Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.

@article{Franco2015StructurebasedDO,
  title={Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.},
  author={Francisco M Franco and Darin E. Jones and P. Harris and Z. Han and S. Wildman and C. Jarvis and J. Janetka},
  journal={Bioorganic \& medicinal chemistry},
  year={2015},
  volume={23 10},
  pages={
          2328-43
        }
}
Hepatocyte growth factor activator (HGFA), matriptase and hepsin are all S1 trypsin-like serine endopeptidases. HGFA is a plasma protease while hepsin and matriptase are type II transmembrane proteases (TTSPs). Upregulated expression and activity of all three proteases is associated with aberrant cancer cell signaling through c-MET and RON tyrosine kinase cell-signaling pathways in cancer. We modeled known benzamidine protease inhibitor scaffolds into the active sites of matriptase, hepsin and… Expand
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