Target intelligence / Profile preview

Nitric oxide synthase 3 (endothelial) (eNOS)

Target
eNOS
Molecular classification
Enzyme, Oxidoreductase, Monooxygenase, Calmodulin-binding protein
01

Overview

Nitric oxide synthase 3 (eNOS) is a constitutive enzyme primarily expressed in vascular endothelial cells, where it plays a critical role in maintaining cardiovascular homeostasis. It catalyzes the production of nitric oxide (NO), a potent signaling molecule that induces vasodilation, inhibits platelet aggregation, and prevents leukocyte adhesion to the vessel wall (UniProt P29474; PubMed 11418480). Dysregulation or 'uncoupling' of eNOS, where the enzyme produces reactive oxygen species instead of NO, is a hallmark of endothelial dysfunction and contributes significantly to the pathogenesis of atherosclerosis, hypertension, and diabetes (PubMed 15142844). Pharmacological strategies often focus on enhancing eNOS activity or expression through the use of statins, ACE inhibitors, or supplemental cofactors like tetrahydrobiopterin to restore vascular health (StatPearls NBK538315). Conversely, excessive NO production can lead to pathological hypotension, making the precise modulation of this enzyme a key therapeutic challenge.

Other names
Endothelial nitric oxide synthaseNOS3Nitric oxide synthase type IIIConstitutive NOSEC-NOS
02

Mechanism of action

Catalyzes the oxidation of L-arginine to L-citrulline and nitric oxide (NO) in the presence of NADPH, oxygen, and cofactors like tetrahydrobiopterin (BH4). NO then activates soluble guanylate cyclase in smooth muscle cells, increasing cGMP and leading to vasodilation.

03

Biological functions

VasodilationAngiogenesisPlatelet aggregation inhibitionLeukocyte adhesion inhibitionBlood pressure regulationVascular homeostasisSmooth muscle relaxation
04

Disease associations

HypertensionAtherosclerosisErectile dysfunctionCardiovascular diseasePre-eclampsiaDiabetes mellitusIschemic stroke
05

Safety considerations

Enzyme uncoupling leading to superoxide productionSevere hypotension from over-activationOxidative stress in BH4 deficiencyTolerance development to organic nitrates
06

Interacting drugs

L-arginine

7 more in the full profile.

07

Biomarkers

Flow-mediated dilation (FMD)Plasma nitrite/nitrate levelsL-arginine/ADMA ratioUrinary cyclic GMPEndothelial microparticles

Beyond the preview

Go deeper on Nitric oxide synthase 3 (endothelial) (eNOS).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Nitric oxide synthase 3 (endothelial) (eNOS).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call