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Int. J. Mol. Sci. 2018, 19(2), 573; doi:10.3390/ijms19020573

Protease-Activated Receptor 4 (PAR4): A Promising Target for Antiplatelet Therapy

School of Life Science & Technology, China Pharmaceutical University, 24 Tong Jia Street, Nanjing 210009, China
Jiangsu Center for Pharmacodynamics Research, Evaluation and Drug Screening, China Pharmaceutical University, Nanjing 210009, China
Author to whom correspondence should be addressed.
Received: 19 December 2017 / Revised: 9 February 2018 / Accepted: 9 February 2018 / Published: 14 February 2018
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Cardiovascular diseases (CVDs) are currently among the leading causes of death worldwide. Platelet aggregation is a key cellular component of arterial thrombi and major cause of CVDs. Protease-activated receptors (PARs), including PAR1, PAR2, PAR3 and PAR4, fall within a subfamily of seven-transmembrane G-protein-coupled receptors (GPCR). Human platelets express PAR1 and PAR4, which contribute to the signaling transduction processes. In association with CVDs, PAR4 not only contributes to platelet activation but also is a modulator of cellular responses that serve as hallmarks of inflammation. Although several antiplatelet drugs are available on the market, they have many side effects that limit their use. Emerging evidence shows that PAR4 targeting is a safer strategy for preventing thrombosis and consequently may improve the overall cardiac safety profile. Our present review summarizes the PAR4 structural characteristics, activation mechanism, role in the pathophysiology of diseases and understanding the association of PAR4 targeting for improved cardiac protection. Conclusively, this review highlights the importance of PAR4 antagonists and its potential utility in different CVDs. View Full-Text
Keywords: protease-activated receptor 4 (PAR4); thrombin; platelet; thrombosis; PAR4 antagonist protease-activated receptor 4 (PAR4); thrombin; platelet; thrombosis; PAR4 antagonist

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Rwibasira Rudinga, G.; Khan, G.J.; Kong, Y. Protease-Activated Receptor 4 (PAR4): A Promising Target for Antiplatelet Therapy. Int. J. Mol. Sci. 2018, 19, 573.

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