Target intelligence / Profile preview

Vascular Smooth Muscle Cell Relaxation via Cyclic GMP Pathway (cGMP Pathway)

Target
cGMP Pathway
Molecular classification
Signaling pathway
01

Overview

Vascular smooth muscle cell (VSMC) relaxation via the cyclic GMP (cGMP) pathway is a critical physiological process that regulates vascular tone and blood pressure. This pathway is primarily activated by nitric oxide (NO) or natriuretic peptides, which stimulate the production of cGMP in VSMCs. The increase in cGMP leads to activation of protein kinase G (PKG), resulting in a cascade of events that culminate in smooth muscle relaxation. Pharmacological agents targeting this pathway include nitrates, phosphodiesterase inhibitors, and natriuretic peptides—all used clinically for their vasodilatory properties. Disruption or dysfunction within this signaling cascade can contribute to pathological conditions such as hypertension.

Other names
cGMP-PKG signaling pathway in vascular smooth muscleNitric oxide-cGMP pathwayNO-cGMP pathwayCyclic GMP signaling in VSMC
02

Mechanism of action

Stimulation of cGMP production, activation of PKG, leading to decreased intracellular calcium and smooth muscle relaxation.

03

Biological functions

VasodilationRegulation of vascular toneBlood pressure regulationSmooth muscle relaxationInhibition of VSMC proliferationInhibition of VSMC migration
04

Disease associations

HypertensionAtherosclerosisCardiovascular disease
05

Safety considerations

HypotensionDrug interactions (e.g., with nitrates)PDE5 inhibitor side effects (e.g., headache, flushing)
06

Interacting drugs

Nitrates

5 more in the full profile.

07

Biomarkers

cGMP levelsPKG activityVASP phosphorylation

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