1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti-Trypanosoma brucei Agents: SAR and in Vivo Efficacy

Por Buchynskyy, Andriy, Gillespie, J. Robert, Herbst, Zackary M., Ranade, Ranae M., Buckner, Frederick S., Gelb, Michael H.
Publicado no ACS Med Chem Lett (2017)

Induced Resistance to Methionyl-tRNA Synthetase Inhibitors in Trypanosoma brucei Is Due to Overexpression of the Target

Por Ranade, Ranae M., Gillespie, J. Robert, Shibata, Sayaka, Verlinde, Christophe L. M. J., Fan, Erkang, Hol, Wim G. J., Buckner, Frederick S.
Publicado em 2013

New Class of Antitrypanosomal Agents Based on Imidazopyridines

Por Silva, Daniel G., Gillespie, J. Robert, Ranade, Ranae M., Herbst, Zackary M., Nguyen, Uyen T. T., Buckner, Frederick S., Montanari, Carlos A., Gelb, Michael H.
Publicado no ACS Med Chem Lett (2017)

Inhibitors of Methionyl-tRNA Synthetase Have Potent Activity against Giardia intestinalis Trophozoites

Por Ranade, Ranae M., Zhang, Zhongsheng, Gillespie, J. Robert, Shibata, Sayaka, Verlinde, Christophe L. M. J., Hol, Wim G. J., Fan, Erkang, Buckner, Frederick S.
Publicado no Antimicrob Agents Chemother (2015)

Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors

Por Buchynskyy, Andriy, Gillespie, J. Robert, Hulverson, Matthew A., McQueen, Joshua, Creason, Sharon A., Ranade, Ranae M., Duster, Nicole A., Gelb, Michael H., Buckner, Frederick S.
Publicado no Bioorg Med Chem (2016)

The crystal structure of the drug target Mycobacterium tuberculosis methionyl-tRNA synthetase in complex with a catalytic intermediate

Por Barros-Álvarez, Ximena, Turley, Stewart, Ranade, Ranae M., Gillespie, J. Robert, Duster, Nicole A., Verlinde, Christophe L. M. J., Fan, Erkang, Buckner, Frederick S., Hol, Wim G. J.
Publicado no Acta Crystallogr F Struct Biol Commun (2018)

Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis

Por Patrick, Donald A., Gillespie, J. Robert, McQueen, Joshua, Hulverson, Matthew A., Ranade, Ranae M., Creason, Sharon A., Herbst, Zackary M., Gelb, Michael H., Buckner, Frederick S., Tidwell, Richard R.
Publicado no J Med Chem (2016)

Distinct states of methionyl-tRNA synthetase indicates inhibitor binding by conformational selection

Por Koh, Cho Yeow, Kim, Jessica E., Shibata, Sayaka, Ranade, Ranae M., Yu, Mingyan, Liu, Jiyun, Gillespie, J. Robert, Buckner, Frederick S., Verlinde, Christophe L.M.J., Fan, Erkang, Hol, Wim G.J.
Publicado em 2012

A binding hotspot in Trypanosoma cruzi histidyl-tRNA synthetase revealed by fragment-based crystallographic cocktail screens

Por Koh, Cho Yeow, Kallur Siddaramaiah, Latha, Ranade, Ranae M., Nguyen, Jasmine, Jian, Tengyue, Zhang, Zhongsheng, Gillespie, J. Robert, Buckner, Frederick S., Verlinde, Christophe L. M. J., Fan, Erkang, Hol, Wim G. J.
Publicado no Acta Crystallogr D Biol Crystallogr (2015)

Optimization of a binding fragment targeting the “enlarged methionine pocket” leads to potent Trypanosoma brucei methionyl-tRNA synthetase inhibitors

Por Huang, Wenlin, Zhang, Zhongsheng, Ranade, Ranae M., Gillespie, J. Robert, Barros-Álvarez, Ximena, Creason, Sharon A., Shibata, Sayaka, Verlinde, Christophe L. M. J., Hol, Wim G. J., Buckner, Frederick S., Fan, Erkang
Publicado no Bioorg Med Chem Lett (2017)

Urea-based inhibitors of Trypanosoma brucei methionyl-tRNA synthetase: selectivity and in vivo characterization

Por Shibata, Sayaka, Gillespie, J. Robert, Ranade, Ranae M., Koh, Cho Yeow, Kim, Jessica E., Laydbak, Joy U., Zucker, Frank H., Hol, Wim G. J., Verlinde, Christophe L. M. J., Buckner, Frederick S., Fan, Erkang
Publicado em 2012

Development of Methionyl-tRNA Synthetase Inhibitors as Antibiotics for Gram-Positive Bacterial Infections

Por Faghih, Omeed, Zhang, Zhongsheng, Ranade, Ranae M., Gillespie, J. Robert, Creason, Sharon A., Huang, Wenlin, Shibata, Sayaka, Barros-Álvarez, Ximena, Verlinde, Christophe L. M. J., Hol, Wim G. J., Fan, Erkang, Buckner, Frederick S.
Publicado no Antimicrob Agents Chemother (2017)

Structure-Guided Design of Novel Trypanosoma brucei Methionyl-tRNA Synthetase Inhibitors

Por Huang, Wenlin, Zhang, Zhongsheng, Barros-Álvarez, Ximena, Koh, Cho Yeow, Ranade, Ranae M., Gillespie, J. Robert, Creason, Sharon A., Shibata, Sayaka, Verlinde, Christophe L. M. J., Hol, Wim G. J., Buckner, Frederick S., Fan, Erkang
Publicado no Eur J Med Chem (2016)

Leishmania donovani tyrosyl-tRNA synthetase structure in complex with a tyrosyl adenylate analog and comparisons with human and protozoan counterparts

Por Barros-Álvarez, Ximena, Kerchner, Keshia M., Koh, Cho Yeow, Turley, Stewart, Pardon, Els, Steyaert, Jan, Ranade, Ranae M., Gillespie, J. Robert, Zhang, Zhongsheng, Verlinde, Christophe L. M. J., Fan, Erkang, Buckner, Frederick S., Hol, Wim G. J.
Publicado no Biochimie (2017)

Glycogen Synthase Kinase 3 Is a Potential Drug Target for African Trypanosomiasis Therapy

Por Ojo, Kayode K., Gillespie, J. Robert, Riechers, Aaron J., Napuli, Alberto J., Verlinde, Christophe L. M. J., Buckner, Frederick S., Gelb, Michael H., Domostoj, Mathias M., Wells, Susan J., Scheer, Alexander, Wells, Timothy N. C., Van Voorhis, Wesley C.
Publicado em 2008

Characterization of Trypanosoma brucei dihydroorotate dehydrogenase as a possible drug target; structural, kinetic and RNAi studies

Por Arakaki, Tracy L, Buckner, Frederick S, Gillespie, J Robert, Malmquist, Nicholas A, Phillips, Margaret A, Kalyuzhniy, Oleksandr, Luft, Joseph R, DeTitta, George T, Verlinde, Christophe L M J, Van Voorhis, Wesley C, Hol, Wim G J, Merritt, Ethan A
Publicado em 2008

5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors

Por Zhang, Zhongsheng, Koh, Cho Yeow, Ranade, Ranae M., Shibata, Sayaka, Gillespie, J. Robert, Hulverson, Matthew A., Huang, Wenlin, Nguyen, Jasmine, Pendem, Nagendar, Gelb, Michael H., Verlinde, Christophe L. M. J., Hol, Wim G. J., Buckner, Frederick S., Fan, Erkang
Publicado no ACS Infect Dis (2016)

Structures of Trypanosoma brucei Methionyl-tRNA Synthetase with Urea-Based Inhibitors Provide Guidance for Drug Design against Sleeping Sickness

Por Koh, Cho Yeow, Kim, Jessica E., Wetzel, Allan B., de van der Schueren, Will J., Shibata, Sayaka, Ranade, Ranae M., Liu, Jiyun, Zhang, Zhongsheng, Gillespie, J. Robert, Buckner, Frederick S., Verlinde, Christophe L. M. J., Fan, Erkang, Hol, Wim G. J.
Publicado em 2014

Crystal structures of trypanosomal histidyl-tRNA synthetase illuminate differences between eukaryotic and prokaryotic homologs

Por Merritt, Ethan A, Arakaki, Tracy L, Gillespie, J Robert, Larson, Eric T, Kelley, Angela, Mueller, Natascha, Napuli, Alberto J, Kim, Jessica, Zhang, Li, Verlinde, Christophe L M J, Fan, Erkang, Zucker, Frank, Buckner, Frederick S, Van Voorhis, Wesley C, Hol, Wim G J
Publicado em 2010

Identification of Potent Inhibitors of the Trypanosoma brucei Methionyl-tRNA Synthetase via High Throughput Orthogonal Screening

Por Pedró-Rosa, Laura, Buckner, Frederick S., Ranade, Ranae M., Eberhart, Christina, Madoux, Franck, Gillespie, J. Robert, Koh, Cho Yeow, Brown, Steven, Lohse, Jacqueline, Verlinde, Christophe L. M., Fan, Erkang, Bannister, Thomas, Scampavia, Louis, Hol, Wim G. J., Spicer, Timothy, Hodder, Peter
Publicado no J Biomol Screen (2014)