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Br J Pharmacol. 2018 Aug;175(15):3063-3079. doi: 10.1111/bph.14172. Epub 2018 Apr 17.

GPCRs in pulmonary arterial hypertension: tipping the balance.

Author information

1
College of Life Sciences and Medicine, School of Medicine, Medical Sciences and Nutrition, University of Aberdeen, Aberdeen, UK.

Abstract

Pulmonary arterial hypertension (PAH) is a progressive, fatal disease characterised by increased pulmonary vascular resistance and excessive proliferation of pulmonary artery smooth muscle cells (PASMC). GPCRs, which are attractive pharmacological targets, are important regulators of pulmonary vascular tone and PASMC phenotype. PAH is associated with the altered expression and function of a number of GPCRs in the pulmonary circulation, which leads to the vasoconstriction and proliferation of PASMC and thereby contributes to the imbalance of pulmonary vascular tone associated with PAH; drugs targeting GPCRs are currently used clinically to treat PAH and extensive preclinical work supports the utility of a number of additional GPCRs. Here we review how GPCR expression and function changes with PAH and discuss why GPCRs continue to be relevant drug targets for the disease.

PMID:
29468655
PMCID:
PMC6031878
[Available on 2019-08-01]
DOI:
10.1111/bph.14172

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