Koide A, Koide S, Kossiakoff AA, Li S, Carragher B, Potter CS, Tang WJ.

Elife. 2018 Mar 29;7. pii: e33572. doi: 10.7554/eLife.33572.

14.

Daytime variation of perioperative myocardial injury in cardiac surgery and its prevention by Rev-Erbα antagonism: a single-centre propensity-matched cohort study and a randomised study.

Montaigne D, Marechal X, Modine T, Coisne A, Mouton S, Fayad G, Ninni S, Klein C, Ortmans S, Seunes C, Potelle C, Berthier A, Gheeraert C, Piveteau C, Deprez R, Eeckhoute J, Duez H, Lacroix D, Deprez B, Jegou B, Koussa M, Edme JL, Lefebvre P, Staels B.

Lancet. 2018 Jan 6;391(10115):59-69. doi: 10.1016/S0140-6736(17)32132-3. Epub 2017 Oct 26.

PMID:
29107324
15.

Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox.

Hermant P, Bosc D, Piveteau C, Gealageas R, Lam B, Ronco C, Roignant M, Tolojanahary H, Jean L, Renard PY, Lemdani M, Bourotte M, Herledan A, Bedart C, Biela A, Leroux F, Deprez B, Deprez-Poulain R.

J Med Chem. 2017 Nov 9;60(21):9067-9089. doi: 10.1021/acs.jmedchem.7b01444. Epub 2017 Oct 24.

PMID:
28985084
16.

Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis.

Boiteau JG, Ouvry G, Arlabosse JM, Astri S, Beillard A, Bhurruth-Alcor Y, Bonnary L, Bouix-Peter C, Bouquet K, Bourotte M, Cardinaud I, Comino C, Deprez B, Duvert D, Féret A, Hacini-Rachinel F, Harris CS, Luzy AP, Mathieu A, Millois C, Orsini N, Pascau J, Pinto A, Piwnica D, Polge G, Reitz A, Reversé K, Rodeville N, Rossio P, Spiesse D, Tabet S, Taquet N, Tomas L, Vial E, Hennequin LF.

Bioorg Med Chem. 2018 Feb 15;26(4):945-956. doi: 10.1016/j.bmc.2017.07.054. Epub 2017 Aug 2.

PMID:
28818461
17.

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.

18.

Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance.

Lasalle M, Hoguet V, Hennuyer N, Leroux F, Piveteau C, Belloy L, Lestavel S, Vallez E, Dorchies E, Duplan I, Sevin E, Culot M, Gosselet F, Boulahjar R, Herledan A, Staels B, Deprez B, Tailleux A, Charton J.

J Med Chem. 2017 May 25;60(10):4185-4211. doi: 10.1021/acs.jmedchem.6b01873. Epub 2017 May 5.

19.

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
20.

Identification of novel TACE inhibitors compatible with topical application.

Ouvry G, Berton Y, Bhurruth-Alcor Y, Bonnary L, Bouix-Peter C, Bouquet K, Bourotte M, Chambon S, Comino C, Deprez B, Duvert D, Duvert G, Hacini-Rachinel F, Harris CS, Luzy AP, Mathieu A, Millois C, Pascau J, Pinto A, Polge G, Reitz A, Reversé K, Rosignoli C, Taquet N, Hennequin LF.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1848-1853. doi: 10.1016/j.bmcl.2017.02.035. Epub 2017 Feb 20.

PMID:
28274635
21.

Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism.

Chapuis J, Flaig A, Grenier-Boley B, Eysert F, Pottiez V, Deloison G, Vandeputte A, Ayral AM, Mendes T, Desai S, Goate AM, Kauwe JSK, Leroux F, Herledan A, Demiautte F, Bauer C, Checler F, Petersen RC, Blennow K, Zetterberg H, Minthon L, Van Deerlin VM, Lee VM, Shaw LM, Trojanowski JQ, Albert M, Moghekar A, O'Brien R, Peskind ER, Malmanche N, Schellenberg GD, Dourlen P, Song OR, Cruchaga C, Amouyel P, Deprez B, Brodin P, Lambert JC; ADGC, Alzheimer’s Disease Neuroimaging Initiative.

