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Optimization of a binding fragment targeting the "enlarged methionine pocket" leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors.
Huang W, Zhang Z, Ranade RM, Gillespie JR, Barros-Álvarez X, Creason SA, Shibata S, Verlinde CLMJ, Hol WGJ, Buckner FS, Fan E. Huang W, et al. Among authors: shibata s. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2702-2707. doi: 10.1016/j.bmcl.2017.04.048. Epub 2017 Apr 17. Bioorg Med Chem Lett. 2017. PMID: 28465105 Free PMC article.
Selective inhibitors of methionyl-tRNA synthetase have potent activity against Trypanosoma brucei Infection in Mice.
Shibata S, Gillespie JR, Kelley AM, Napuli AJ, Zhang Z, Kovzun KV, Pefley RM, Lam J, Zucker FH, Van Voorhis WC, Merritt EA, Hol WG, Verlinde CL, Fan E, Buckner FS. Shibata S, et al. Antimicrob Agents Chemother. 2011 May;55(5):1982-9. doi: 10.1128/AAC.01796-10. Epub 2011 Jan 31. Antimicrob Agents Chemother. 2011. PMID: 21282428 Free PMC article.
Induced resistance to methionyl-tRNA synthetase inhibitors in Trypanosoma brucei is due to overexpression of the target.
Ranade RM, Gillespie JR, Shibata S, Verlinde CL, Fan E, Hol WG, Buckner FS. Ranade RM, et al. Among authors: shibata s. Antimicrob Agents Chemother. 2013 Jul;57(7):3021-8. doi: 10.1128/AAC.02578-12. Epub 2013 Apr 15. Antimicrob Agents Chemother. 2013. PMID: 23587950 Free PMC article.
Inhibitors of methionyl-tRNA synthetase (MetRS) have excellent potential to be developed for this purpose (S. Shibata, J. R. Gillespie, A. M. Kelley, A. J. Napuli, Z. Zhang, K. ...Van Voorhis, E. A. Merritt, W. G. Hol, C. L. Verlinde, E. Fan, and F. S. Buckne …
Inhibitors of methionyl-tRNA synthetase (MetRS) have excellent potential to be developed for this purpose (S. Shibata, J. R. G …
Structures of Trypanosoma brucei methionyl-tRNA synthetase with urea-based inhibitors provide guidance for drug design against sleeping sickness.
Koh CY, Kim JE, Wetzel AB, de van der Schueren WJ, Shibata S, Ranade RM, Liu J, Zhang Z, Gillespie JR, Buckner FS, Verlinde CL, Fan E, Hol WG. Koh CY, et al. Among authors: shibata s. PLoS Negl Trop Dis. 2014 Apr 17;8(4):e2775. doi: 10.1371/journal.pntd.0002775. eCollection 2014 Apr. PLoS Negl Trop Dis. 2014. PMID: 24743796 Free PMC article.
5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors.
Zhang Z, Koh CY, Ranade RM, Shibata S, Gillespie JR, Hulverson MA, Huang W, Nguyen J, Pendem N, Gelb MH, Verlinde CL, Hol WG, Buckner FS, Fan E. Zhang Z, et al. Among authors: shibata s. ACS Infect Dis. 2016 Jun 10;2(6):399-404. doi: 10.1021/acsinfecdis.6b00036. Epub 2016 Apr 11. ACS Infect Dis. 2016. PMID: 27627628 Free PMC article.
Structure-guided design of novel Trypanosoma brucei Methionyl-tRNA synthetase inhibitors.
Huang W, Zhang Z, Barros-Álvarez X, Koh CY, Ranade RM, Gillespie JR, Creason SA, Shibata S, Verlinde CLMJ, Hol WGJ, Buckner FS, Fan E. Huang W, et al. Among authors: shibata s. Eur J Med Chem. 2016 Nov 29;124:1081-1092. doi: 10.1016/j.ejmech.2016.10.024. Epub 2016 Oct 14. Eur J Med Chem. 2016. PMID: 27788467 Free PMC article.
Development of Methionyl-tRNA Synthetase Inhibitors as Antibiotics for Gram-Positive Bacterial Infections.
Faghih O, Zhang Z, Ranade RM, Gillespie JR, Creason SA, Huang W, Shibata S, Barros-Álvarez X, Verlinde CLMJ, Hol WGJ, Fan E, Buckner FS. Faghih O, et al. Among authors: shibata s. Antimicrob Agents Chemother. 2017 Oct 24;61(11):e00999-17. doi: 10.1128/AAC.00999-17. Print 2017 Nov. Antimicrob Agents Chemother. 2017. PMID: 28848016 Free PMC article.
3,066 results