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Items: 35

1.

Antibiotic prophylaxis after open fractures needs to be (re)assessed.

Roxane M, Raymond R, Pascal B, Christophe T, Johan C.

Clin Microbiol Infect. 2019 Oct 9. pii: S1198-743X(19)30526-9. doi: 10.1016/j.cmi.2019.09.025. [Epub ahead of print] No abstract available.

PMID:
31605744
2.

Identification of GLPG/ABBV-2737, a Novel Class of Corrector, Which Exerts Functional Synergy With Other CFTR Modulators.

de Wilde G, Gees M, Musch S, Verdonck K, Jans M, Wesse AS, Singh AK, Hwang TC, Christophe T, Pizzonero M, Van der Plas S, Desroy N, Cowart M, Stouten P, Nelles L, Conrath K.

Front Pharmacol. 2019 May 9;10:514. doi: 10.3389/fphar.2019.00514. eCollection 2019.

3.

Correction to Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2- a]pyridine Series of Autotaxin Inhibitors.

Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B.

J Med Chem. 2018 May 10;61(9):4270. doi: 10.1021/acs.jmedchem.8b00579. Epub 2018 Apr 19. No abstract available.

PMID:
29672037
4.

Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Channels to a High Extent.

Van der Plas SE, Kelgtermans H, De Munck T, Martina SLX, Dropsit S, Quinton E, De Blieck A, Joannesse C, Tomaskovic L, Jans M, Christophe T, van der Aar E, Borgonovi M, Nelles L, Gees M, Stouten P, Van Der Schueren J, Mammoliti O, Conrath K, Andrews M.

J Med Chem. 2018 Feb 22;61(4):1425-1435. doi: 10.1021/acs.jmedchem.7b01288. Epub 2018 Jan 10.

PMID:
29148763
5.

Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.

Joncour A, Desroy N, Housseman C, Bock X, Bienvenu N, Cherel L, Labeguere V, Peixoto C, Annoot D, Lepissier L, Heiermann J, Hengeveld WJ, Pilzak G, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Galien R, David C, Vandervoort N, Christophe T, Conrath K, Jans M, Wohlkonig A, Soror S, Steyaert J, Touitou R, Fleury D, Vercheval L, Mollat P, Triballeau N, van der Aar E, Brys R, Heckmann B.

J Med Chem. 2017 Sep 14;60(17):7371-7392. doi: 10.1021/acs.jmedchem.7b00647. Epub 2017 Aug 18. Erratum in: J Med Chem. 2018 May 10;61(9):4270.

PMID:
28731719
6.

Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis.

Desroy N, Housseman C, Bock X, Joncour A, Bienvenu N, Cherel L, Labeguere V, Rondet E, Peixoto C, Grassot JM, Picolet O, Annoot D, Triballeau N, Monjardet A, Wakselman E, Roncoroni V, Le Tallec S, Blanque R, Cottereaux C, Vandervoort N, Christophe T, Mollat P, Lamers M, Auberval M, Hrvacic B, Ralic J, Oste L, van der Aar E, Brys R, Heckmann B.

J Med Chem. 2017 May 11;60(9):3580-3590. doi: 10.1021/acs.jmedchem.7b00032. Epub 2017 May 1.

PMID:
28414242
7.

Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic.

Pizzonero M, Dupont S, Babel M, Beaumont S, Bienvenu N, Blanqué R, Cherel L, Christophe T, Crescenzi B, De Lemos E, Delerive P, Deprez P, De Vos S, Djata F, Fletcher S, Kopiejewski S, L'Ebraly C, Lefrançois JM, Lavazais S, Manioc M, Nelles L, Oste L, Polancec D, Quénéhen V, Soulas F, Triballeau N, van der Aar EM, Vandeghinste N, Wakselman E, Brys R, Saniere L.

J Med Chem. 2014 Dec 11;57(23):10044-57. doi: 10.1021/jm5012885. Epub 2014 Dec 1.

PMID:
25380412
8.

Triazolopyridines as selective JAK1 inhibitors: from hit identification to GLPG0634.

Menet CJ, Fletcher SR, Van Lommen G, Geney R, Blanc J, Smits K, Jouannigot N, Deprez P, van der Aar EM, Clement-Lacroix P, Lepescheux L, Galien R, Vayssiere B, Nelles L, Christophe T, Brys R, Uhring M, Ciesielski F, Van Rompaey L.

J Med Chem. 2014 Nov 26;57(22):9323-42. doi: 10.1021/jm501262q. Epub 2014 Nov 17.

PMID:
25369270
9.

Mycobacterial toxin induces analgesia in buruli ulcer by targeting the angiotensin pathways.

Marion E, Song OR, Christophe T, Babonneau J, Fenistein D, Eyer J, Letournel F, Henrion D, Clere N, Paille V, Guérineau NC, Saint André JP, Gersbach P, Altmann KH, Stinear TP, Comoglio Y, Sandoz G, Preisser L, Delneste Y, Yeramian E, Marsollier L, Brodin P.

Cell. 2014 Jun 19;157(7):1565-76. doi: 10.1016/j.cell.2014.04.040.

10.

Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases.

Van Rompaey L, Galien R, van der Aar EM, Clement-Lacroix P, Nelles L, Smets B, Lepescheux L, Christophe T, Conrath K, Vandeghinste N, Vayssiere B, De Vos S, Fletcher S, Brys R, van 't Klooster G, Feyen JH, Menet C.

J Immunol. 2013 Oct 1;191(7):3568-77. doi: 10.4049/jimmunol.1201348. Epub 2013 Sep 4.

11.

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis.

Pethe K, Bifani P, Jang J, Kang S, Park S, Ahn S, Jiricek J, Jung J, Jeon HK, Cechetto J, Christophe T, Lee H, Kempf M, Jackson M, Lenaerts AJ, Pham H, Jones V, Seo MJ, Kim YM, Seo M, Seo JJ, Park D, Ko Y, Choi I, Kim R, Kim SY, Lim S, Yim SA, Nam J, Kang H, Kwon H, Oh CT, Cho Y, Jang Y, Kim J, Chua A, Tan BH, Nanjundappa MB, Rao SP, Barnes WS, Wintjens R, Walker JR, Alonso S, Lee S, Kim J, Oh S, Oh T, Nehrbass U, Han SJ, No Z, Lee J, Brodin P, Cho SN, Nam K, Kim J.

Nat Med. 2013 Sep;19(9):1157-60. doi: 10.1038/nm.3262. Epub 2013 Aug 4.

PMID:
23913123
12.

Identification of a novel sulfonamide non-nucleoside reverse transcriptase inhibitor by a phenotypic HIV-1 full replication assay.

Kim TH, Ko Y, Christophe T, Cechetto J, Kim J, Kim KA, Boese AS, Garcia JM, Fenistein D, Ju MK, Kim J, Han SJ, Kwon HJ, Brondani V, Sommer P.

PLoS One. 2013 Jul 18;8(7):e68767. doi: 10.1371/journal.pone.0068767. Print 2013.

13.

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
14.

New taxonomy and old collections: integrating DNA barcoding into the collection curation process.

Puillandre N, Bouchet P, Boisselier-Dubayle MC, Brisset J, Buge B, Castelin M, Chagnoux S, Christophe T, Corbari L, Lambourdière J, Lozouet P, Marani G, Rivasseau A, Silva N, Terryn Y, Tillier S, Utge J, Samadi S.

Mol Ecol Resour. 2012 May;12(3):396-402. doi: 10.1111/j.1755-0998.2011.03105.x. Epub 2012 Jan 4.

PMID:
22221866
15.

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
16.

High-content screening in infectious diseases.

Brodin P, Christophe T.

Curr Opin Chem Biol. 2011 Aug;15(4):534-9. doi: 10.1016/j.cbpa.2011.05.023. Epub 2011 Jun 20. Review.

PMID:
21684803
17.

High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery.

Christophe T, Ewann F, Jeon HK, Cechetto J, Brodin P.

Future Med Chem. 2010 Aug;2(8):1283-93. doi: 10.4155/fmc.10.223.

PMID:
21426019
18.

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
19.

High content phenotypic cell-based visual screen identifies Mycobacterium tuberculosis acyltrehalose-containing glycolipids involved in phagosome remodeling.

Brodin P, Poquet Y, Levillain F, Peguillet I, Larrouy-Maumus G, Gilleron M, Ewann F, Christophe T, Fenistein D, Jang J, Jang MS, Park SJ, Rauzier J, Carralot JP, Shrimpton R, Genovesio A, Gonzalo-Asensio JA, Puzo G, Martin C, Brosch R, Stewart GR, Gicquel B, Neyrolles O.

PLoS Pathog. 2010 Sep 9;6(9):e1001100. doi: 10.1371/journal.ppat.1001100.

20.

Antileishmanial high-throughput drug screening reveals drug candidates with new scaffolds.

Siqueira-Neto JL, Song OR, Oh H, Sohn JH, Yang G, Nam J, Jang J, Cechetto J, Lee CB, Moon S, Genovesio A, Chatelain E, Christophe T, Freitas-Junior LH.