Acta Neuropathol. 2017 Jun;133(6):955-966. doi: 10.1007/s00401-016-1652-z. Epub 2016 Dec 8.

22.

ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease.

Letronne F, Laumet G, Ayral AM, Chapuis J, Demiautte F, Laga M, Vandenberghe ME, Malmanche N, Leroux F, Eysert F, Sottejeau Y, Chami L, Flaig A, Bauer C, Dourlen P, Lesaffre M, Delay C, Huot L, Dumont J, Werkmeister E, Lafont F, Mendes T, Hansmannel F, Dermaut B, Deprez B, Hérard AS, Dhenain M, Souedet N, Pasquier F, Tulasne D, Berr C, Hauw JJ, Lemoine Y, Amouyel P, Mann D, Déprez R, Checler F, Hot D, Delzescaux T, Gevaert K, Lambert JC.

EBioMedicine. 2016 Jul;9:278-292. doi: 10.1016/j.ebiom.2016.06.002. Epub 2016 Jun 2.

23.

Kinetic target-guided synthesis in drug discovery and chemical biology: a comprehensive facts and figures survey.

Bosc D, Jakhlal J, Deprez B, Deprez-Poulain R.

Future Med Chem. 2016;8(4):381-404. doi: 10.4155/fmc-2015-0007. Epub 2016 Feb 15. Review.

24.

Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice.

Deprez-Poulain R, Hennuyer N, Bosc D, Liang WG, Enée E, Marechal X, Charton J, Totobenazara J, Berte G, Jahklal J, Verdelet T, Dumont J, Dassonneville S, Woitrain E, Gauriot M, Paquet C, Duplan I, Hermant P, Cantrelle FX, Sevin E, Culot M, Landry V, Herledan A, Piveteau C, Lippens G, Leroux F, Tang WJ, van Endert P, Staels B, Deprez B.

Nat Commun. 2015 Sep 23;6:8250. doi: 10.1038/ncomms9250.

25.

Characterization of monoclonal antibodies by a fast and easy liquid chromatography-mass spectrometry time-of-flight analysis on culture supernatant.

Henninot A, Terrier A, Charton J, Urbain R, Fontayne A, Deprez B, Beghyn T.

Anal Biochem. 2015 Dec 15;491:52-4. doi: 10.1016/j.ab.2015.08.006. Epub 2015 Aug 22.

PMID:
26302360
26.

The Bile Acid Chenodeoxycholic Acid Increases Human Brown Adipose Tissue Activity.

Broeders EP, Nascimento EB, Havekes B, Brans B, Roumans KH, Tailleux A, Schaart G, Kouach M, Charton J, Deprez B, Bouvy ND, Mottaghy F, Staels B, van Marken Lichtenbelt WD, Schrauwen P.

Cell Metab. 2015 Sep 1;22(3):418-26. doi: 10.1016/j.cmet.2015.07.002. Epub 2015 Jul 30.

27.

Inhibition of the glucose transporter SGLT2 with dapagliflozin in pancreatic alpha cells triggers glucagon secretion.

Bonner C, Kerr-Conte J, Gmyr V, Queniat G, Moerman E, Thévenet J, Beaucamps C, Delalleau N, Popescu I, Malaisse WJ, Sener A, Deprez B, Abderrahmani A, Staels B, Pattou F.

Nat Med. 2015 May;21(5):512-7. doi: 10.1038/nm.3828. Epub 2015 Apr 20.

PMID:
25894829
28.

Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme.

Charton J, Gauriot M, Totobenazara J, Hennuyer N, Dumont J, Bosc D, Marechal X, Elbakali J, Herledan A, Wen X, Ronco C, Gras-Masse H, Heninot A, Pottiez V, Landry V, Staels B, Liang WG, Leroux F, Tang WJ, Deprez B, Deprez-Poulain R.

Eur J Med Chem. 2015 Jan 27;90:547-67. doi: 10.1016/j.ejmech.2014.12.005. Epub 2014 Dec 4.

29.

In vivo efficacy of microbiota-sensitive coatings for colon targeting: a promising tool for IBD therapy.

Karrout Y, Dubuquoy L, Piveteau C, Siepmann F, Moussa E, Wils D, Beghyn T, Neut C, Flament MP, Guerin-Deremaux L, Dubreuil L, Deprez B, Desreumaux P, Siepmann J.

J Control Release. 2015 Jan 10;197:121-30. doi: 10.1016/j.jconrel.2014.11.006. Epub 2014 Nov 10.

PMID:
25445696
30.

Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis.

El Bakali J, Gras-Masse H, Maingot L, Deprez B, Dumont J, Leroux F, Deprez-Poulain R.

Future Med Chem. 2014;6(12):1399-412. doi: 10.4155/fmc.14.84. Review.

PMID:
25329196
31.

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
32.

Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737.

Mathieu AL, Sperandio O, Pottiez V, Balzarin S, Herlédan A, Elkaïm JO, Fogeron ML, Piveteau C, Dassonneville S, Deprez B, Villoutreix BO, Bonnefoy N, Leroux F.

J Biomol Screen. 2014 Aug;19(7):1035-46. doi: 10.1177/1087057114534070. Epub 2014 May 8.

PMID:
24809353
33.

Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis.

Charton J, Gauriot M, Guo Q, Hennuyer N, Marechal X, Dumont J, Hamdane M, Pottiez V, Landry V, Sperandio O, Flipo M, Buee L, Staels B, Leroux F, Tang WJ, Deprez B, Deprez-Poulain R.

Eur J Med Chem. 2014 May 22;79:184-93. doi: 10.1016/j.ejmech.2014.04.009. Epub 2014 Apr 4.

34.

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
35.

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
36.

Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group.

Maingot L, Elbakali J, Dumont J, Bosc D, Cousaert N, Urban A, Deglane G, Villoutreix B, Nagase H, Sperandio O, Leroux F, Deprez B, Deprez-Poulain R.

Eur J Med Chem. 2013 Nov;69:244-61. doi: 10.1016/j.ejmech.2013.08.027. Epub 2013 Aug 30.

PMID:
24044937
37.

Structure-activity relationships and blood distribution of antiplasmodial aminopeptidase-1 inhibitors.

Deprez-Poulain R, Flipo M, Piveteau C, Leroux F, Dassonneville S, Florent I, Maes L, Cos P, Deprez B.

J Med Chem. 2012 Dec 27;55(24):10909-17. doi: 10.1021/jm301506h. Epub 2012 Dec 5.

PMID:
23176597
38.

Setting Up a Bioluminescence Resonance Energy Transfer High throughput Screening Assay to Search for Protein/Protein Interaction Inhibitors in Mammalian Cells.

Couturier C, Deprez B.

Front Endocrinol (Lausanne). 2012 Sep 11;3:100. doi: 10.3389/fendo.2012.00100. eCollection 2012.

39.

Rescue of nonsense mutations by amlexanox in human cells.

Gonzalez-Hilarion S, Beghyn T, Jia J, Debreuck N, Berte G, Mamchaoui K, Mouly V, Gruenert DC, Déprez B, Lejeune F.

Orphanet J Rare Dis. 2012 Aug 31;7:58. doi: 10.1186/1750-1172-7-58.

40.

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
41.

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
42.

Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds.

Beghyn TB, Charton J, Leroux F, Henninot A, Reboule I, Cos P, Maes L, Deprez B.

J Med Chem. 2012 Feb 9;55(3):1274-86. doi: 10.1021/jm201422e. Epub 2012 Jan 24.

PMID:
22204607
43.

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.

44.

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
45.

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
46.

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
47.

Drug to genome to drug: discovery of new antiplasmodial compounds.

Beghyn TB, Charton J, Leroux F, Laconde G, Bourin A, Cos P, Maes L, Deprez B.

J Med Chem. 2011 May 12;54(9):3222-40. doi: 10.1021/jm1014617. Epub 2011 Apr 19.

PMID:
21504142
48.

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
49.

New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold.

Maingot L, Leroux F, Landry V, Dumont J, Nagase H, Villoutreix B, Sperandio O, Deprez-Poulain R, Deprez B.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6213-6. doi: 10.1016/j.bmcl.2010.08.108. Epub 2010 Aug 27.

PMID:
20846863
50.

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

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