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Proteases and Their Receptors in Inflammation pp 291–303Cite as

Terminating Protease Receptor Signaling

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Part of the book series: Progress in Inflammation Research ((PIR))

Abstract

Signals generated by proteolytic activation of Protease-activated receptors (PARs) must be terminated to avoid uncontrolled cellular events, such as proliferation, cell migration, and inflammation. Because PARs are irreversibly activated, this is of paramount importance because, unlike most other GPCRs, the ligand cannot dissociate or diffuse away. Signal termination within the cell consists of a multi-step process involving desensitization and internalization of receptors. Furthermore, given the wealth of available proteases to activate these receptors, mechanisms exist to disarm these receptors extracellularly, rendering them insensitive to activation. In this chapter, the process of signal termination will be separated into: (1) Receptor uncoupling, in which we discuss intracellular and extracellular mechanisms of receptor desensitization, (2) Receptor Endocytosis, and (3) Termination of downstream signaling pathways. Discussion will focus on PAR1, PAR2, and PAR4, as PAR3 is thought to signal primarily through activation of either PAR1 or PAR4.

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Authors and Affiliations

  1. Biomedical Sciences Division, University of California, Riverside, CA, 92521, USA

    Kathryn A. DeFea

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  1. Kathryn A. DeFea
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Correspondence to Kathryn A. DeFea .

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Editors and Affiliations

  1. CHU Purpan, INSERM U 563, BP 3028, Toulouse Cedex, 31024, France

    Nathalie Vergnolle

  2. Institut Pasteur, Unite de Defense Innee et Inflammation, INSERM U 874, Rue du Dr. Roux 25, Paris Cedex 15, 75724, France

    Michel Chignard

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© 2011 Springer Basel

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DeFea, K.A. (2011). Terminating Protease Receptor Signaling. In: Vergnolle, N., Chignard, M. (eds) Proteases and Their Receptors in Inflammation. Progress in Inflammation Research. Springer, Basel. https://doi.org/10.1007/978-3-0348-0157-7_13

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  • DOI: https://doi.org/10.1007/978-3-0348-0157-7_13

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  • Publisher Name: Springer, Basel

  • Print ISBN: 978-3-0348-0156-0

  • Online ISBN: 978-3-0348-0157-7

  • eBook Packages: MedicineMedicine (R0)

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