Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Proteinase-Activated Receptor 2

  • Anke Rattenholl
  • Tobias Görge
  • Stefan W. Schneider
  • Martin Steinhoff
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_4807-2

Synonyms

Definition

PAR2 is a G-protein-coupled receptor which can be activated by trypsin, tryptase, factor VIIa, factor Xa, matriptase (MT-SP1), and proteinase 3. It consists of 397 amino acids (44 kDa) including the amino-terminal signal sequence and is widely expressed in different tissues and upregulated in numerous cancers. The gene maps to 5q13.3 (gene name: F2RL1).

Characteristics

PAR2 is activated by specific proteolysis at the site SKGR36 ↓ S37LIGKV to expose the tethered ligand SLIGKV which binds to the second extracellular loop, thus activating the receptor, resulting in signal transduction. A synthetic peptide (“activating peptide”) that mimics the tethered ligand domain (SLIGKV-NH2) directly binds to and activates PAR2 in vitro without proteolytic cleavage. In vivo, PAR2 can also be stimulated by transactivation through PAR1: the tethered ligand domain of PAR1is able to...

Keywords

Vascular Endothelial Growth Factor Epidermal Growth Factor Receptor Pancreatic Cancer Squamous Cell Carcinoma Factor VIIa 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  • Anke Rattenholl
    • 1
  • Tobias Görge
    • 2
  • Stefan W. Schneider
    • 3
  • Martin Steinhoff
    • 2
  1. 1.Applied Biotechnology Division, Department of Engineering and MathematicsBielefeldGermany
  2. 2.UCD Charles Institute of DermatologyUniversity College DublinBelfieldIreland
  3. 3.Hauttumorzentrum Mannheim (HTZM)Universitätsmedizn MannheimMannheimGermany