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  • Review Article
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Review Article

Protease activated receptors: theme and variations

Oncogene volume 20, pages 1570–1581 (2001)Cite this article

Abstract

The four PAR family members are G protein coupled receptors that are normally activated by proteolytic exposure of an occult tethered ligand. Three of the family members are thrombin receptors. The fourth (PAR2) is not activated by thrombin, but can be activated by other proteases, including trypsin, tryptase and Factor Xa. This review focuses on recent information about the manner in which signaling through these receptors is initiated and terminated, including evidence for inter- as well as intramolecular modes of activation, and continuing efforts to identify additional, biologically-relevant proteases that can activate PAR family members.

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Acknowledgements

This work was supported by the NIH HLBI (HL40387).

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  1. Peter J O'Brien

    Present address: Department of Genetics, University of Pennsylvania, ARC 509, 3516 Civic Center Blvd., Philadelphia, 19104, PA, USA

  2. Mark Kahn

    Present address: Department of Medicine, University of Pennsylvania, 952 BRB II/III, 421 Curie Blvd, Philadelphia, 19104-6069, PA, USA

  3. Lawrence F Brass

    Present address: Departments of Medicine and Pharmacology, Center for Experimental Therapeutics, 913 BRB II/III, 421 Curie Blvd, Philadelphia, 19104-6069, PA, USA

Authors and Affiliations

  1. Department of Medicine, University of Pennsylvania, Philadelphia, 19104, Pennsylvania, PA, USA

    Peter J O'Brien, Mark Kahn & Lawrence F Brass

  2. Department of Pharmacology, University of Pennsylvania, Philadelphia, 19104, Pennsylvania, PA, USA

    Peter J O'Brien, Mark Kahn & Lawrence F Brass

  3. Center for Experimental Therapeutics at the University of Pennsylvania, Philadelphia, 19104, Pennsylvania, PA, USA

    Peter J O'Brien, Mark Kahn & Lawrence F Brass

  4. Istituto di Ricerche Farmacologiche Mario Negri, Consorzio Mario Negri Sud, Santa Maria Imbaro, Italy

    Marina Molino

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O'Brien, P., Molino, M., Kahn, M. et al. Protease activated receptors: theme and variations. Oncogene 20, 1570–1581 (2001). https://doi.org/10.1038/sj.onc.1204194

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