Fibroblast activation protein: A potential therapeutic target in cancer

Cancer Biol Ther. 2012 Feb 1;13(3):123-9. doi: 10.4161/cbt.13.3.18696. Epub 2012 Feb 1.


The concept of targeting antigens selectively expressed on the surface of tumor capillary endothelial cells or in tumor stroma has emerged as a promising strategy for cancer therapeutics. Identification of stromal targets for anticancer therapy and development of selective inhibitors of these targets are of great clinical interest. Fibroblast activation protein (FAP), a member of the serine protease family, selectively expressed in the stromal fibroblasts associated with epithelial cancers, whereas with low or undetectable expression in the resting fibroblasts of normal adult tissues. The proteolytic activity of FAP has been shown to support tumor growth and proliferation, making it a potential target for novel anticancer therapies, such as those by immune-based approaches.

Publication types

  • Review

MeSH terms

  • Animals
  • Antibodies, Monoclonal, Humanized / pharmacology
  • Antibodies, Monoclonal, Humanized / therapeutic use
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use
  • Clinical Trials as Topic
  • Endopeptidases
  • Extracellular Matrix / metabolism
  • Gelatinases / antagonists & inhibitors*
  • Gelatinases / metabolism
  • Humans
  • Membrane Proteins / antagonists & inhibitors*
  • Membrane Proteins / metabolism
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neoplasms / metabolism
  • Serine Endopeptidases / metabolism
  • Tumor Microenvironment


  • Antibodies, Monoclonal, Humanized
  • Antineoplastic Agents
  • Membrane Proteins
  • sibrotuzumab
  • Endopeptidases
  • Serine Endopeptidases
  • fibroblast activation protein alpha
  • Gelatinases