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Items: 20

1.

Inhibiting the stringent response blocks Mycobacterium tuberculosis entry into quiescence and reduces persistence.

Dutta NK, Klinkenberg LG, Vazquez MJ, Segura-Carro D, Colmenarejo G, Ramon F, Rodriguez-Miquel B, Mata-Cantero L, Porras-De Francisco E, Chuang YM, Rubin H, Lee JJ, Eoh H, Bader JS, Perez-Herran E, Mendoza-Losana A, Karakousis PC.

Sci Adv. 2019 Mar 20;5(3):eaav2104. doi: 10.1126/sciadv.aav2104. eCollection 2019 Mar.

2.

Mycobacterial Aminoglycoside Acetyltransferases: A Little of Drug Resistance, and a Lot of Other Roles.

Sanz-García F, Anoz-Carbonell E, Pérez-Herrán E, Martín C, Lucía A, Rodrigues L, Aínsa JA.

Front Microbiol. 2019 Jan 30;10:46. doi: 10.3389/fmicb.2019.00046. eCollection 2019.

3.

Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis.

Guardia A, Baiget J, Cacho M, Pérez A, Ortega-Guerra M, Nxumalo W, Khanye SD, Rullas J, Ortega F, Jiménez E, Pérez-Herrán E, Fraile-Gabaldón MT, Esquivias J, Fernández R, Porras-De Francisco E, Encinas L, Alonso M, Giordano I, Rivero C, Miguel-Siles J, Osende JG, Badiola KA, Rutledge PJ, Todd MH, Remuiñán M, Alemparte C.

J Med Chem. 2018 Dec 27;61(24):11327-11340. doi: 10.1021/acs.jmedchem.8b01533. Epub 2018 Dec 12.

PMID:
30457865
4.

Identification and characterization of aspartyl-tRNA synthetase inhibitors against Mycobacterium tuberculosis by an integrated whole-cell target-based approach.

Soto R, Perez-Herran E, Rodriguez B, Duma BM, Cacho-Izquierdo M, Mendoza-Losana A, Lelievre J, Aguirre DB, Ballell L, Cox LR, Alderwick LJ, Besra GS.

Sci Rep. 2018 Aug 23;8(1):12664. doi: 10.1038/s41598-018-31157-3.

5.

Synthesis, antimycobacterial activity and influence on mycobacterial InhA and PknB of 12-membered cyclodepsipeptides.

Laqua K, Klemm M, Richard-Greenblatt M, Richter A, Liebe L, Huang T, Lin S, Guardia A, Pérez-Herran E, Ballell L, Av-Gay Y, Imming P.

Bioorg Med Chem. 2018 Jul 23;26(12):3166-3190. doi: 10.1016/j.bmc.2018.04.045. Epub 2018 Apr 22.

PMID:
29706526
6.

Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656).

Li X, Hernandez V, Rock FL, Choi W, Mak YSL, Mohan M, Mao W, Zhou Y, Easom EE, Plattner JJ, Zou W, Pérez-Herrán E, Giordano I, Mendoza-Losana A, Alemparte C, Rullas J, Angulo-Barturen I, Crouch S, Ortega F, Barros D, Alley MRK.

J Med Chem. 2017 Oct 12;60(19):8011-8026. doi: 10.1021/acs.jmedchem.7b00631. Epub 2017 Sep 27.

PMID:
28953378
7.

Inhibiting mycobacterial tryptophan synthase by targeting the inter-subunit interface.

Abrahams KA, Cox JAG, Fütterer K, Rullas J, Ortega-Muro F, Loman NJ, Moynihan PJ, Pérez-Herrán E, Jiménez E, Esquivias J, Barros D, Ballell L, Alemparte C, Besra GS.

Sci Rep. 2017 Aug 25;7(1):9430. doi: 10.1038/s41598-017-09642-y.

8.

Detection of a Putative TetR-Like Gene Related to Mycobacterium bovis BCG Growth in Cholesterol Using a gfp-Transposon Mutagenesis System.

