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Associated with tumor aggression, cathepsins are a family of proteases that are pivotal components of signaling pathways that can enhance cancer cell growth and inflammation. Within the human lysosomal cysteine cathepsin family, there are 11 members, including cathepsin B, L, S, and Plasmin. As a family, cysteine cathepsins are involved in the response to anticancer therapy within the tumor microenvironment and play crucial roles in the development of resistance to therapeutics. In particular, cathepsin B expression correlates with the invasive and metastatic capabilities of many tumors, such as in breast cancer where high expression levels of cathepsin B have been linked to highly aggressive tumors. Cathepsin B is also upregulated in a variety of inflammatory cells (including eosinophils, neutrophils, and macrophages).