PLoS Negl Trop Dis. 2010 May 4;4(5):e675. doi: 10.1371/journal.pntd.0000675.

21.

Confocal-based method for quantification of diffusion kinetics in microwell plates and its application for identifying a rapid mixing method for high-content/throughput screening.

Song OR, Kim TH, Perrodon X, Lee C, Jeon HK, Seghiri Z, Kwon HJ, Cechetto J, Christophe T.

J Biomol Screen. 2010 Feb;15(2):138-47. doi: 10.1177/1087057109357787. Epub 2010 Jan 19.

PMID:
20086214
22.

High content screening identifies decaprenyl-phosphoribose 2' epimerase as a target for intracellular antimycobacterial inhibitors.

Christophe T, Jackson M, Jeon HK, Fenistein D, Contreras-Dominguez M, Kim J, Genovesio A, Carralot JP, Ewann F, Kim EH, Lee SY, Kang S, Seo MJ, Park EJ, Skovierová H, Pham H, Riccardi G, Nam JY, Marsollier L, Kempf M, Joly-Guillou ML, Oh T, Shin WK, No Z, Nehrbass U, Brosch R, Cole ST, Brodin P.

PLoS Pathog. 2009 Oct;5(10):e1000645. doi: 10.1371/journal.ppat.1000645. Epub 2009 Oct 30.

23.

Mediodorsal thalamic lesions block the stress-induced inversion of serial memory retrieval pattern in mice.

Chauveau F, Piérard C, Corio M, Célérier A, Christophe T, Vouimba RM, Guillou JL, Béracochéa D.

Behav Brain Res. 2009 Nov 5;203(2):270-8. doi: 10.1016/j.bbr.2009.05.014. Epub 2009 May 21.

PMID:
19464320
24.

Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis.

Makarov V, Manina G, Mikusova K, Möllmann U, Ryabova O, Saint-Joanis B, Dhar N, Pasca MR, Buroni S, Lucarelli AP, Milano A, De Rossi E, Belanova M, Bobovska A, Dianiskova P, Kordulakova J, Sala C, Fullam E, Schneider P, McKinney JD, Brodin P, Christophe T, Waddell S, Butcher P, Albrethsen J, Rosenkrands I, Brosch R, Nandi V, Bharath S, Gaonkar S, Shandil RK, Balasubramanian V, Balganesh T, Tyagi S, Grosset J, Riccardi G, Cole ST.

Science. 2009 May 8;324(5928):801-4. doi: 10.1126/science.1171583. Epub 2009 Mar 19.

25.

A fast, fully automated cell segmentation algorithm for high-throughput and high-content screening.

Fenistein D, Lenseigne B, Christophe T, Brodin P, Genovesio A.

Cytometry A. 2008 Oct;73(10):958-64. doi: 10.1002/cyto.a.20627.

26.

pH-independent endocytic cycling of the chemokine receptor CCR5.

Signoret N, Christophe T, Oppermann M, Marsh M.

Traffic. 2004 Jul;5(7):529-43.

28.

Phagocyte activation by Trp-Lys-Tyr-Met-Val-Met, acting through FPRL1/LXA4R, is not affected by lipoxin A4.

Christophe T, Karlsson A, Rabiet MJ, Boulay F, Dahlgren C.

Scand J Immunol. 2002 Nov;56(5):470-6.

29.

A proinflammatory peptide from Helicobacter pylori activates monocytes to induce lymphocyte dysfunction and apoptosis.

Betten A, Bylund J, Christophe T, Boulay F, Romero A, Hellstrand K, Dahlgren C.

J Clin Invest. 2001 Oct;108(8):1221-8. Erratum in: J Clin Invest. 2006 May;116(5):1457. Cristophe, T [corrected to Christophe, T].

30.

Proinflammatory activity of a cecropin-like antibacterial peptide from Helicobacter pylori.

Bylund J, Christophe T, Boulay F, Nyström T, Karlsson A, Dahlgren C.

Antimicrob Agents Chemother. 2001 Jun;45(6):1700-4.

31.
32.

The synthetic chemoattractant Trp-Lys-Tyr-Met-Val-DMet activates neutrophils preferentially through the lipoxin A(4) receptor.

Dahlgren C, Christophe T, Boulay F, Madianos PN, Rabiet MJ, Karlsson A.

Blood. 2000 Mar 1;95(5):1810-8.

PMID:
10688842
35.

Isolation and characterization of a variant HL60 cell line defective in the activation of the NADPH oxidase by phorbol myristate acetate.

Tardif M, Rabiet MJ, Christophe T, Milcent MD, Boulay F.

J Immunol. 1998 Dec 15;161(12):6885-95.

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