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--> Search for: Home Faculty Members Departmental Information Directories Giving Webmail Home Faculty Members Departmental Information Directories Giving Webmail Search for: James W. Janetka, Ph.D. Professor Biochemistry and Molecular Biophysics Publications (PubMed / NIH) Office: 2614 Cancer Research Phone: 314-362-0509 Email: [email protected] Research The Janetka research laboratory is broadly interested in the X-ray structure-based drug design, medicinal chemistry and organic synthesis of chemical tools and small molecule drugs. In multiple drug discovery projects, we are developing inhibitors of proteases, kinases, lectins, and other protein targets for studying and treating cancer and a variety of infectious disease. One project is targeting several serine proteases including HGFA and hepsin which activate growth factors and cytokines in tumors. Another project is working on inhibitors of transmembrane serine proteases such as TMPRSS2 and matriptase as broad-spectrum antiviral drugs. We have a project focused on aspartic protease inhibitors and GPCR antagonists as novel therapy for River Blindness, caused by parasitic filarial worm infections. We are also working on phosphodiesterase inhibitors as well as inhibitors of PIM kinase and others as new anthelmintic drugs to treat intestinal worm infections caused by whipworm and hookworm. Further studies are directed on the rational design of CDPK1 kinase inhibitors as novel drugs to treat acute and cure chronic Toxoplasmosis. Finally, a large research effort is dedicated to the structure-guided design of glycomimetic lectin antagonists such as PapG as innovative antivirulence therapeutics for the treatment and prevention of bacterial infections and in one project targeting Fap2 for colon cancer. Select Patents Compounds and methods for treating bacterial infections (US Patent # 20180194792) Inhibitors of growth factor activation enzymes (US Patent # 20180066015) Select Books Extracellular Targeting of Cell Signaling in Cancer: Strategies Directed at MET and RON Receptor Tyrosine Kinase Pathways, available from the publisher (Wiley), Amazon, Barnes &＃038; Noble, and other bookstores. Select Publications Vishnu C Damalanka, Victoria Banas, Paolo De Bona, Maithri M Kashipathy, Kevin Battaile, Scott Lovell, James W Janetka (2024). &＃8220;Mechanism-Based Macrocyclic Inhibitors of Serine Proteases&＃8221; J Med Chem. 2024 Mar 28;67(6):4833-4854. doi: 10.1021/acs.jmedchem.3c02388. Epub 2024 Mar 13. (Abstract) Robert Obermann, Bereket Yemane, Cassie Jarvis, Francisco M Franco, Yevhenii Kyriukha, William Nolan, Beth Gohara, Andrzej M Krezel, Scott A Wildman &＃038; James W Janetka (2024). &＃8220;Small Molecule Antagonists of the DNA Repair ERCC1/XPA Protein-Protein Interaction&＃8221; ChemMedChem. 2024 Apr 16;19(8):e202300648. doi: 10.1002/cmdc.202300648. Epub 2024 Mar 5. (Abstract) Adrianus C M Boon, Traci L Bricker, Ethan J Fritch, Sarah R Leist, Kendra Gully, Ralph S Baric, Rachel L Graham, Brigid V Troan, Matthew Mahoney &＃038; James W Janetka (2024). &＃8220;Efficacy of Host Cell Serine Protease Inhibitor MM3122 against SARS-CoV-2 for Treatment and Prevention of COVID-19&＃8221; bioRxiv. [Preprint]. 2024 Feb 12:2024.02.09.579701. doi: 10.1101/2024.02.09.579701.. (Abstract) Amarendar Reddy Maddirala, Kevin Tamadonfar, Jerome S Pinkner, Denise Sanick, Scott J Hultgren &＃038; James W Janetka (2024). &＃8220;Discovery of Orally Bioavailable FmlH Lectin Antagonists as Treatment for Urinary Tract Infections&＃8221; J Med Chem. 2024 Mar 14;67(5):3668-3678. doi: 10.1021/acs.jmedchem.3c02128. Epub 2024 Feb 3. (Abstract) Alpha Raj Mekapogu, Zhihong Xu, Srinivasa Pothula, Chamini Perera, Tony Pang, S M Zahid Hosen, Vishnu Damalanka, James Janetka, David Goldstein, Romano Pirola, Jeremy Wilson &＃038; Minoti Apte (2023). &＃8220;HGF/c-Met pathway inhibition combined with chemotherapy increases cytotoxic T-cell infiltration and inhibits pancreatic tumour growth and metastasis&＃8221; Cancer Lett. 2023 Aug 1:568:216286. doi: 10.1016/j.canlet.2023.216286. Epub 2023 Jun 22. (Abstract) Denis Belitškin, Pauliina Munne, Shishir M Pant, Johanna M Anttila, Ilida Suleymanova, Kati Belitškina, Daniel Kirchhofer, James Janetka, Taivo Käsper, Sami Jalil, Jeroen Pouwels, Topi A Tervonen &＃038; Juha Klefström (2024). &＃8220;Hepsin promotes breast tumor growth signaling via the TGFβ-EGFR axis&＃8221; Mol Oncol. 