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Curr Opin Hematol. 2007 May;14(3):230-5.

Protease-activated receptor signaling: new roles and regulatory mechanisms.

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  • 1Department of Pharmacology, Emory University School of Medicine, Rollins Research Center, Atlanta, Georgia, USA.



Protease-activated receptors are G-protein-coupled receptors that transmit cellular responses to coagulant proteases in a variety of cell types in the vasculature and other tissues. Several other proteases can activate protease-activated receptors in vitro and may affect their function in vivo. While a role for these receptors in hemostasis and thrombosis has been established, their functions in inflammatory and other responses have yet to be fully elucidated. In addition, the mechanisms responsible for protease and cell type-specific signaling mediated by these receptors are largely undefined. Here, we highlight recent advances in understanding the roles and regulation of protease-activated receptor signaling.


Recent studies have increased our knowledge of the function of protease-activated receptor signaling in platelets and its contribution to thrombosis. In other cell types, recent work has revealed new connections between these receptors and signaling effectors important for vascular development and inflammatory responses. Other studies have advanced our understanding of protease and cell type-specific responses as well as novel regulatory mechanisms for control of protease-activated receptor signaling.


Thus, elucidating the signaling and regulatory mechanisms of protease-activated receptors in various tissues and cell types is important for understanding their biological function as well as for designing therapeutic strategies to control their function.

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