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Page 1
The Tuberculosis Drug Accelerator at year 10: what have we learned?
Aldridge BB, Barros-Aguirre D, Barry CE 3rd, Bates RH, Berthel SJ, Boshoff HI, Chibale K, Chu XJ, Cooper CB, Dartois V, Duncan K, Fotouhi N, Gusovsky F, Hipskind PA, Kempf DJ, Lelièvre J, Lenaerts AJ, McNamara CW, Mizrahi V, Nathan C, Olsen DB, Parish T, Petrassi HM, Pym A, Rhee KY, Robertson GT, Rock JM, Rubin EJ, Russell B, Russell DG, Sacchettini JC, Schnappinger D, Schrimpf M, Upton AM, Warner P, Wyatt PG, Yuan Y. Aldridge BB, et al. Among authors: lelievre j. Nat Med. 2021 Aug;27(8):1333-1337. doi: 10.1038/s41591-021-01442-2. Nat Med. 2021. PMID: 34226736 Free PMC article.
GSK2556286 Is a Novel Antitubercular Drug Candidate Effective In Vivo with the Potential To Shorten Tuberculosis Treatment.
Nuermberger EL, Martínez-Martínez MS, Sanz O, Urones B, Esquivias J, Soni H, Tasneen R, Tyagi S, Li SY, Converse PJ, Boshoff HI, Robertson GT, Besra GS, Abrahams KA, Upton AM, Mdluli K, Boyle GW, Turner S, Fotouhi N, Cammack NC, Siles JM, Alonso M, Escribano J, Lelievre J, Rullas-Trincado J, Pérez-Herrán E, Bates RH, Maher-Edwards G, Barros D, Ballell L, Jiménez E. Nuermberger EL, et al. Among authors: lelievre j. Antimicrob Agents Chemother. 2022 Jun 21;66(6):e0013222. doi: 10.1128/aac.00132-22. Epub 2022 May 24. Antimicrob Agents Chemother. 2022. PMID: 35607978 Free PMC article.
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI. Park Y, et al. Among authors: lelievre j. ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17. ACS Infect Dis. 2017. PMID: 27704782 Free PMC article.
A Mycobacterium tuberculosis NBTI DNA Gyrase Inhibitor Is Active against Mycobacterium abscessus.
Ganapathy US, Del Río RG, Cacho-Izquierdo M, Ortega F, Lelièvre J, Barros-Aguirre D, Aragaw WW, Zimmerman MD, Lindman M, Dartois V, Gengenbacher M, Dick T. Ganapathy US, et al. Among authors: lelievre j. Antimicrob Agents Chemother. 2021 Nov 17;65(12):e0151421. doi: 10.1128/AAC.01514-21. Epub 2021 Oct 4. Antimicrob Agents Chemother. 2021. PMID: 34606340 Free PMC article.
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
Wilson CR, Gessner RK, Moosa A, Seldon R, Warner DF, Mizrahi V, Soares de Melo C, Simelane SB, Nchinda A, Abay E, Taylor D, Njoroge M, Brunschwig C, Lawrence N, Boshoff HIM, Barry CE 3rd, Sirgel FA, van Helden P, Harris CJ, Gordon R, Ghidelli-Disse S, Pflaumer H, Boesche M, Drewes G, Sanz O, Santos G, Rebollo-Lopez MJ, Urones B, Selenski C, Lafuente-Monasterio MJ, Axtman M, Lelièvre J, Ballell L, Mueller R, Street LJ, Ghorpade SR, Chibale K. Wilson CR, et al. Among authors: lelievre j. J Med Chem. 2017 Dec 28;60(24):10118-10134. doi: 10.1021/acs.jmedchem.7b01347. Epub 2017 Dec 7. J Med Chem. 2017. PMID: 29148755 Free PMC article.
Accelerating Early Antituberculosis Drug Discovery by Creating Mycobacterial Indicator Strains That Predict Mode of Action.
Boot M, Commandeur S, Subudhi AK, Bahira M, Smith TC 2nd, Abdallah AM, van Gemert M, Lelièvre J, Ballell L, Aldridge BB, Pain A, Speer A, Bitter W. Boot M, et al. Among authors: lelievre j. Antimicrob Agents Chemother. 2018 Jun 26;62(7):e00083-18. doi: 10.1128/AAC.00083-18. Print 2018 Jul. Antimicrob Agents Chemother. 2018. PMID: 29661879 Free PMC article.
A Leucyl-tRNA Synthetase Inhibitor with Broad-Spectrum Anti-Mycobacterial Activity.
Ganapathy US, Del Rio RG, Cacho-Izquierdo M, Ortega F, Lelièvre J, Barros-Aguirre D, Lindman M, Dartois V, Gengenbacher M, Dick T. Ganapathy US, et al. Among authors: lelievre j. Antimicrob Agents Chemother. 2023 May 1;95(5):e02420-20. doi: 10.1128/AAC.02420-20. Epub 2021 Feb 8. Antimicrob Agents Chemother. 2023. PMID: 33558292 Free PMC article.
Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.
Machutta CA, Kollmann CS, Lind KE, Bai X, Chan PF, Huang J, Ballell L, Belyanskaya S, Besra GS, Barros-Aguirre D, Bates RH, Centrella PA, Chang SS, Chai J, Choudhry AE, Coffin A, Davie CP, Deng H, Deng J, Ding Y, Dodson JW, Fosbenner DT, Gao EN, Graham TL, Graybill TL, Ingraham K, Johnson WP, King BW, Kwiatkowski CR, Lelièvre J, Li Y, Liu X, Lu Q, Lehr R, Mendoza-Losana A, Martin J, McCloskey L, McCormick P, O'Keefe HP, O'Keeffe T, Pao C, Phelps CB, Qi H, Rafferty K, Scavello GS, Steiginga MS, Sundersingh FS, Sweitzer SM, Szewczuk LM, Taylor A, Toh MF, Wang J, Wang M, Wilkins DJ, Xia B, Yao G, Zhang J, Zhou J, Donahue CP, Messer JA, Holmes D, Arico-Muendel CC, Pope AJ, Gross JW, Evindar G. Machutta CA, et al. Among authors: lelievre j. Nat Commun. 2017 Jul 17;8:16081. doi: 10.1038/ncomms16081. Nat Commun. 2017. PMID: 28714473 Free PMC article.
Release of 50 new, drug-like compounds and their computational target predictions for open source anti-tubercular drug discovery.
Rebollo-Lopez MJ, Lelièvre J, Alvarez-Gomez D, Castro-Pichel J, Martínez-Jiménez F, Papadatos G, Kumar V, Colmenarejo G, Mugumbate G, Hurle M, Barroso V, Young RJ, Martinez-Hoyos M, González del Río R, Bates RH, Lopez-Roman EM, Mendoza-Losana A, Brown JR, Alvarez-Ruiz E, Marti-Renom MA, Overington JP, Cammack N, Ballell L, Barros-Aguire D. Rebollo-Lopez MJ, et al. Among authors: lelievre j. PLoS One. 2015 Dec 7;10(12):e0142293. doi: 10.1371/journal.pone.0142293. eCollection 2015. PLoS One. 2015. PMID: 26642067 Free PMC article.
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. Among authors: lelievre j. Nat Commun. 2016 Sep 1;7:12581. doi: 10.1038/ncomms12581. Nat Commun. 2016. PMID: 27581223 Free PMC article.
357 results