Tags

Type your tag names separated by a space and hit enter

Protease-activated receptors in cardiovascular diseases.
Circulation. 2006 Sep 05; 114(10):1070-7.Circ

Abstract

Thrombosis associated with the pathophysiological activation of platelets and vascular cells has brought thrombin and its receptors to the forefront of cardiovascular medicine. Thrombin signaling through the protease-activated receptors (PARs) has been shown to influence a wide range of physiological responses including platelet activation, intimal hyperplasia, inflammation, and maintenance of vascular tone and barrier function. The thrombin receptors PAR1 and PAR4 can be effectively targeted in animals in which acute or prolonged exposure to thrombin leads to thrombosis and/or restenosis. In the present study, we describe the molecular and pharmacological basis of small-molecule inhibitors that target PAR1. In addition, we discuss a new class of cell-penetrating inhibitors, termed pepducins, that provide insight into previously unidentified roles of PAR1 and PAR4 in protease signaling.

Authors+Show Affiliations

Hemostasis and Thrombosis Laboratory, Division of Hematology/Oncology, Molecular Oncology Research Institute, Tufts-New England Medical Center, Boston, MA 02111, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

16952995

Citation

Leger, Andrew J., et al. "Protease-activated Receptors in Cardiovascular Diseases." Circulation, vol. 114, no. 10, 2006, pp. 1070-7.
Leger AJ, Covic L, Kuliopulos A. Protease-activated receptors in cardiovascular diseases. Circulation. 2006;114(10):1070-7.
Leger, A. J., Covic, L., & Kuliopulos, A. (2006). Protease-activated receptors in cardiovascular diseases. Circulation, 114(10), 1070-7.
Leger AJ, Covic L, Kuliopulos A. Protease-activated Receptors in Cardiovascular Diseases. Circulation. 2006 Sep 5;114(10):1070-7. PubMed PMID: 16952995.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Protease-activated receptors in cardiovascular diseases. AU - Leger,Andrew J, AU - Covic,Lidija, AU - Kuliopulos,Athan, PY - 2006/9/6/pubmed PY - 2006/10/25/medline PY - 2006/9/6/entrez SP - 1070 EP - 7 JF - Circulation JO - Circulation VL - 114 IS - 10 N2 - Thrombosis associated with the pathophysiological activation of platelets and vascular cells has brought thrombin and its receptors to the forefront of cardiovascular medicine. Thrombin signaling through the protease-activated receptors (PARs) has been shown to influence a wide range of physiological responses including platelet activation, intimal hyperplasia, inflammation, and maintenance of vascular tone and barrier function. The thrombin receptors PAR1 and PAR4 can be effectively targeted in animals in which acute or prolonged exposure to thrombin leads to thrombosis and/or restenosis. In the present study, we describe the molecular and pharmacological basis of small-molecule inhibitors that target PAR1. In addition, we discuss a new class of cell-penetrating inhibitors, termed pepducins, that provide insight into previously unidentified roles of PAR1 and PAR4 in protease signaling. SN - 1524-4539 UR - https://www.unboundmedicine.com/medline/citation/16952995/Protease_activated_receptors_in_cardiovascular_diseases_ L2 - https://www.ahajournals.org/doi/10.1161/CIRCULATIONAHA.105.574830?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -