J4-5529 — Annual report 2015
1.
Nitroxoline impairs tumor progression in vitro and in vivo by regulating cathepsin B activity

Cathepsin B been shown to be involved in cancer progression. We reported an established antibiotic nitroxoline as a potent and selective inhibitor of cathepsin and elucidated its anti-tumor properties in in vitro and in vivo tumor models. Nitroxoline significantly abrogated tumor growth, angiogenesis and metastasis in vivo in LPB fibrosarcoma and MMTV-PyMT breast cancer mouse models. Overall, our results designate nitroxoline as a promising drug candidate for anti-cancer treatment.

COBISS.SI-ID: 3834225
2.
Lysosomal cysteine peptidases - molecules signaling tumor cell death and survival

Lysosomal cysteine peptidases - cysteine cathepsins - are general intracellular protein-degrading enzymes that control also a variety of specific physiological processes. They can trigger irreversible events leading to signal transduction and activation of signaling pathways, resulting in cell survival and proliferation or cell death. In cancer cells, lysosomal cysteine peptidases are involved in multiple processes during malignant progression.

COBISS.SI-ID: 3908977
3.
Inhibition of endopeptidase and exopeptidase activity of cathepsin B impairs extracellular matrix degradation and tumour invasion

By using specific inhibitors of endopeptidase and exopeptidase activity of cathepsin B, developed on the basis of the structure of nitroxoline, we demonstrted that both mentioned activities are needed for the development of malignant diseases, what partially changes our paradigm on the role of cathepsin B in cancer.

COBISS.SI-ID: 3979633