Category: Janetka Publications

A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells

Matthew Mahoney, Vishnu C. Damalanka, Michael A. Tartell, Dong Hee Chung, André Luiz Lourenco, Dustin Pwee, Anne E. Mayer Bridwell, Markus Hoffmann, Jorine Voss, Partha Karmakar, Nurit Azouz, Andrea M. Klingler, Paul W. Rothlauf, Cassandra E. Thompson, Melody Lee, Lidija Klampfer, Christina Stallings, Marc E. Rothenberg, Stefan Pöhlmann, Sean P. Whelan, Anthony J. O’Donoghue, Charles S. Craik, & James W. Janetka (2021). “A novel class of TMPRSS2 inhibitors potently block SARS-CoV-2 and MERS-CoV viral entry and protect human epithelial lung cells” Proc Natl Acad Sci U S A. 2021 Oct 26;118(43):e2108728118. doi: 10.1073/pnas.2108728118. (Abstract)

A host receptor enables type 1 pilus-mediated pathogenesis of Escherichia coli pyelonephritis

Lisa K. McLellan, Michael R. McAllaster, Arthur S. Kim, Ľubomíra Tóthová, Patrick D. Olson, Jerome S. Pinkner, Allyssa L. Daugherty, Teri N. Hreha, James W. Janetka, Daved H. Fremont, Scott J. Hultgren, Herbert W. Virgin, & David A Hunstad (2021). “A host receptor enables type 1 pilus-mediated pathogenesis of Escherichia coli pyelonephritis” PLoS Pathog. 2021 Jan 29;17(1):e1009314. doi: 10.1371/journal.ppat.1009314. eCollection 2021 Jan. (Abstract)

An Integrated Approach to Identify New Anti-Filarial Leads to Treat River Blindness, a Neglected Tropical Disease

Rahul Tyagi, Christina A. Bulman, Fidelis Cho-Ngwa, Chelsea Fischer, Chris Marcellino, Michelle R. Arkin, James H. McKerrow, Case W. McNamara, Matthew Mahoney, Nancy Tricoche, Shabnam Jawahar, James W. Janetka, Sara Lustigman, Judy Sakanari, & Makedonka Mitreva (2021). “An Integrated Approach to Identify New Anti-Filarial Leads to Treat River Blindness, a Neglected Tropical Disease” Pathogens. 2021 Jan 14;10(1):71. doi: 10.3390/pathogens10010071. (Abstract)

Novel approaches to glycomimetic design: Development of small molecular weight lectin antagonists

Vishnu C. Damalanka, Amarendar Reddy Maddirala, & James W. Janetka (2020). “Novel approaches to glycomimetic design: Development of small molecular weight lectin antagonists” Expert Opin Drug Discov. 2020 Dec 18. doi: 10.1080/17460441.2021.1857721. Online ahead of print. (Abstract)

Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis

James W Janetka, Allen T Hopper, Ziping Yang, Jennifer Barks, Mary Savari Dhason, Qiuling Wang, & L David Sibley (2020). “Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis” J Med Chem. 2020 Jun 11;63(11):6144-6163. doi: 10.1021/acs.jmedchem.0c00419. Epub 2020 Jun 1. (Abstract)

Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).

Yang B., Hird A.W., Bodnarchuk M.S., Zheng X., Dakin L., Su Q., Daly K., Godin R., Hattersley M.M., Brassil P., Redmond S., John Russell D., & Janetka J.W. (2020). “Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).” Bioorg Med Chem. 2020 Jan 15;28(2):115227. doi: 10.1016/j.bmc.2019.115227. Epub 2019 Dec 11. (Abstract)

Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics.

Tyagi R., Elfawal M.A., Wildman S.A., Helander J., Bulman C.A., Sakanari J., Rosa B.A., Brindley P.J., Janetka J.W., Aroian R.V., & Mitreva M. (2019). “Identification of small molecule enzyme inhibitors as broad-spectrum anthelmintics.” Sci Rep. 2019 Jun 24;9(1):9085. doi: 10.1038/s41598-019-45548-7. (Abstract)

Recent progress on inhibitors of the type II transmembrane serine proteases, hepsin, matriptase and matriptase-2.

Damalanka V.C. & Janetka J.W. (2019). “Recent progress on inhibitors of the type II transmembrane serine proteases, hepsin, matriptase and matriptase-2.” Future Med Chem. 2019 Apr;11(7):743-769. doi: 10.4155/fmc-2018-0446. Epub 2019 Apr 4. (Abstract)

Biphenyl Gal and GalNAc FmlH Lectin Antagonists of Uropathogenic E. coli (UPEC): Optimization through iterative rational drug design.

Maddirala A., Klein R.D., Pinkner J., Kalas V., Hultgren S.J., & Janetka J.W. (2019). “Biphenyl Gal and GalNAc FmlH Lectin Antagonists of Uropathogenic E. coli (UPEC): Optimization through iterative rational drug design.” J Med Chem. 2019 Jan 24;62(2):467-479. doi: 10.1021/acs.jmedchem.8b01561. Epub 2019 Jan 2. (Abstract)