Abstract：
:Protease-activated receptors (PARs) are a ubiquitously expressed class of G-protein-coupled receptors (GPCRs) that enable cells to respond to proteases in the extracellular environment in a nuanced and dynamic manner. PAR1 is the archetypal family member and has been the object of large-scale drug development programs since the 1990s. Vorapaxar and drotrecogin-alfa are approved PAR1-targeted therapeutics, but safety concerns have limited the clinical use of vorapaxar and questions regarding the efficacy of drotrecogin-alfa led to its withdrawal from the market. New understanding of mechanisms of PAR1 function, discovery of improved strategies for modifying PAR1 function, and identification of novel indications for PAR1 modulators have provided new opportunities for therapies targeting PAR1. In this review, we critically evaluate prospects for the next generation of PAR1-targeted therapeutics.
journal_name
Trends Pharmacol Scijournal_title
Trends in pharmacological sciencesauthors
Flaumenhaft R,De Ceunynck Kdoi
10.1016/j.tips.2017.05.001subject
Has Abstractpub_date
2017-08-01 00:00:00pages
701-716issue
8eissn
0165-6147issn
1873-3735pii
S0165-6147(17)30107-4journal_volume
38pub_type
杂志文章,评审abstract：:Adenosine, when given by inhalation, initiates the narrowing of airways in subjects with asthma or chronic obstructive pulmonary disease (COPD). The underlying mechanism of this narrowing appears to involve the stimulation of specific mast cell surface adenosine receptors with the subsequent release of mediators and c...
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
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journal_title：Trends in pharmacological sciences
pub_type： 杂志文章,评审
doi：
更新日期：1996-10-01 00:00:00
