James Janetka, PhD

James Janetka, PhD

Primary Academic Title

Professor of Biochemistry and Molecular Biophysics, Washington University School of Medicine

Research Interest

The rational design and synthesis of small molecule and peptide-based chemical tools for studying cancer biology and as potential therapeutics. In particular, we are interested in understanding the molecular mechanisms of growth factor and kinase receptor regulation outside the cell by proteolytic enzymes as related to cell signaling, tumor progression and metastasis. We are currently focused on developing potent and selective inhibitors of the serine proteases HGFA, matriptase and hepsin. These proteases process and activate the growth factors HGF and MSP which regulate cell signaling of c-MET and RON, tyrosine kinases validated as key therapeutic targets in angiogenesis, cancer cell adhesion, invasion, motility and metastasis. We are studying the individual role and regulation of these proteases in metastatic breast cancer, ultimately aimed at developing non-kinase novel small molecule therapeutics. We utilize structure-based drug design (SBDD), medicinal chemistry, organic synthesis, biochemical, molecular biology and cell biology techniques.


  • 1996: PhD, organic chemistry, University of Wisconsin, Madison


  • 1996 - 1997: Fellow, medicinal chemistry, National Institutes of Health, Bethesda, Md.

Selected Research Publications

Small Molecule Antagonists of the DNA Repair ERCC1/XPA Protein-Protein Interaction.
  • Obermann R, Yemane B, Jarvis C, [...] Janetka JW
  • ChemMedChem 2024
Mechanism-Based Macrocyclic Inhibitors of Serine Proteases.
  • Damalanka VC, Banas V, De Bona P, [...] Janetka JW
  • J Med Chem 2024

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