Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Proteinase-Activated Receptor-4

  • Anke Rattenholl
  • Tobias Görge
  • Stefan W. Schneider
  • Martin Steinhoff
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_4809-2

Synonyms

Definition

PAR4 is a G-protein-coupled receptor which can be activated by thrombin (factor IIa), plasmin, trypsin, and cathepsin G. It consists of 385 amino acids (41 kDa), including the amino-terminal signal sequence, and is widely expressed in various tissues. It is not expressed in the brain, kidney, spinal cord, and peripheral blood leukocytes. The gene maps to 19p2 (gene name: F2RL3).

Characteristics

PAR4 is activated by specific proteolysis at the site PAPR47 ↓ G48YPGQV to expose the tethered ligand GYPGKV which binds to the second extracellular loop, thus activating the receptor. A synthetic peptide (“activating peptide”) that mimics the tethered ligand domain (GYPGQV-NH2) directly binds to and activates PAR4 in vitro without proteolytic cleavage. PAR4 does not carry a hirudin-like binding site for thrombin as observed in PAR1 and PAR3. Thus, PAR4is a low-affinity receptor for thrombin. Despite this...

Keywords

Spinal Cord Squamous Cell Carcinoma Squamous Cell Cellular Response Signal Sequence 
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
    • 4
  1. 1.Applied Biotechnology Division, Department of Engineering and MathematicsBielefeldGermany
  2. 2.Department of DermatologyUniversity of MünsterMünsterGermany
  3. 3.Hauttumorzentrum Mannheim (HTZM)Universitätsmedizn MannheimMannheimGermany
  4. 4.UCD Charles Institute of DermatologyUniversity College DublinBelfieldIreland