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KGP-94 is a specific small molecule inhibitor of cathepsin-L (Cts-L), a lysosomal cysteine protease that is frequently upregulated in human cancers, including prostate cancer. Developed by researchers at the University of Florida, KGP-94 is designed to inhibit the metastatic phenotype of cancer cells by targeting secreted Cts-L, which is involved in the degradative proteolysis of the extracellular matrix and basement membrane. In preclinical studies using prostate cancer cell lines (PC-3 and its sublines), KGP-94 significantly reduced migratory and invasive potential and induced G1 cell cycle arrest without causing direct cytotoxicity. The compound specifically targets the secreted isoform rather than the nuclear isoform of the enzyme, suggesting its primary role is in blocking the physical processes of metastasis.
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