ProteXase Therapeutics

Publications

Prior to establishing ProteXase Therapeutics, Robert Galemmo, James Janetka, and Lidija Klampfer collaborated on the Wiley book, Extracellular Targeting of Cell Signaling in Cancer: Strategies Directed at MET and RON Receptor Tyrosine Kinase Pathways. 


In addition to being the book editor, Dr Janetka wrote Chapter 9 “Inhibitors of the Growth-Factor Activating Proteases Matriptase, Hepsin and HGFA: Strategies for Rational Drug Design and Optimization” with Dr. Galemmo. While Dr. Klampfer and her colleague, Benjamin Yaw Owusu, contributed the book’s second chapter, “The Role of HGF/MET and MSP/RON Signaling in Tumor Progression and Resistance to Anticancer Therapy.”


A list of Drs. Galemmo, Janetka, and Klampfer other significant publications follow:


1. Piperidine Carbamate Peptidomimetic Inhibitors of the Serine Proteases HGFA, Matriptase and Hepsin. Damalanka, V. C., Wildman, S. A., Janetka, J.W., Med Chem Commun., 2019, 10, 1646–1655.


2. Recent progress on inhibitors of the type II transmembrane serine proteases, hepsin, matriptase and matriptase-2. Damalanka VC, Janetka JW., Future Med Chem. 2019 Apr;11(7):743-769.


3. 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 JW, Kataoka H., Commun Biol. 2019 Jan 4;2:11.


4. Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology. Damalanka VC, Han Z, Karmakar P, O'Donoghue AJ, La Greca F, Kim T, Pant SM, Helander J, Klefström J, Craik CS, Janetka JW., J Med Chem. 2019 Jan 24;62(2):480-490.


5. Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation. Owusu BY, Thomas S, Venukadasula P, Han Z, Janetka JW, Galemmo RA Jr, Klampfer L., Oncotarget. 2017 May 29;8(38):63014-63025.


6. Hepatocyte Growth Factor, a Key Tumor-Promoting Factor in the Tumor Microenvironment. Owusu BY, Galemmo R, Janetka J, Klampfer L., Cancers (Basel). 2017 Apr 17;9(4). pii: E35.


7. α-Ketobenzothiazole Serine Protease Inhibitors of Aberrant HGF/c-MET and MSP/RON Kinase Pathway Signaling in Cancer. Han Z, Harris PK, Karmakar P, Kim T, Owusu BY, Wildman SA, Klampfer L, Janetka JW., ChemMedChem. 2016 Mar 17;11(6):585-99.


8. Inhibition of pro-HGF activation by SRI31215, a novel approach to block oncogenic HGF/MET signaling. Owusu BY, Bansal N, Venukadasula PK, Ross LJ, Messick TE, Goel S, Galemmo RA, Klampfer L., Oncotarget. 2016 May 17;7(20):29492-506.


9. Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets. Franco FM, Jones DE, Harris PK, Han Z, Wildman SA, Jarvis CM, Janetka JW., Bioorg Med Chem. 2015 May 15;23(10):2328-43.


10. Design and Synthesis of Nonpeptide Inhibitors of Hepatocyte Growth Factor Activation. Venukadasula PK, Owusu BY, Bansal N, Ross LJ, Hobrath JV, Bao D, Truss JW, Stackhouse M, Messick TE, Klampfer L, Galemmo RA Jr., ACS Med Chem Lett. 2015 Dec 22;7(2):177-81.


11. Inhibitors of HGFA, matriptase and hepsin serine proteases: A non-kinase strategy to block cell signaling in cancer. Han, Z., Harris, P.K.W., Jones, D.E., Chugani, R., Kim, T., Agarwal, M., Shen, W., Wildman, S.A., Janetka, J.W. (2014) ACS Med. Chem. Lett., 5 (11), 1219-1224. 

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