• 2330 Citations
19952020

Research output per year

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Personal profile

Research interests

We are interested in the discovery and development of novel therapeutics for treatment and prevention of cancer and infectious disease. One aim of our current research focuses on the identification of unconventional allosteric inhibitors of the trypsin-like serine proteases, HGFA, matriptase, and hepsin. These proteases are up-regulated in many invasive cancers and regulate the activation of hepatocyte growth factor (HGF) and macrophage stimulating protein (MSP-1). Another aim of our research centers on the developing small-molecule antagonists of the UPEC bacterial adhesion protein FimH for the treatment of urinary tract infections (UTI).

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Research Output

  • 2330 Citations
  • 46 Article
  • 8 Review article

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., Jan 15 2020, In : Bioorganic and Medicinal Chemistry. 28, 2, 115227.

Research output: Contribution to journalArticle

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

    Janetka, J. W., Hopper, A. T., Yang, Z., Barks, J., Dhason, M. S., Wang, Q. & Sibley, L. D., Jun 11 2020, In : Journal of Medicinal Chemistry. 63, 11, p. 6144-6163 20 p.

    Research output: Contribution to journalArticle

  • Biphenyl Gal and GalNAc FmlH Lectin Antagonists of Uropathogenic E. coli (UPEC): Optimization through Iterative Rational Drug Design

    Maddirala, A. R., Klein, R., Pinkner, J. S., Kalas, V., Hultgren, S. J. & Janetka, J. W., Jan 24 2019, In : Journal of Medicinal Chemistry. 62, 2, p. 467-479 13 p.

    Research output: Contribution to journalArticle

  • 6 Scopus citations

    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. M., Helander, J., Klefström, J., Craik, C. S. & Janetka, J. W., Jan 24 2019, In : Journal of Medicinal Chemistry. 62, 2, p. 480-490 11 p.

    Research output: Contribution to journalArticle

  • 8 Scopus citations

    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., Dec 1 2019, In : Communications Biology. 2, 1, 11.

    Research output: Contribution to journalArticle

    Open Access
  • 5 Scopus citations