GPCRs in pulmonary arterial hypertension: tipping the balance

Jean Iyinikkel, Fiona Murray (Corresponding Author)

Research output: Contribution to journalReview article

8 Citations (Scopus)
5 Downloads (Pure)

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.
Original languageEnglish
Pages (from-to)3063-3079
Number of pages17
JournalBritish Journal of Pharmacology
Volume175
Issue number15
Early online date17 Apr 2018
DOIs
Publication statusPublished - Aug 2018

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