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Items: 28

1.

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
2.

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.

Cleghorn LAT, Ray PC, Odingo J, Kumar A, Wescott H, Korkegian A, Masquelin T, Lopez Moure A, Wilson C, Davis S, Huggett M, Turner P, Smith A, Epemolu O, Zuccotto F, Riley J, Scullion P, Shishikura Y, Ferguson L, Rullas J, Guijarro L, Read KD, Green SR, Hipskind P, Parish T, Wyatt PG.

J Med Chem. 2018 Aug 9;61(15):6592-6608. doi: 10.1021/acs.jmedchem.8b00172. Epub 2018 Jul 26.

3.

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
4.

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.

5.

The multistate tuberculosis pharmacometric model: a semi-mechanistic pharmacokinetic-pharmacodynamic model for studying drug effects in an acute tuberculosis mouse model.

Chen C, Ortega F, Rullas J, Alameda L, Angulo-Barturen I, Ferrer S, Simonsson US.

J Pharmacokinet Pharmacodyn. 2017 Apr;44(2):133-141. doi: 10.1007/s10928-017-9508-2. Epub 2017 Feb 15.

6.

Identification of KasA as the cellular target of an anti-tubercular scaffold.

Abrahams KA, Chung CW, Ghidelli-Disse S, Rullas J, Rebollo-López MJ, Gurcha SS, Cox JA, Mendoza A, Jiménez-Navarro E, Martínez-Martínez MS, Neu M, Shillings A, Homes P, Argyrou A, Casanueva R, Loman NJ, Moynihan PJ, Lelièvre J, Selenski C, Axtman M, Kremer L, Bantscheff M, Angulo-Barturen I, Izquierdo MC, Cammack NC, Drewes G, Ballell L, Barros D, Besra GS, Bates RH.

Nat Commun. 2016 Sep 1;7:12581. doi: 10.1038/ncomms12581.

7.

THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria.

Cox JA, Abrahams KA, Alemparte C, Ghidelli-Disse S, Rullas J, Angulo-Barturen I, Singh A, Gurcha SS, Nataraj V, Bethell S, Remuiñán MJ, Encinas L, Jervis PJ, Cammack NC, Bhatt A, Kruse U, Bantscheff M, Fütterer K, Barros D, Ballell L, Drewes G, Besra GS.

Nat Microbiol. 2016 Jan 18;1:15006. doi: 10.1038/nmicrobiol.2015.6.

PMID:
27571973
8.

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.

9.

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
10.

A Focused Screen Identifies Antifolates with Activity on Mycobacterium tuberculosis.

Kumar A, Guardia A, Colmenarejo G, Pérez E, Gonzalez RR, Torres P, Calvo D, Gómez RM, Ortega F, Jiménez E, Gabarro RC, Rullás J, Ballell L, Sherman DR.

ACS Infect Dis. 2015 Dec 11;1(12):604-14. doi: 10.1021/acsinfecdis.5b00063. Epub 2015 Aug 12.

11.

Combinations of β-Lactam Antibiotics Currently in Clinical Trials Are Efficacious in a DHP-I-Deficient Mouse Model of Tuberculosis Infection.

Rullas J, Dhar N, McKinney JD, García-Pérez A, Lelievre J, Diacon AH, Hugonnet JE, Arthur M, Angulo-Barturen I, Barros-Aguirre D, Ballell L.

Antimicrob Agents Chemother. 2015 Aug;59(8):4997-9. doi: 10.1128/AAC.01063-15. Epub 2015 May 18.

12.

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.

13.

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
14.

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.

15.

Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection.

Poce G, Bates RH, Alfonso S, Cocozza M, Porretta GC, Ballell L, Rullas J, Ortega F, De Logu A, Agus E, La Rosa V, Pasca MR, De Rossi E, Wae B, Franzblau SG, Manetti F, Botta M, Biava M.

PLoS One. 2013;8(2):e56980. doi: 10.1371/journal.pone.0056980. Epub 2013 Feb 21.

16.

Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.

Rullas J, García JI, Beltrán M, Cardona PJ, Cáceres N, García-Bustos JF, Angulo-Barturen I.

