Title:Therapeutic Potential of Targeting Protease Activated Receptors in Cardiovascular Diseases
Volume: 21
Issue: 30
Author(s): Yogesh Bulani and Shyam S. Sharma
Affiliation:
Keywords:
Protease activated receptor, cardiovascular system, heart, blood vessels.
Abstract: From the discovery of protease activated receptors (PARs) to the development of first clinically available
PAR1 antagonist (vorapaxar) more than two decades of continuous research have passed. There are four different
types of PARs named as PAR1, 2, 3 and 4 having a unique mechanism of signaling. These receptors are present
in different organs, including the cardiovascular system. Presence of PARs in heart and blood vessels, alteration
in the level and activity of the receptors in pathological conditions along with availability of antagonists makes
these receptors targetable in several cardiac diseases. Therapeutic benefits of PAR antagonist have been proven in
animal model of cardiac diseases such as myocardial infarction, viral myocarditis, atherosclerosis, pulmonary arterial
hypertension, etc. PAR signaling plays a vital role in mediating cardiac hypertrophy, inflammation and fibrosis.
Apart from having cardiac importance PAR antagonist are also continuously experimented for their beneficial effects
in improving insulin resistance in metabolic syndromes. In the present review, we have discussed the functions of individual PARs
in the heart and blood vessels along with the expected usefulness of PAR modulators in cardiovascular diseases.
