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Using PAR4 Inhibition as an Anti-Thrombotic Approach: Why, How, and When?

Australian Centre for Blood Diseases, Monash University, Melbourne VIC 3800, Australia
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Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2019, 20(22), 5629; https://doi.org/10.3390/ijms20225629
Received: 20 September 2019 / Revised: 6 November 2019 / Accepted: 6 November 2019 / Published: 11 November 2019
(This article belongs to the Special Issue Mechanisms and Therapeutics of Platelet Thrombus Formation)
Protease-activated receptors (PARs) are a family of four GPCRs with a variety of cellular functions, yet the only advanced clinical endeavours to target these receptors for therapeutic gain to date relates to the impairment of platelet function for anti-thrombotic therapy. The only approved PAR antagonist is the PAR1 inhibitor, vorapaxar—the sole anti-platelet drug against a new target approved in the past 20 years. However, there are two PARs on human platelets, PAR1 and PAR4, and more recent efforts have focused on the development of the first PAR4 antagonists, with first-in-class agents recently beginning clinical trial. Here, we review the rationale for this approach, outline the various modes of PAR4 inhibition, and speculate on the specific therapeutic potential of targeting PAR4 for the prevention of thrombotic conditions. View Full-Text
Keywords: protease-activated receptors; thrombin; platelet; thrombosis; antagonists; anti-thrombotics; anti-platelets protease-activated receptors; thrombin; platelet; thrombosis; antagonists; anti-thrombotics; anti-platelets
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Li, S.; Tarlac, V.; Hamilton, J.R. Using PAR4 Inhibition as an Anti-Thrombotic Approach: Why, How, and When? Int. J. Mol. Sci. 2019, 20, 5629.

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