Category: Janetka Publications

Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology.

Damalanka V.C., Han Z., Karmakar P., O’Donoghue A.J., La Greca F., Kim T., Pant S., Helander J., Klefström J., Craik C.S., & Janetka J.W. (2019). “Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology.” J Med Chem. 2019 Jan 24;62(2):480-490. doi: 10.1021/acs.jmedchem.8b01536. Epub 2019 Jan 4. (Abstract)

Hepatocyte growth factor activator inhibitor-2 stabilizes Epcam and maintains epithelial organization in the mouse intestine.

Kawaguchi M., Yamamoto K., Takeda N., Fukushima T., Yamashita F., Sato K., Kitamura K., Hippo Y., Janetka J.W., & Kataoka H. (2019). “Hepatocyte growth factor activator inhibitor-2 stabilizes Epcam and maintains epithelial organization in the mouse intestine.” Commun Biol. 2019 Jan 4;2:11. doi: 10.1038/s42003-018-0255-8. eCollection 2019. (Abstract)

Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics.

Tyagi R., Maddirala A.R., Elfawal M., Fischer C., Bulman C.A., Rosa B.A., Gao X., Chugani R., Zhou M., Helander J., Brindley P.J., Tseng C.C., Greig I.R., Sakanari J., Wildman S.A., Aroian R., Janetka J.W., & Mitreva M. (2018). “Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics.” ACS Infect Dis. 2018 Jul 13;4(7):1130-1145. doi: 10.1021/acsinfecdis.8b00090. Epub 2018 May 14. (Abstract)

MFN2 agonists reverse mitochondrial defects in preclinical models of Charcot-Marie-Tooth disease type 2A.

Rocha A.G., Franco A., Krezel A.M., Rumsey J.M., Alberti J.M., Knight W.C., Biris N., Zacharioudakis E., Janetka J.W., Baloh R.H., Kitsis R.N., Mochly-Rosen D., Townsend R.R., Gavathiotis E., & Dorn G.W. 2nd (2018). “MFN2 agonists reverse mitochondrial defects in preclinical models of Charcot-Marie-Tooth disease type 2A.” Science. 2018 Apr 20;360(6386):336-341. doi: 10.1126/science.aao1785. (Abstract)

Structure-based discovery of glycomimetic FmlH ligands as inhibitors of bacterial adhesion during urinary tract infection.

Kalas V., Hibbing M.E., Maddirala A.R., Chugani R., Pinkner J.S., Mydock-McGrane L.K., Conover M.S., Janetka J.W., & Hultgren S.J. (2018). “Structure-based discovery of glycomimetic FmlH ligands as inhibitors of bacterial adhesion during urinary tract infection.” Proc Natl Acad Sci U S A. 2018 Mar 5. pii: 201720140. doi: 10.1073/pnas.1720140115. (Abstract)

Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.

Yang B., Vasbinder M., Hird A.W., Su Q., Wang H., Yu Y., Toader D., Lyne P.D., Read J.A., Breed J., Ioannidis S., Deng C., Grondine M., DeGrace N., Whitston D., Brassil P., & Janetka J.W. (2018). “Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors.” J Med Chem. doi: 10.1021/acs.jmedchem.7b01490. (Abstract)

Inhibition of calcium dependent protein kinase 1 (CDPK1) by pyrazolopyrimidine analogs decreases establishment and reoccurrence of central nervous system disease by Toxoplasma gondii.

Rutaganira F.U., Barks J., Dhason M.S., Wang Q., Lopez M.S., Long S., Radke J.B., Jones N.G., Maddirala A.R., Janetka J.W., El Bakkouri M., Hui R., Shokat K.M., & Sibley L.D. (2017). “Inhibition of calcium dependent protein kinase 1 (CDPK1) by pyrazolopyrimidine analogs decreases establishment and reoccurrence of central nervous system disease by Toxoplasma gondii.” J Med Chem. 2017 Dec 28;60(24):9976-9989. doi: 10.1021/acs.jmedchem.7b01192. Epub 2017 Oct 9. (Abstract)

Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist.

Spaulding C.N., Klein R.D., Ruer S., Kau A.L., Schreiber H.L., Cusumano Z.T., Dodson K.W., Pinkner J.S., Fremont D.H., Janetka J.W., Remaut H., Gordon J.I., & Hultgren S.J. (2017). “Selective depletion of uropathogenic E. coli from the gut by a FimH antagonist.” Nature. 2017 Jun 22;546(7659):528-532. doi: 10.1038/nature22972. Epub 2017 Jun 14. (Abstract)