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Proteinase-activated receptor 1: A target for repurposing in the treatment of COVID-19?
Br J Pharmacol. 2020 11; 177(21):4971-4974.BJ

Abstract

In the search to rapidly identify effective therapies that will mitigate the morbidity and mortality of COVID-19, attention has been directed towards the repurposing of existing drugs. Candidates for repurposing include drugs that target COVID-19 pathobiology, including agents that alter angiotensin signalling. Recent data indicate that key findings in COVID-19 patients include thrombosis and endotheliitis. Activation of proteinase-activated receptor 1 (PAR1), in particular by the serine protease thrombin, is a critical element in platelet aggregation and coagulation. PAR1 activation also impacts on the actions of other cell types involved in COVID-19 pathobiology, including endothelial cells, fibroblasts and pulmonary alveolar epithelial cells. Vorapaxar is an approved inhibitor of PAR1, used for treatment of patients with myocardial infarction or peripheral arterial disease. We discuss evidence for a possible beneficial role for vorapaxar in the treatment of COVID-19 patients and other as-yet non-approved antagonists of PAR1 and proteinase-activated receptor 4 (PAR4). LINKED ARTICLES: This article is part of a themed issue on The Pharmacology of COVID-19. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v177.21/issuetoc.

Authors+Show Affiliations

Department of Pharmacology, University of California San Diego, La Jolla, CA, USA.Department of Pharmacology, University of California San Diego, La Jolla, CA, USA. Department of Medicine, University of California San Diego, La Jolla, CA, USA.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

32639031

Citation

Sriram, Krishna, and Paul A. Insel. "Proteinase-activated Receptor 1: a Target for Repurposing in the Treatment of COVID-19?" British Journal of Pharmacology, vol. 177, no. 21, 2020, pp. 4971-4974.
Sriram K, Insel PA. Proteinase-activated receptor 1: A target for repurposing in the treatment of COVID-19? Br J Pharmacol. 2020;177(21):4971-4974.
Sriram, K., & Insel, P. A. (2020). Proteinase-activated receptor 1: A target for repurposing in the treatment of COVID-19? British Journal of Pharmacology, 177(21), 4971-4974. https://doi.org/10.1111/bph.15194
Sriram K, Insel PA. Proteinase-activated Receptor 1: a Target for Repurposing in the Treatment of COVID-19. Br J Pharmacol. 2020;177(21):4971-4974. PubMed PMID: 32639031.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Proteinase-activated receptor 1: A target for repurposing in the treatment of COVID-19? AU - Sriram,Krishna, AU - Insel,Paul A, Y1 - 2020/07/27/ PY - 2020/06/10/received PY - 2020/06/18/revised PY - 2020/06/22/accepted PY - 2020/7/9/pubmed PY - 2020/10/28/medline PY - 2020/7/9/entrez SP - 4971 EP - 4974 JF - British journal of pharmacology JO - Br J Pharmacol VL - 177 IS - 21 N2 - In the search to rapidly identify effective therapies that will mitigate the morbidity and mortality of COVID-19, attention has been directed towards the repurposing of existing drugs. Candidates for repurposing include drugs that target COVID-19 pathobiology, including agents that alter angiotensin signalling. Recent data indicate that key findings in COVID-19 patients include thrombosis and endotheliitis. Activation of proteinase-activated receptor 1 (PAR1), in particular by the serine protease thrombin, is a critical element in platelet aggregation and coagulation. PAR1 activation also impacts on the actions of other cell types involved in COVID-19 pathobiology, including endothelial cells, fibroblasts and pulmonary alveolar epithelial cells. Vorapaxar is an approved inhibitor of PAR1, used for treatment of patients with myocardial infarction or peripheral arterial disease. We discuss evidence for a possible beneficial role for vorapaxar in the treatment of COVID-19 patients and other as-yet non-approved antagonists of PAR1 and proteinase-activated receptor 4 (PAR4). LINKED ARTICLES: This article is part of a themed issue on The Pharmacology of COVID-19. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v177.21/issuetoc. SN - 1476-5381 UR - https://www.unboundmedicine.com/medline/citation/32639031/Proteinase_activated_receptor_1:_A_target_for_repurposing_in_the_treatment_of_COVID_19 L2 - https://doi.org/10.1111/bph.15194 DB - PRIME DP - Unbound Medicine ER -