Otal I, Pérez-Herrán E, Garcia-Morales L, Menéndez MC, Gonzalez-Y-Merchand JA, Martín C, García MJ.

Front Microbiol. 2017 Mar 6;8:315. doi: 10.3389/fmicb.2017.00315. eCollection 2017.

9.

Whole Cell Target Engagement Identifies Novel Inhibitors of Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase.

Batt SM, Cacho Izquierdo M, Castro Pichel J, Stubbs CJ, Vela-Glez Del Peral L, Pérez-Herrán E, Dhar N, Mouzon B, Rees M, Hutchinson JP, Young RJ, McKinney JD, Barros Aguirre D, Ballell L, Besra GS, Argyrou A.

ACS Infect Dis. 2015 Dec 11;1(12):615-26. doi: 10.1021/acsinfecdis.5b00065. Epub 2015 Aug 25.

PMID:
27623058
10.

Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase.

Palencia A, Li X, Bu W, Choi W, Ding CZ, Easom EE, Feng L, Hernandez V, Houston P, Liu L, Meewan M, Mohan M, Rock FL, Sexton H, Zhang S, Zhou Y, Wan B, Wang Y, Franzblau SG, Woolhiser L, Gruppo V, Lenaerts AJ, O'Malley T, Parish T, Cooper CB, Waters MG, Ma Z, Ioerger TR, Sacchettini JC, Rullas J, Angulo-Barturen I, Pérez-Herrán E, Mendoza A, Barros D, Cusack S, Plattner JJ, Alley MR.

Antimicrob Agents Chemother. 2016 Sep 23;60(10):6271-80. doi: 10.1128/AAC.01339-16. Print 2016 Oct.

11.

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor.

Martínez-Hoyos M, Perez-Herran E, Gulten G, Encinas L, Álvarez-Gómez D, Alvarez E, Ferrer-Bazaga S, García-Pérez A, Ortega F, Angulo-Barturen I, Rullas-Trincado J, Blanco Ruano D, Torres P, Castañeda P, Huss S, Fernández Menéndez R, González Del Valle S, Ballell L, Barros D, Modha S, Dhar N, Signorino-Gelo F, McKinney JD, García-Bustos JF, Lavandera JL, Sacchettini JC, Jimenez MS, Martín-Casabona N, Castro-Pichel J, Mendoza-Losana A.

EBioMedicine. 2016 Jun;8:291-301. doi: 10.1016/j.ebiom.2016.05.006. Epub 2016 May 8.

12.

N-Benzyl-4-((heteroaryl)methyl)benzamides: A New Class of Direct NADH-Dependent 2-trans Enoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors with Antitubercular Activity.

Guardia A, Gulten G, Fernandez R, Gómez J, Wang F, Convery M, Blanco D, Martínez M, Pérez-Herrán E, Alonso M, Ortega F, Rullás J, Calvo D, Mata L, Young R, Sacchettini JC, Mendoza-Losana A, Remuiñán M, Ballell Pages L, Castro-Pichel J.

ChemMedChem. 2016 Apr 5;11(7):687-701. doi: 10.1002/cmdc.201600020. Epub 2016 Mar 2.

PMID:
26934341
13.

New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold.

Pajk S, Živec M, Šink R, Sosič I, Neu M, Chung CW, Martínez-Hoyos M, Pérez-Herrán E, Álvarez-Gómez D, Álvarez-Ruíz E, Mendoza-Losana A, Castro-Pichel J, Barros D, Ballell-Pages L, Young RJ, Convery MA, Encinas L, Gobec S.

Eur J Med Chem. 2016 Apr 13;112:252-257. doi: 10.1016/j.ejmech.2016.02.008. Epub 2016 Feb 8.

PMID:
26900657
14.

Antimicrobial susceptibility testing for Mycobacterium sp.

