Vascular G protein-coupled receptors (Vascular GPCRs)

Vascular G protein-coupled receptors (GPCRs) are a broad class of integral membrane proteins that mediate the effects of various hormones, neurotransmitters, and vasoactive peptides on the cardiovascular system. Located primarily on vascular smooth muscle cells and endothelial cells, these receptors regulate essential physiological processes such as vascular tone, permeability, and cell proliferation (Insel et al., 2007). Key members include the angiotensin II type 1 receptor (AT1R), alpha- and beta-adrenoceptors, and endothelin receptors, which collectively maintain blood pressure and regional blood flow (Alexander et al., 2023). Maladaptive signaling through these receptors is a hallmark of diseases like hypertension, atherosclerosis, and heart failure, making them primary targets for pharmacological intervention (StatPearls, 2023). Therapeutic agents targeting vascular GPCRs, such as angiotensin receptor blockers (ARBs) and beta-blockers, work by modulating intracellular signaling cascades involving G proteins like Gq, Gs, and Gi to restore vascular homeostasis. These drugs typically act as competitive antagonists or inverse agonists to inhibit pathological signaling pathways. Ongoing research focuses on biased signaling and allosteric modulation to improve efficacy and reduce side effects. The diversity of these receptors allows for highly specific therapeutic targeting depending on the vascular bed and disease state.

Other names

V-GPCRsCardiovascular G protein-coupled receptorsVascular G protein-coupled receptor superfamily

Modulation of vascular tone and signaling through agonism or antagonism of specific G protein-coupled receptors, influencing intracellular secondary messengers like cAMP and IP3/calcium.