The heparanase/syndecan-1 axis in cancer: mechanisms and therapies

FEBS J. 2013 May;280(10):2294-306. doi: 10.1111/febs.12168. Epub 2013 Mar 4.

Abstract

Heparanase is an endoglucuronidase that cleaves heparan sulfate chains of proteoglycans. In many malignancies, high heparanase expression and activity correlate with an aggressive tumour phenotype. A major consequence of heparanase action in cancer is a robust up-regulation of growth factor expression and increased shedding of syndecan-1 (a transmembrane heparan sulfate proteoglycan). Substantial evidence indicates that heparanase and syndecan-1 work together to drive growth factor signalling and regulate cell behaviours that enhance tumour growth, dissemination, angiogenesis and osteolysis. Preclinical and clinical studies have demonstrated that therapies targeting the heparanase/syndecan-1 axis hold promise for blocking the aggressive behaviour of cancer.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Biomimetic Materials / pharmacology
  • Cell Nucleus / enzymology
  • Cell Nucleus / pathology
  • Enzyme Activation
  • Enzyme Inhibitors / pharmacology
  • Exosomes / metabolism
  • Exosomes / pathology
  • Gene Expression Regulation, Neoplastic*
  • Glucuronidase / antagonists & inhibitors
  • Glucuronidase / metabolism*
  • Heparitin Sulfate / metabolism
  • Hepatocyte Growth Factor / metabolism
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / pathology
  • Signal Transduction
  • Syndecan-1 / genetics
  • Syndecan-1 / metabolism*

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • HGF protein, human
  • SDC1 protein, human
  • Syndecan-1
  • Hepatocyte Growth Factor
  • Heparitin Sulfate
  • heparanase
  • Glucuronidase