Cathepsin L targeting in cancer treatment

Pharmacol Ther. 2015 Nov;155:105-16. doi: 10.1016/j.pharmthera.2015.08.007. Epub 2015 Aug 20.


Proteolytic enzymes may serve as promising targets for novel therapeutic treatment strategies seeking to impede cancer progression and metastasis. One such enzyme is cathepsin L (CTSL), a lysosomal cysteine protease. CTSL upregulation, a common occurrence in a variety of human cancers, has been widely correlated with metastatic aggressiveness and poor patient prognosis. In addition, CTSL has been implicated to contribute to cancer-associated osteolysis, a debilitating morbidity affecting both life expectancy and the quality of life. In this review, we highlight the mechanisms by which CTSL contributes to tumor progression and dissemination and discuss the therapeutic utility of CTSL intervention strategies aimed at impeding metastatic progression and bone resorption.

Keywords: Bone resorption; Cancer; Cathepsin L; Metastasis; Protease targeting.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Cathepsin L / antagonists & inhibitors
  • Cathepsin L / metabolism*
  • Cysteine Proteinase Inhibitors / therapeutic use
  • Humans
  • Neoplasms / drug therapy
  • Neoplasms / metabolism*


  • Cysteine Proteinase Inhibitors
  • Cathepsin L