Category: Janetka Publications

Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.

Simpson C., Jones N.G., Hull-Ryde E.A., Kireev D., Stashko M., Tang K., Janetka J., Wildman S.A., Zuercher W.J., Schapira M., Hui R., Janzen W., & Sibley L.D. (2016). “Identification of small molecule inhibitors that block the Toxoplasma gondii rhoptry kinase ROP18.” ACS Infect Dis. 2016 Mar 11;2(3):194-206. Epub 2015 Dec 28. (Abstract)

Antivirulence Isoquinolone Mannosides: Optimization of the Biaryl Aglycone for FimH Lectin Binding Affinity and Efficacy in the Treatment of Chronic UTI.

Jarvis C., Han Z., Kalas V., Klein R., Pinkner J.S., Ford B., Binkley J., Cusumano C.K., Cusumano Z., Mydock-McGrane L., Hultren S.J., & Janetka J.W. (2016). “Antivirulence Isoquinolone Mannosides: Optimization of the Biaryl Aglycone for FimH Lectin Binding Affinity and Efficacy in the Treatment of Chronic UTI.” ChemMedChem. 2016 Feb 17;11(4):367-73. doi: 10.1002/cmdc.201600006. Epub 2016 Jan 26. (Abstract)

Mannose-derived FimH antagonists: a promising anti-virulence therapeutic strategy for urinary tract infections and Crohn’s disease.

Mydock-McGrane L.K., Cusumano Z.T., & Janetka J.W. (2016). “Mannose-derived FimH antagonists: a promising anti-virulence therapeutic strategy for urinary tract infections and Crohn’s disease.” Expert Opin Ther Pat. 2016;26(2):175-97. doi: 10.1517/13543776.2016.1131266. Epub 2016 Jan 22. (Abstract)

Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.

Franco F.M., Jones D.E., Harris P.K., Han Z., Wildman S.A., Jarvis C.M., & Janetka J.W. (2015). “Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.” Bioorg Med Chem. 2015 May 15;23(10):2328-43. doi: 10.1016/j.bmc.2015.03.072. Epub 2015 Apr 4. (Abstract)

Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.

Han Z., Harris P.K., Jones D.E., Chugani R., Kim T., Agarwal M., Shen W., Wildman S.A., & Janetka J.W. (2014). “Inhibitors of HGFA, Matriptase, and Hepsin Serine Proteases: A Nonkinase Strategy to Block Cell Signaling in Cancer.” ACS Med Chem Lett. 2014 Oct 9;5(11):1219-24. doi: 10.1021/ml500254r. eCollection 2014 Nov 13. (Abstract)

A FimH inhibitor prevents acute bladder infection and treats chronic cystitis caused by multidrug-resistant uropathogenic Escherichia coli ST131.

Totsika M., Kostakioti M., Hannan T.J., Upton M., Beatson S.A., Janetka J.W., Hultgren S.J., & Schembri M.A. (2013). “A FimH inhibitor prevents acute bladder infection and treats chronic cystitis caused by multidrug-resistant uropathogenic Escherichia coli ST131.” J Infect Dis. 2013 Sep;208(6):921-8. doi: 10.1093/infdis/jit245. Epub 2013 Jun 3. (Abstract)

Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.

Yang B., Hird A.W., Russell D.J., Fauber B.P., Dakin L.A., Zheng X., Su Q., Godin R., Brassil P., Devereaux E., and Janetka J.W. (2012) “Discovery of novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.” Bioorg Med Chem Lett. 2012 Jul 15;22(14):4907-11. doi: 10.1016/j.bmcl.2012.04.104. Epub 2012 Apr 30. (Abstract)

Combinatorial small-molecule therapy prevents uropathogenic Escherichia coli catheter-associated urinary tract infections in mice.

Guiton P.S., Cusumano C.K., Kline K.A., Dodson K.W., Han Z., Janetka J.W., Henderson J.P., Caparon M.G., & Hultgren S.J. (2012). “Combinatorial small-molecule therapy prevents uropathogenic Escherichia coli catheter-associated urinary tract infections in mice.” Antimicrob Agents Chemother. 2012 Sep;56(9):4738-45. doi: 10.1128/AAC.00447-12. Epub 2012 Jun 25.

Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.

Oza V., Ashwell S., Almeida L., Brassil P., Breed J., Deng C., Gero T., Grondine M., Horn C., Ioannidis S., Liu D., Lyne P., Newcombe N., Pass M., Read J., Ready S., Rowsell S., Su M., Toader D., Vasbinder M., Yu D., Yu Y., Xue Y., Zabludoff S., and Janetka J. (2012) “Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.” J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4. (Abstract)