Antimicrob Agents Chemother. 2010 May;54(5):2262-4. doi: 10.1128/AAC.01423-09. Epub 2010 Feb 16.

17.

A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes.

Angulo-Barturen I, Jiménez-Díaz MB, Mulet T, Rullas J, Herreros E, Ferrer S, Jiménez E, Mendoza A, Regadera J, Rosenthal PJ, Bathurst I, Pompliano DL, Gómez de las Heras F, Gargallo-Viola D.

PLoS One. 2008 May 21;3(5):e2252. doi: 10.1371/journal.pone.0002252.

18.

Basal shuttle of NF-kappaB/I kappaB alpha in resting T lymphocytes regulates HIV-1 LTR dependent expression.

Coiras M, López-Huertas MR, Rullas J, Mittelbrunn M, Alcamí J.

Retrovirology. 2007 Aug 8;4:56.

19.

Fas activation of a proinflammatory program in rheumatoid synoviocytes and its regulation by FLIP and caspase 8 signaling.

Palao G, Santiago B, Galindo MA, Rullas JN, Alcamí J, Ramirez JC, Pablos JL.

Arthritis Rheum. 2006 May;54(5):1473-81.

20.

Improvement of detection specificity of Plasmodium-infected murine erythrocytes by flow cytometry using autofluorescence and YOYO-1.

Jiménez-Díaz MB, Rullas J, Mulet T, Fernández L, Bravo C, Gargallo-Viola D, Angulo-Barturen I.

Cytometry A. 2005 Sep;67(1):27-36.

21.

Prostratin induces HIV activation and downregulates HIV receptors in peripheral blood lymphocytes.

Rullas J, Bermejo M, García-Pérez J, Beltán M, González N, Hezareh M, Brown SJ, Alcamí J.

Antivir Ther. 2004 Aug;9(4):545-54.

PMID:
15456086
22.

TRAF family proteins link PKR with NF-kappa B activation.

Gil J, García MA, Gomez-Puertas P, Guerra S, Rullas J, Nakano H, Alcamí J, Esteban M.

Mol Cell Biol. 2004 May;24(10):4502-12.

23.

MC159L protein from the poxvirus molluscum contagiosum virus inhibits NF-kappaB activation and apoptosis induced by PKR.

Gil J, Rullas J, Alcamí J, Esteban M.

J Gen Virol. 2001 Dec;82(Pt 12):3027-34.

PMID:
11714980
24.

The hepatitis B virus X protein induces HIV-1 replication and transcription in synergy with T-cell activation signals: functional roles of NF-kappaB/NF-AT and SP1-binding sites in the HIV-1 long terminal repeat promoter.

Gómez-Gonzalo M, Carretero M, Rullas J, Lara-Pezzi E, Aramburu J, Berkhout B, Alcamí J, López-Cabrera M.

J Biol Chem. 2001 Sep 21;276(38):35435-43. Epub 2001 Jul 16.

25.

Chemokine expression by systemic sclerosis fibroblasts: abnormal regulation of monocyte chemoattractant protein 1 expression.

Galindo M, Santiago B, Rivero M, Rullas J, Alcami J, Pablos JL.

Arthritis Rheum. 2001 Jun;44(6):1382-6.

26.

The catalytic activity of dsRNA-dependent protein kinase, PKR, is required for NF-kappaB activation.

Gil J, Rullas J, García MA, Alcamí J, Esteban M.

Oncogene. 2001 Jan 18;20(3):385-94.

27.

Early myeloid cells are high producers of nitric oxide upon CD40 plus IFN-gamma stimulation through a mechanism dependent on endogenous TNF-alpha and IL-1alpha.

Angulo I, Rullas J, Campillo JA, Obregón E, Heath A, Howard M, Muñoz-Fernández MA, Subiza JL.

Eur J Immunol. 2000 May;30(5):1263-71.

28.

Sialoadhesin expression by bone marrow macrophages derived from Ehrlich-tumor-bearing mice.

Kusmartsev S, Ruiz de Morales JM, Rullas J, Danilets MG, Subiza JL.

Cancer Immunol Immunother. 1999 Dec;48(9):493-8.

PMID:
10602886

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