Related Experiment Video
Updated: Aug 22, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
The cardiovascular actions of protease-activated receptors
1Department of Pharmacology, College of Physicians and Surgeons, Columbia University, 630 West 168 Street, New York, NY 10032, USA. sfs1@columbia.edu
Abstract:
Protease-activated receptors (PARs) comprise a family of G protein-coupled receptors with a unique proteolytic activation mechanism. PARs are activated by thrombin or other coagulation or inflammatory proteases formed at sites of tissue injury. PARs play a particularly important role in the pathogenesis of clinical disorders characterized by chronic inflammation or smoldering activation of the coagulation cascade. Individual PARs have been linked to the regulation of a broad range of cellular functions. Recent studies identify PAR family members in the vasculature (including within atherosclerotic lesions) and in the heart. Here, PAR-triggered responses contribute to vasoregulation and influence cardiac electrical and mechanical activity. PAR activation also is linked to structural remodeling of the vasculature and the myocardium. This review focuses on the cardiovascular actions of PARs that play a role in normal cardiovascular physiology and that are likely to contribute to cardiovascular diseases.
More Related Videos
12:03Receptor Autoradiography Protocol for the Localized Visualization of Angiotensin II Receptors
Published on: June 7, 2016
08:56Demonstration of Proteolytic Activation of the Epithelial Sodium Channel (ENaC) by Combining Current Measurements with Detection of Cleavage Fragments
Published on: July 5, 2014
Related Concept Videos
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Enzyme-linked Receptors
Neurotrophin (NT) receptors are a family of RTKs, including trkA, trkB, and trkC (tropomyosin-related kinase) receptors. TrkA is specific for nerve growth factor (NGF), neurotrophin-6, and neurotrophin-7. TrkB binds...
GPCRs Regulate Adenylyl Cylase Activity
Two...
Antihypertensive Drugs: Angiotensin-Converting Enzyme Inhibitors
Adrenergic Receptors: β Subtype
Isoprenaline > Adrenaline > Noradrenaline
Neurotransmitter binding to these receptors causes activation of adenylyl cyclase resulting in increased concentrations of cAMP and modulation of calcium ion channels within the cell. They are further classified into β1, β2, and β3 subtypes.
β1-adrenoceptors: β1-adrenoceptors have equal affinities for...
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System