Key result
Altered expression and function of GPCRs contribute to the imbalance of pulmonary vascular tone in pulmonary arterial hypertension, highlighting their continued relevance as pharmacological targets.
This review highlights the critical role of GPCRs in regulating pulmonary vascular tone and their ongoing relevance as pharmacological targets for treating pulmonary arterial hypertension.
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.
No takes yet. Share an insight, caveat, or question.
Iyinikkel et al. (2018) conducted a review in Pulmonary arterial hypertension (PAH). GPCR-targeted therapies was evaluated. Altered expression and function of GPCRs contribute to the imbalance of pulmonary vascular tone in pulmonary arterial hypertension, highlighting their continued relevance as pharmacological targets.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: