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Items: 1 to 50 of 337

1.

Optimization of Methionyl tRNA-Synthetase Inhibitors for Treatment of Cryptosporidium Infection.

Buckner FS, Ranade RM, Gillespie JR, Shibata S, Hulverson MA, Zhang Z, Huang W, Choi R, Verlinde CLMJ, Hol WGJ, Ochida A, Akao Y, Choy RKM, Van Voorhis WC, Arnold SLM, Jumani RS, Huston CD, Fan E.

Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02061-18. doi: 10.1128/AAC.02061-18. Print 2019 Apr.

PMID:
30745384
2.

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

Barros-Álvarez X, Turley S, Ranade RM, Gillespie JR, Duster NA, Verlinde CLMJ, Fan E, Buckner FS, Hol WGJ.

Acta Crystallogr F Struct Biol Commun. 2018 Apr 1;74(Pt 4):245-254. doi: 10.1107/S2053230X18003151. Epub 2018 Mar 28.

3.

Fragment-Based Screening of a Natural Product Library against 62 Potential Malaria Drug Targets Employing Native Mass Spectrometry.

Vu H, Pedro L, Mak T, McCormick B, Rowley J, Liu M, Di Capua A, Williams-Noonan B, Pham NB, Pouwer R, Nguyen B, Andrews KT, Skinner-Adams T, Kim J, Hol WGJ, Hui R, Crowther GJ, Van Voorhis WC, Quinn RJ.

ACS Infect Dis. 2018 Apr 13;4(4):431-444. doi: 10.1021/acsinfecdis.7b00197. Epub 2018 Mar 3.

4.

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.

Antimicrob Agents Chemother. 2017 Oct 24;61(11). pii: e00999-17. doi: 10.1128/AAC.00999-17. Print 2017 Nov.

5.

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.

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2702-2707. doi: 10.1016/j.bmcl.2017.04.048. Epub 2017 Apr 17.

6.

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

Barros-Álvarez X, Kerchner KM, Koh CY, Turley S, Pardon E, Steyaert J, Ranade RM, Gillespie JR, Zhang Z, Verlinde CLMJ, Fan E, Buckner FS, Hol WGJ.

Biochimie. 2017 Jul;138:124-136. doi: 10.1016/j.biochi.2017.04.006. Epub 2017 Apr 18.

7.

From Cells to Mice to Target: Characterization of NEU-1053 (SB-443342) and Its Analogues for Treatment of Human African Trypanosomiasis.

Devine WG, Diaz-Gonzalez R, Ceballos-Perez G, Rojas D, Satoh T, Tear W, Ranade RM, Barros-Álvarez X, Hol WG, Buckner FS, Navarro M, Pollastri MP.

ACS Infect Dis. 2017 Mar 10;3(3):225-236. doi: 10.1021/acsinfecdis.6b00202. Epub 2017 Feb 8.

8.

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.

Eur J Med Chem. 2016 Nov 29;124:1081-1092. doi: 10.1016/j.ejmech.2016.10.024. Epub 2016 Oct 14.

9.

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.

ACS Infect Dis. 2016 Jun 10;2(6):399-404. doi: 10.1021/acsinfecdis.6b00036. Epub 2016 Apr 11.

10.

Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis.

Vidadala RS, Rivas KL, Ojo KK, Hulverson MA, Zambriski JA, Bruzual I, Schultz TL, Huang W, Zhang Z, Scheele S, DeRocher AE, Choi R, Barrett LK, Siddaramaiah LK, Hol WG, Fan E, Merritt EA, Parsons M, Freiberg G, Marsh K, Kempf DJ, Carruthers VB, Isoherranen N, Doggett JS, Van Voorhis WC, Maly DJ.

J Med Chem. 2016 Jul 14;59(13):6531-46. doi: 10.1021/acs.jmedchem.6b00760. Epub 2016 Jul 1.

11.

Zinc coordination is essential for the function and activity of the type II secretion ATPase EpsE.

Rule CS, Patrick M, Camberg JL, Maricic N, Hol WG, Sandkvist M.

Microbiologyopen. 2016 Oct;5(5):870-882. doi: 10.1002/mbo3.376. Epub 2016 May 10.

12.

SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.

Huang W, Ojo KK, Zhang Z, Rivas K, Vidadala RS, Scheele S, DeRocher AE, Choi R, Hulverson MA, Barrett LK, Bruzual I, Siddaramaiah LK, Kerchner KM, Kurnick MD, Freiberg GM, Kempf D, Hol WG, Merritt EA, Neckermann G, de Hostos EL, Isoherranen N, Maly DJ, Parsons M, Doggett JS, Van Voorhis WC, Fan E.

ACS Med Chem Lett. 2015 Oct 22;6(12):1184-1189. eCollection 2015 Dec 10.

13.

Inhibitors of methionyl-tRNA synthetase have potent activity against Giardia intestinalis trophozoites.

Ranade RM, Zhang Z, Gillespie JR, Shibata S, Verlinde CL, Hol WG, Fan E, Buckner FS.

Antimicrob Agents Chemother. 2015 Nov;59(11):7128-31. doi: 10.1128/AAC.01573-15. Epub 2015 Aug 31.

14.

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

Koh CY, Siddaramaiah LK, Ranade RM, Nguyen J, Jian T, Zhang Z, Gillespie JR, Buckner FS, Verlinde CL, Fan E, Hol WG.

Acta Crystallogr D Biol Crystallogr. 2015 Aug;71(Pt 8):1684-98. doi: 10.1107/S1399004715007683. Epub 2015 Jul 31.

15.

Three-dimensional structures in the design of therapeutics targeting parasitic protozoa: reflections on the past, present and future.

Hol WG.

Acta Crystallogr F Struct Biol Commun. 2015 May;71(Pt 5):485-99. doi: 10.1107/S2053230X15004987. Epub 2015 Apr 16. Review.

16.

Identification of potent inhibitors of the Trypanosoma brucei methionyl-tRNA synthetase via high-throughput orthogonal screening.

Pedró-Rosa L, Buckner FS, Ranade RM, Eberhart C, Madoux F, Gillespie JR, Koh CY, Brown S, Lohse J, Verlinde CL, Fan E, Bannister T, Scampavia L, Hol WG, Spicer T, Hodder P.

J Biomol Screen. 2015 Jan;20(1):122-30. doi: 10.1177/1087057114548832. Epub 2014 Aug 27. Erratum in: J Biomol Screen. 2016 Jul;21(6):653.

17.

Comparison of histidine recognition in human and trypanosomatid histidyl-tRNA synthetases.

Koh CY, Wetzel AB, de van der Schueren WJ, Hol WG.

Biochimie. 2014 Nov;106:111-20. doi: 10.1016/j.biochi.2014.08.005. Epub 2014 Aug 20.

18.

Crystal structure of the full-length ATPase GspE from the Vibrio vulnificus type II secretion system in complex with the cytoplasmic domain of GspL.

Lu C, Korotkov KV, Hol WGJ.

J Struct Biol. 2014 Sep;187(3):223-235. doi: 10.1016/j.jsb.2014.07.006. Epub 2014 Aug 1.

19.

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.

PLoS Negl Trop Dis. 2014 Apr 17;8(4):e2775. doi: 10.1371/journal.pntd.0002775. eCollection 2014 Apr.

20.

Neospora caninum calcium-dependent protein kinase 1 is an effective drug target for neosporosis therapy.

Ojo KK, Reid MC, Kallur Siddaramaiah L, Müller J, Winzer P, Zhang Z, Keyloun KR, Vidadala RS, Merritt EA, Hol WG, Maly DJ, Fan E, Van Voorhis WC, Hemphill A.

PLoS One. 2014 Mar 28;9(3):e92929. doi: 10.1371/journal.pone.0092929. eCollection 2014.

21.

A general protocol for the generation of Nanobodies for structural biology.

Pardon E, Laeremans T, Triest S, Rasmussen SG, Wohlkönig A, Ruf A, Muyldermans S, Hol WG, Kobilka BK, Steyaert J.

Nat Protoc. 2014 Mar;9(3):674-93. doi: 10.1038/nprot.2014.039. Epub 2014 Feb 27.

22.

Potent and selective inhibitors of CDPK1 from T. gondii and C. parvum based on a 5-aminopyrazole-4-carboxamide scaffold.

Zhang Z, Ojo KK, Vidadala R, Huang W, Geiger JA, Scheele S, Choi R, Reid MC, Keyloun KR, Rivas K, Siddaramaiah LK, Comess KM, Robinson KP, Merta PJ, Kifle L, Hol WG, Parsons M, Merritt EA, Maly DJ, Verlinde CL, Van Voorhis WC, Fan E.

ACS Med Chem Lett. 2014 Jan 9;5(1):40-44.

23.

Functional and structural characterization of Vibrio cholerae extracellular serine protease B, VesB.

Gadwal S, Korotkov KV, Delarosa JR, Hol WG, Sandkvist M.

J Biol Chem. 2014 Mar 21;289(12):8288-98. doi: 10.1074/jbc.M113.525261. Epub 2014 Jan 23.

24.

Hexamers of the type II secretion ATPase GspE from Vibrio cholerae with increased ATPase activity.

Lu C, Turley S, Marionni ST, Park YJ, Lee KK, Patrick M, Shah R, Sandkvist M, Bush MF, Hol WG.

Structure. 2013 Sep 3;21(9):1707-17. doi: 10.1016/j.str.2013.06.027. Epub 2013 Aug 15.

25.

The structure of the D3 domain of Plasmodium falciparum myosin tail interacting protein MTIP in complex with a nanobody.

Khamrui S, Turley S, Pardon E, Steyaert J, Fan E, Verlinde CL, Bergman LW, Hol WG.

Mol Biochem Parasitol. 2013 Aug;190(2):87-91. doi: 10.1016/j.molbiopara.2013.06.003. Epub 2013 Jul 4.

PMID:
23831371
26.

The compact conformation of the Plasmodium knowlesi myosin tail interacting protein MTIP in complex with the C-terminal helix of myosin A.

Turley S, Khamrui S, Bergman LW, Hol WG.

Mol Biochem Parasitol. 2013 Aug;190(2):56-9. doi: 10.1016/j.molbiopara.2013.06.004. Epub 2013 Jul 4.

27.

A dodecameric ring-like structure of the N0 domain of the type II secretin from enterotoxigenic Escherichia coli.

Korotkov KV, Delarosa JR, Hol WGJ.

J Struct Biol. 2013 Sep;183(3):354-362. doi: 10.1016/j.jsb.2013.06.013. Epub 2013 Jun 29.

28.

Crystal structures of Plasmodium falciparum cytosolic tryptophanyl-tRNA synthetase and its potential as a target for structure-guided drug design.

Koh CY, Kim JE, Napoli AJ, Verlinde CL, Fan E, Buckner FS, Van Voorhis WC, Hol WG.

Mol Biochem Parasitol. 2013 May;189(1-2):26-32. doi: 10.1016/j.molbiopara.2013.04.007. Epub 2013 May 7.

29.

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.

Antimicrob Agents Chemother. 2013 Jul;57(7):3021-8. doi: 10.1128/AAC.02578-12. Epub 2013 Apr 15.

30.

Crystal structure of the pilotin from the enterohemorrhagic Escherichia coli type II secretion system.

Korotkov KV, Hol WG.

J Struct Biol. 2013 May;182(2):186-91. doi: 10.1016/j.jsb.2013.02.013. Epub 2013 Feb 28.

31.

Structure of a low-melting-temperature anti-cholera toxin: llama V(H)H domain.

Legler PM, Zabetakis D, Anderson GP, Lam A, Hol WG, Goldman ER.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2013 Feb 1;69(Pt 2):90-3. doi: 10.1107/S1744309112050750. Epub 2013 Jan 26.

32.

Structure of the prolyl-tRNA synthetase from the eukaryotic pathogen Giardia lamblia.

Larson ET, Kim JE, Napuli AJ, Verlinde CL, Fan E, Zucker FH, Van Voorhis WC, Buckner FS, Hol WG, Merritt EA.

Acta Crystallogr D Biol Crystallogr. 2012 Sep;68(Pt 9):1194-200. doi: 10.1107/S0907444912024699. Epub 2012 Aug 18.

33.

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

Koh CY, Kim JE, Shibata S, Ranade RM, Yu M, Liu J, Gillespie JR, Buckner FS, Verlinde CL, Fan E, Hol WG.

Structure. 2012 Oct 10;20(10):1681-91. doi: 10.1016/j.str.2012.07.011. Epub 2012 Aug 16.

34.

Explorations of linked editosome domains leading to the discovery of motifs defining conserved pockets in editosome OB-folds.

Park YJ, Hol WG.

J Struct Biol. 2012 Nov;180(2):362-73. doi: 10.1016/j.jsb.2012.07.012. Epub 2012 Aug 10.

35.

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

Shibata S, Gillespie JR, Ranade RM, Koh CY, Kim JE, Laydbak JU, Zucker FH, Hol WG, Verlinde CL, Buckner FS, Fan E.

J Med Chem. 2012 Jul 26;55(14):6342-51. doi: 10.1021/jm300303e. Epub 2012 Jul 11.

36.

The structure of the C-terminal domain of the largest editosome interaction protein and its role in promoting RNA binding by RNA-editing ligase L2.

Park YJ, Budiarto T, Wu M, Pardon E, Steyaert J, Hol WG.

Nucleic Acids Res. 2012 Aug;40(14):6966-77. doi: 10.1093/nar/gks369. Epub 2012 May 4.

37.

The type II secretion system: biogenesis, molecular architecture and mechanism.

Korotkov KV, Sandkvist M, Hol WG.

Nat Rev Microbiol. 2012 Apr 2;10(5):336-51. doi: 10.1038/nrmicro2762. Review.

38.

Crystal structure of GAP50, the anchor of the invasion machinery in the inner membrane complex of Plasmodium falciparum.

Bosch J, Paige MH, Vaidya AB, Bergman LW, Hol WG.

J Struct Biol. 2012 Apr;178(1):61-73. doi: 10.1016/j.jsb.2012.02.009. Epub 2012 Feb 22.

39.

Multiple determinants for selective inhibition of apicomplexan calcium-dependent protein kinase CDPK1.

Larson ET, Ojo KK, Murphy RC, Johnson SM, Zhang Z, Kim JE, Leibly DJ, Fox AM, Reid MC, Dale EJ, Perera BG, Kim J, Hewitt SN, Hol WG, Verlinde CL, Fan E, Van Voorhis WC, Maly DJ, Merritt EA.

J Med Chem. 2012 Mar 22;55(6):2803-10. doi: 10.1021/jm201725v. Epub 2012 Mar 13.

40.

Crystal structure of a heterodimer of editosome interaction proteins in complex with two copies of a cross-reacting nanobody.

Park YJ, Pardon E, Wu M, Steyaert J, Hol WG.

Nucleic Acids Res. 2012 Feb;40(4):1828-40. doi: 10.1093/nar/gkr867. Epub 2011 Oct 27.

41.

Structural and functional studies on the interaction of GspC and GspD in the type II secretion system.

Korotkov KV, Johnson TL, Jobling MG, Pruneda J, Pardon E, Héroux A, Turley S, Steyaert J, Holmes RK, Sandkvist M, Hol WG.

PLoS Pathog. 2011 Sep;7(9):e1002228. doi: 10.1371/journal.ppat.1002228. Epub 2011 Sep 8.

42.

Screening a fragment cocktail library using ultrafiltration.

Shibata S, Zhang Z, Korotkov KV, Delarosa J, Napuli A, Kelley AM, Mueller N, Ross J, Zucker FH, Buckner FS, Merritt EA, Verlinde CL, Van Voorhis WC, Hol WG, Fan E.

Anal Bioanal Chem. 2011 Sep;401(5):1585-91. doi: 10.1007/s00216-011-5225-7. Epub 2011 Jul 13.

43.

Secretins: dynamic channels for protein transport across membranes.

Korotkov KV, Gonen T, Hol WG.

Trends Biochem Sci. 2011 Aug;36(8):433-43. doi: 10.1016/j.tibs.2011.04.002. Epub 2011 May 11. Review.

44.

The double-length tyrosyl-tRNA synthetase from the eukaryote Leishmania major forms an intrinsically asymmetric pseudo-dimer.

Larson ET, Kim JE, Castaneda LJ, Napuli AJ, Zhang Z, Fan E, Zucker FH, Verlinde CL, Buckner FS, Van Voorhis WC, Hol WG, Merritt EA.

J Mol Biol. 2011 Jun 3;409(2):159-76. doi: 10.1016/j.jmb.2011.03.026. Epub 2011 Mar 21.

45.

The binding of cholera toxin to the periplasmic vestibule of the type II secretion channel.

Reichow SL, Korotkov KV, Gonen M, Sun J, Delarosa JR, Hol WG, Gonen T.

Channels (Austin). 2011 May-Jun;5(3):215-8. Epub 2011 May 1.

46.

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.

Antimicrob Agents Chemother. 2011 May;55(5):1982-9. doi: 10.1128/AAC.01796-10. Epub 2011 Jan 31.

47.

Crystal structures of three protozoan homologs of tryptophanyl-tRNA synthetase.

Merritt EA, Arakaki TL, Gillespie R, Napuli AJ, Kim JE, Buckner FS, Van Voorhis WC, Verlinde CL, Fan E, Zucker F, Hol WG.

Mol Biochem Parasitol. 2011 May;177(1):20-8. doi: 10.1016/j.molbiopara.2011.01.003. Epub 2011 Jan 19.

48.

In vivo cross-linking of EpsG to EpsL suggests a role for EpsL as an ATPase-pseudopilin coupling protein in the Type II secretion system of Vibrio cholerae.

Gray MD, Bagdasarian M, Hol WG, Sandkvist M.

Mol Microbiol. 2011 Feb;79(3):786-98. doi: 10.1111/j.1365-2958.2010.07487.x.

49.

Oligomerization of EpsE coordinates residues from multiple subunits to facilitate ATPase activity.

Patrick M, Korotkov KV, Hol WG, Sandkvist M.

J Biol Chem. 2011 Mar 25;286(12):10378-86. doi: 10.1074/jbc.M110.167031. Epub 2011 Jan 5.

50.

Structure determination of glycogen synthase kinase-3 from Leishmania major and comparative inhibitor structure-activity relationships with Trypanosoma brucei GSK-3.

Ojo KK, Arakaki TL, Napuli AJ, Inampudi KK, Keyloun KR, Zhang L, Hol WG, Verlinde CL, Merritt EA, Van Voorhis WC.

Mol Biochem Parasitol. 2011 Apr;176(2):98-108. doi: 10.1016/j.molbiopara.2010.12.009. Epub 2010 Dec 30.

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