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Page 1
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. Palencia A, et al. Antimicrob Agents Chemother. 2016 Sep 23;60(10):6271-80. doi: 10.1128/AAC.01339-16. Print 2016 Oct. Antimicrob Agents Chemother. 2016. PMID: 27503647 Free PMC article.
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. Blanco D, et al. Antimicrob Agents Chemother. 2015 Apr;59(4):1868-75. doi: 10.1128/AAC.03913-14. Epub 2015 Jan 12. Antimicrob Agents Chemother. 2015. PMID: 25583730 Free PMC article.
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. Rullas J, et al. Antimicrob Agents Chemother. 2015 Aug;59(8):4997-9. doi: 10.1128/AAC.01063-15. Epub 2015 May 18. Antimicrob Agents Chemother. 2015. PMID: 25987618 Free PMC article.
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. Encinas L, et al. J Med Chem. 2014 Feb 27;57(4):1276-88. doi: 10.1021/jm401326j. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24450589
Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis.
Šink R, Sosič I, Živec M, Fernandez-Menendez R, Turk S, Pajk S, Alvarez-Gomez D, Lopez-Roman EM, Gonzales-Cortez C, Rullas-Triconado J, Angulo-Barturen I, Barros D, Ballell-Pages L, Young RJ, Encinas L, Gobec S. Šink R, et al. J Med Chem. 2015 Jan 22;58(2):613-24. doi: 10.1021/jm501029r. Epub 2014 Dec 29. J Med Chem. 2015. PMID: 25517015
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. Abrahams KA, et al. Nat Commun. 2016 Sep 1;7:12581. doi: 10.1038/ncomms12581. Nat Commun. 2016. PMID: 27581223 Free PMC article.
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. Remuiñán MJ, et al. PLoS One. 2013 Apr 17;8(4):e60933. doi: 10.1371/journal.pone.0060933. Print 2013. PLoS One. 2013. PMID: 23613759 Free PMC article.
A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria.
Phillips MA, Lotharius J, Marsh K, White J, Dayan A, White KL, Njoroge JW, El Mazouni F, Lao Y, Kokkonda S, Tomchick DR, Deng X, Laird T, Bhatia SN, March S, Ng CL, Fidock DA, Wittlin S, Lafuente-Monasterio M, Benito FJ, Alonso LM, Martinez MS, Jimenez-Diaz MB, Bazaga SF, Angulo-Barturen I, Haselden JN, Louttit J, Cui Y, Sridhar A, Zeeman AM, Kocken C, Sauerwein R, Dechering K, Avery VM, Duffy S, Delves M, Sinden R, Ruecker A, Wickham KS, Rochford R, Gahagen J, Iyer L, Riccio E, Mirsalis J, Bathhurst I, Rueckle T, Ding X, Campo B, Leroy D, Rogers MJ, Rathod PK, Burrows JN, Charman SA. Phillips MA, et al. Sci Transl Med. 2015 Jul 15;7(296):296ra111. doi: 10.1126/scitranslmed.aaa6645. Sci Transl Med. 2015. PMID: 26180101 Free PMC article.
82 results