Expression of proteinase-activated receptor 1-4 (PAR 1-4) in human cancer

J Mol Histol. 2010 Apr;41(2-3):89-99. doi: 10.1007/s10735-010-9274-6. Epub 2010 Jun 20.


Proteinase activated receptors (PAR 1-4) are membrane receptors with a unique way of activation by proteinases like thrombin, trypsin and matrix metalloproteinases which lead to a specific cellular response. To evaluate the significance of expression and co-expression of PAR in cancer we performed a survey on published data. A Pubmed literature search on "PAR, thrombin, cancer" was performed and 46 publications were selected for systematic review based on the availability of information on tumor type, material type, detection method and specification of positive cases. PAR-1 was found in 77.3% of malignant samples (n = 678), PAR-2 in 79.5% (n = 592), PAR-3 in 12.6% (n = 87) and PAR-4 in 54.9% (n = 153). PAR-1 and -2 were present in adenocarcinomas, melanomas, osteosarcomas, glioblastomas, meningiomas, leukaemias and squamous cell carcinomas. Presence of PAR-3 was limited to kidney and liver cancer. The data on PAR-4 expression was inconclusive. Those studies analysing PAR-1 and PAR-2 reported coexpression of the two receptors. PAR-1 and -2 are widely expressed in human tumors suggesting an important role in tumorigenesis and providing potential targets for therapy. PAR-3 and PAR-4 are less frequently detectable, their expression and potential role in tumorigenesis require further investigation.

Publication types

  • Review
  • Systematic Review

MeSH terms

  • Cell Line, Tumor
  • Humans
  • Neoplasms / metabolism*
  • Neoplasms / pathology
  • Receptor, PAR-1 / biosynthesis*
  • Receptor, PAR-2 / biosynthesis*
  • Receptors, Thrombin / biosynthesis*


  • Receptor, PAR-1
  • Receptor, PAR-2
  • Receptors, Thrombin
  • protease-activated receptor 3
  • protease-activated receptor 4