GPCRs in pulmonary arterial hypertension: tipping the balance

British Journal of Pharmacology
Jean Iyinikkel, Fiona Murray

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.

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Citations

Dec 21, 2018·Antioxidants & Redox Signaling·Laura Weise-CrossNikki L Jernigan
Nov 12, 2019·British Journal of Pharmacology·Astrid WeissRalph T Schermuly
Jan 9, 2019·Frontiers in Cardiovascular Medicine·Gayathri ViswanathanSudarshan Rajagopal
Oct 1, 2020·International Journal of Molecular Sciences·Olga SadowskaHanna Kozłowska
Apr 1, 2021·European Journal of Pharmacology·Hicham LabaziMargaret R MacLean

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