HomeAboutRankingsData Sources
© 2026 GeneE
🧬
GeneE
25 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
ⓘGeneE is for informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment.
CYP1A2
cytochrome P450 family 1 subfamily A member 2
Chromosome 15 · 15q24.1
NCBI Gene: 1544Ensembl: ENSG00000140505.8HGNC: HGNC:2596UniProt: P05177
511PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Hub Gene
RESEARCH IMPACT
Highly Studied
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
demethylase activityprotein bindingoxidoreductase activityoxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenhypertensionessential hypertensioncoffee consumptionhearing loss
✦AI Summary

CYP1A2 (cytochrome P450 family 1 subfamily A member 2) is a major hepatic drug-metabolizing enzyme that catalyzes the oxidative metabolism of numerous endogenous substrates and xenobiotics. As a monooxygenase, CYP1A2 uses molecular oxygen to insert one oxygen atom into substrates while reducing the second to water, with electrons provided by NADPH via cytochrome P450 reductase 12. The enzyme exhibits high catalytic activity for estrogen metabolism, converting estrone and 17β-estradiol to their 2-hydroxy derivatives 23, and metabolizes cholesterol to 25-hydroxycholesterol 4. CYP1A2 also catalyzes retinoic acid biosynthesis through sequential oxidation of retinol 1 and performs stereoselective epoxidation of polyunsaturated fatty acids 5. In xenobiotic metabolism, CYP1A2 processes various drugs including sumatriptan through N-demethylation 6, phenacetin through O-deethylation 7, and caffeine via N3-demethylation. The enzyme's activity is subject to inhibition by natural compounds like quercetin and fucoxanthin 8 and pterostilbene 9. Genetic polymorphisms in CYP1A2 influence drug response, with clinical implications for personalized medicine approaches in conditions like depression 10 and cancer risk assessment 11.

Sources cited
1
CYP1A2 metabolizes sumatriptan through N-demethylation
PMID: 36655303
2
CYP1A2 activity is inhibited by quercetin and fucoxanthin
PMID: 33260381
3
CYP1A2 polymorphisms influence duloxetine response in depression treatment
PMID: 37686266
4
Pterostilbene inhibits CYP1A2 metabolic activity
PMID: 33849700
5
CYP1A2 genetic variants are associated with breast cancer risk and caffeine metabolism
PMID: 25921178
6
CYP1A2 uses NADPH-dependent electron transfer for monooxygenase activity and catalyzes retinoic acid biosynthesis
PMID: 10681376
7
CYP1A2 exhibits high activity for estrogen 2-hydroxylation
PMID: 11555828
8
CYP1A2 metabolizes estrone and estradiol to hydroxy derivatives
PMID: 12865317
9
CYP1A2 metabolizes cholesterol to 25-hydroxycholesterol
PMID: 21576599
10
CYP1A2 performs stereoselective epoxidation of polyunsaturated fatty acids
PMID: 19965576
11
CYP1A2 catalyzes O-deethylation of phenacetin
PMID: 14725854
Disease Associationsⓘ20
hypertensionOpen Targets
0.41Moderate
essential hypertensionOpen Targets
0.29Weak
coffee consumptionOpen Targets
0.29Weak
hearing lossOpen Targets
0.29Weak
osteoarthritisOpen Targets
0.28Weak
Increased blood pressureOpen Targets
0.26Weak
arthritisOpen Targets
0.25Weak
cardiovascular diseaseOpen Targets
0.25Weak
joint diseaseOpen Targets
0.23Weak
Abdominal Aortic AneurysmOpen Targets
0.22Weak
scleritisOpen Targets
0.21Weak
osteoarthritis, hipOpen Targets
0.21Weak
goutOpen Targets
0.19Weak
degeneration of macula and posterior poleOpen Targets
0.17Weak
Abnormal urine sodium concentrationOpen Targets
0.17Weak
chronic kidney diseaseOpen Targets
0.16Weak
kidney failureOpen Targets
0.15Weak
Abnormality of the skeletal systemOpen Targets
0.15Weak
hepatocellular carcinomaOpen Targets
0.12Weak
breast cancerOpen Targets
0.10Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
GAPDHProtein interaction99%UGT1A4Protein interaction98%UGT1A8Protein interaction98%UGT1A1Protein interaction97%UGT1A7Protein interaction97%UGT1A10Protein interaction97%
Tissue Expression6 tissues
Liver
100%
Brain
0%
Lung
0%
Ovary
0%
Heart
0%
Bone Marrow
0%
Gene Interaction Network
Click a node to explore
CYP1A2GAPDHUGT1A4UGT1A8UGT1A1UGT1A7UGT1A10
PROTEIN STRUCTURE
Preparing viewer…
PDB2HI4 · 1.95 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.35LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF1.02 [0.78–1.35]
RankingsWhere CYP1A2 stands among ~20K protein-coding genes
  • #518of 20,598
    Most Researched511 · top 5%
  • #14,159of 17,882
    Most Constrained (LOEUF)1.35
Genes detectedCYP1A2
Sources retrieved25 papers
Response time—
📄 Sources
25▼
1
Metabolism of sumatriptan revisited.
PMID: 36655303
Pharmacol Res Perspect · 2023
1.00
2
Screening of Human CYP1A2 and CYP3A4 Inhibitors from Seaweed In Silico and In Vitro.
PMID: 33260381
Mar Drugs · 2020
0.90
3
The Impact of the CYP2D6 and CYP1A2 Gene Polymorphisms on Response to Duloxetine in Patients with Major Depression.
PMID: 37686266
Int J Mol Sci · 2023
0.80
4
Adenomyosis: genetics of estrogen metabolism.
PMID: 30878995
Horm Mol Biol Clin Investig · 2019
0.76
5
Pharmacogenetics and pharmacogenomics.
PMID: 11411304
Pediatr Clin North Am · 2001
0.70