2024 Mar;18(3):547-561. doi: 10.1002/1878-0261.13545. Epub 2023 Nov 13. (Abstract) Vivian Truong Jones, Ramona Graves-Deal, Zheng Cao, Galina Bogatcheva, Marisol A Ramirez, Sarah J Harmych, James N Higginbotham, Vineeta Sharma, Vishnu C Damalanka, Claudia C Wahoski, Neeraj Joshi, Maria Johnson Irudayam, Joseph T Roland, Gregory D Ayers, Qi Liu, Robert J Coffey, James W Janetka &＃038; Bhuminder Singh (2024). &＃8220;Inhibition of autocrine HGF maturation overcomes cetuximab resistance in colorectal cancer&＃8221; Cell Mol Life Sci. 2024 Jan 12;81(1):28. doi: 10.1007/s00018-023-05071-5. (Abstract) Alpha Raj Mekapogu, Zhihong Xu, Srinivasa Pothula, Chamini Perera, Tony Pang, S M Zahid Hosen, Vishnu Damalanka, James Janetka, David Goldstein, Romano Pirola, Jeremy Wilson &＃038; Minoti Apte (2023). &＃8220;HGF/c-Met pathway inhibition combined with chemotherapy increases cytotoxic T-cell infiltration and inhibits pancreatic tumour growth and metastasis&＃8221; Cancer Lett. 2023 Aug 1:568:216286. doi: 10.1016/j.canlet.2023.216286. Epub 2023 Jun 22. (Abstract) Denis Belitškin, Pauliina Munne, Shishir M Pant, Johanna M Anttila, Ilida Suleymanova, Kati Belitškina, Daniel Kirchhofer, James Janetka, Taivo Käsper, Sami Jalil, Jeroen Pouwels, Topi A Tervonen & Juha Klefström (2024). &＃8220;Hepsin promotes breast tumor growth signaling via the TGFβ-EGFR axis&＃8221; Mol Oncol. 2024 Mar;18(3):547-561. doi: 10.1002/1878-0261.13545. Epub 2023 Nov 13. (Abstract) Vivian Truong Jones, Ramona Graves-Deal, Zheng Cao, Galina Bogatcheva, Marisol A Ramirez, Sarah J Harmych, James N Higginbotham, Vineeta Sharma, Vishnu C Damalanka, Claudia C Wahoski, Neeraj Joshi, Maria Johnson Irudayam, Joseph T Roland, Gregory D Ayers, Qi Liu, Robert J Coffey, James W Janetka &＃038; Bhuminder Singh (2024). &＃8220;Inhibition of autocrine HGF maturation overcomes cetuximab resistance in colorectal cancer&＃8221; Cell Mol Life Sci. 2024 Jan 12;81(1):28. doi: 10.1007/s00018-023-05071-5. (Abstract) Robert Obermann, Bereket Yemane, Cassie Jarvis, Francisco M Franco, Yevhenii Kyriukha, William Nolan, Beth Gohara, Andrzej M Krezel, Scott A Wildman & James W Janetka (2024). &＃8220;Small Molecule Antagonists of the DNA Repair ERCC1/XPA Protein-Protein Interaction&＃8221; ChemMedChem. 2024 Feb 1:e202300648. doi: 10.1002/cmdc.202300648. Online ahead of print. (Abstract) Amarendar Reddy Maddirala, Kevin Tamadonfar, Jerome S Pinkner, Denise Sanick, Scott J Hultgren & James W Janetka (2024). &＃8220;Discovery of Orally Bioavailable FmlH Lectin Antagonists as Treatment for Urinary Tract Infections&＃8221; J Med Chem. 2024 Mar 14;67(5):3668-3678. doi: 10.1021/acs.jmedchem.3c02128. Epub 2024 Feb 3. (Abstract) Vishnu C Damalanka, Victoria Banas, Paolo De Bona, Maithri M Kashipathy, Kevin Battaile, Scott Lovell & James W Janetka (2024). &＃8220;Mechanism-Based Macrocyclic Inhibitors of Serine Proteases&＃8221; J Med Chem2024 Mar 28;67(6):4833-4854. doi: 10.1021/acs.jmedchem.3c02388. Epub 2024 Mar 13. (Abstract) Adrianus C. M. Boon, Traci L. Bricker, Ethan J. Fritch, Sarah R. Leist, Kendra Gully, Ralph S. Baric, Rachel L. Graham, Brigid V. Troan, Matthew Mahoney & James W. Janetka (2024). &＃8220;Efficacy of host cell serine protease inhibitor MM3122 against SARS-CoV-2 for treatment and prevention of COVID-19.&＃8221; J Virol. 2024 Apr;9. doi:10.1128/jvi.01903-23 (Abstract) Liana Beld, Hyeim Jung, Christina A. Bulman, Bruce A. Rosa, Peter U. Fischer, James W. Janetka, Sara Lustigman, Judy A. Sakanari, and Makedonka Mitreva (2022). &＃8220;Aspartyl Protease Inhibitors as Anti-Filarial Drugs&＃8221; Pathogens. 2022 Jun 18;11(6):707. doi: 10.3390/pathogens11060707. (Abstract) Home Member Directories Media and Newsletters News and Events Contact Us: Washington University School of Medicine Dept. of Biochemistry and Molecular Biophysics 660 S. Euclid Ave., Box 8231 St. Louis, MO 63110 Fax: 314-362-7183 Webmaster