Blanco-Ruano D, Roberts DM, Gonzalez-Del-Rio R, Álvarez D, Rebollo MJ, Pérez-Herrán E, Mendoza A.

Methods Mol Biol. 2015;1285:257-68. doi: 10.1007/978-1-4939-2450-9_15.

PMID:
25779321
15.

Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs.

Blanco D, Perez-Herran E, Cacho M, Ballell L, Castro J, González Del Río R, Lavandera JL, Remuiñán MJ, Richards C, Rullas J, Vázquez-Muñiz MJ, Woldu E, Zapatero-González MC, Angulo-Barturen I, Mendoza A, Barros D.

Antimicrob Agents Chemother. 2015 Apr;59(4):1868-75. doi: 10.1128/AAC.03913-14. Epub 2015 Jan 12.

16.

Pulmonary Mycobacterium bovis BCG vaccination confers dose-dependent superior protection compared to that of subcutaneous vaccination.

Aguilo N, Toledo AM, Lopez-Roman EM, Perez-Herran E, Gormley E, Rullas-Trincado J, Angulo-Barturen I, Martin C.

Clin Vaccine Immunol. 2014 Apr;21(4):594-7. doi: 10.1128/CVI.00700-13. Epub 2014 Feb 5.

17.

Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.

Encinas L, O'Keefe H, Neu M, Remuiñán MJ, Patel AM, Guardia A, Davie CP, Pérez-Macías N, Yang H, Convery MA, Messer JA, Pérez-Herrán E, Centrella PA, Alvarez-Gómez D, Clark MA, Huss S, O'Donovan GK, Ortega-Muro F, McDowell W, Castañeda P, Arico-Muendel CC, Pajk S, Rullás J, Angulo-Barturen I, Alvarez-Ruíz E, Mendoza-Losana A, Ballell Pages L, Castro-Pichel J, Evindar G.

J Med Chem. 2014 Feb 27;57(4):1276-88. doi: 10.1021/jm401326j. Epub 2014 Feb 5.

PMID:
24450589
18.

Tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL3.

Remuiñán MJ, Pérez-Herrán E, Rullás J, Alemparte C, Martínez-Hoyos M, Dow DJ, Afari J, Mehta N, Esquivias J, Jiménez E, Ortega-Muro F, Fraile-Gabaldón MT, Spivey VL, Loman NJ, Pallen MJ, Constantinidou C, Minick DJ, Cacho M, Rebollo-López MJ, González C, Sousa V, Angulo-Barturen I, Mendoza-Losana A, Barros D, Besra GS, Ballell L, Cammack N.

PLoS One. 2013 Apr 17;8(4):e60933. doi: 10.1371/journal.pone.0060933. Print 2013.

19.

Fueling open-source drug discovery: 177 small-molecule leads against tuberculosis.

Ballell L, Bates RH, Young RJ, Alvarez-Gomez D, Alvarez-Ruiz E, Barroso V, Blanco D, Crespo B, Escribano J, González R, Lozano S, Huss S, Santos-Villarejo A, Martín-Plaza JJ, Mendoza A, Rebollo-Lopez MJ, Remuiñan-Blanco M, Lavandera JL, Pérez-Herran E, Gamo-Benito FJ, García-Bustos JF, Barros D, Castro JP, Cammack N.

ChemMedChem. 2013 Feb;8(2):313-21. doi: 10.1002/cmdc.201200428. Epub 2013 Jan 10.

20.

4-Substituted thioquinolines and thiazoloquinolines: potent, selective, and Tween-80 in vitro dependent families of antitubercular agents with moderate in vivo activity.

Escribano J, Rivero-Hernández C, Rivera H, Barros D, Castro-Pichel J, Pérez-Herrán E, Mendoza-Losana A, Angulo-Barturen I, Ferrer-Bazaga S, Jiménez-Navarro E, Ballell L.

ChemMedChem. 2011 Dec 9;6(12):2252-63. doi: 10.1002/cmdc.201100309. Epub 2011 Sep 16.

PMID:
21922671

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