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10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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SLCO1A2
solute carrier organic anion transporter family member 1A2
Chromosome 12 · 12p12.1
NCBI Gene: 6579Ensembl: ENSG00000084453.17HGNC: HGNC:10956UniProt: B4DJE6
71PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Transporter
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
basal plasma membraneplasma membranetransmembrane transporter activityprotein bindingAbnormality of the skeletal systemnormal pressure hydrocephalusatrial fibrillationresponse to neuromuscular blocker
✦AI Summary

SLCO1A2 encodes organic anion-transporting polypeptide 1A2 (OATP1A2), a sodium-independent transporter mediating cellular uptake of diverse organic anions at the plasma membrane. Primary substrates include bile acids (cholate, taurocholate, glycocholate) 1, steroid sulfates (DHEAS, estrone-3-sulfate) 23, all-trans-retinol for visual cycle maintenance 4, thyroid hormones (T3, T4) 15, and prostaglandin E2 1. SLCO1A2 mediates apical uptake across intestinal epithelial cells and retinal pigment epithelium, with expression regulated by vitamin D receptor signaling 6 and suppressed by TNFα-NFκB signaling 7. Clinically, SLCO1A2 transports methotrexate and other chemotherapeutic drugs 8. Loss-of-function variants (E184K, D185N, T259P, D288N) impair membrane expression and reduce transport of estrone-3-sulfate, imatinib, and methotrexate by 20-50% 8, associating with increased methotrexate toxicity risk in rheumatoid arthritis patients 9. Genetic variants in SLCO1A2 show associations with late-life cognitive outcomes in APOE-ε4 carriers 10 and progressive supranuclear palsy susceptibility 1112, suggesting broader roles in neurological function beyond drug transport.

Sources cited
1
Primary substrates include bile acids (cholate, taurocholate, glycocholate) , steroid sulfates (DHEAS, estrone-3-sulfate) , , all-trans-retinol for visual cycle maintenance , thyroid hormones (T3, T4) , , and prostaglandin E2 .
PMID: 19129463
2
Primary substrates include bile acids (cholate, taurocholate, glycocholate) , steroid sulfates (DHEAS, estrone-3-sulfate) , , all-trans-retinol for visual cycle maintenance , thyroid hormones (T3, T4) , , and prostaglandin E2 .
PMID: 25560245
3
SLCO1A2 mediates apical uptake across intestinal epithelial cells and retinal pigment epithelium, with expression regulated by vitamin D receptor signaling and suppressed by TNFα-NFκB signaling .
PMID: 22474172
4
SLCO1A2 mediates apical uptake across intestinal epithelial cells and retinal pigment epithelium, with expression regulated by vitamin D receptor signaling and suppressed by TNFα-NFκB signaling .
PMID: 29549185
5
Clinically, SLCO1A2 transports methotrexate and other chemotherapeutic drugs .
PMID: 23918469
6
Loss-of-function variants (E184K, D185N, T259P, D288N) impair membrane expression and reduce transport of estrone-3-sulfate, imatinib, and methotrexate by 20-50% , associating with increased methotrexate toxicity risk in rheumatoid arthritis patients .
PMID: 32304147
7
Genetic variants in SLCO1A2 show associations with late-life cognitive outcomes in APOE-ε4 carriers and progressive supranuclear palsy susceptibility , , suggesting broader roles in neurological function beyond drug transport.
PMID: 41720779
Disease Associationsⓘ20
Abnormality of the skeletal systemOpen Targets
0.46Moderate
normal pressure hydrocephalusOpen Targets
0.40Weak
atrial fibrillationOpen Targets
0.33Weak
response to neuromuscular blockerOpen Targets
0.30Weak
hypertensionOpen Targets
0.30Weak
response to xenobiotic stimulusOpen Targets
0.30Weak
HydrocephalusOpen Targets
0.29Weak
progressive supranuclear palsyOpen Targets
0.28Weak
goutOpen Targets
0.15Weak
complicationOpen Targets
0.14Weak
hemorrhageOpen Targets
0.14Weak
response to statinOpen Targets
0.13Weak
neoplasmOpen Targets
0.10Suggestive
bilirubin metabolism diseaseOpen Targets
0.09Suggestive
glioblastoma multiformeOpen Targets
0.07Suggestive
response to antineoplastic agentOpen Targets
0.07Suggestive
Okt4 epitope deficiencyOpen Targets
0.06Suggestive
malariaOpen Targets
0.06Suggestive
cancerOpen Targets
0.06Suggestive
gastric cancerOpen Targets
0.05Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
ABCC2Protein interaction93%SLC10A1Protein interaction93%ABCB11Protein interaction92%CYP7A1Protein interaction91%NR1H4Protein interaction88%NR0B2Protein interaction87%
Tissue Expression6 tissues
Brain
100%
Liver
19%
Lung
1%
Ovary
1%
Bone Marrow
0%
Heart
0%
Gene Interaction Network
Click a node to explore
SLCO1A2ABCC2SLC10A1ABCB11CYP7A1NR1H4NR0B2
PROTEIN STRUCTURE
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AlphaFoldAI-predicted · UniProt P46721
View on AlphaFold ↗
Constraintⓘ
LOEUFⓘ
1.24LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.89 [0.65–1.24]
RankingsWhere SLCO1A2 stands among ~20K protein-coding genes
  • #6,678of 20,598
    Most Researched71
  • #13,063of 17,882
    Most Constrained (LOEUF)1.24
Genes detectedSLCO1A2
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Targeting inhibition of prognosis-related lipid metabolism genes including CYP19A1 enhances immunotherapeutic response in colon cancer.
PMID: 37055842
J Exp Clin Cancer Res · 2023
1.00
2
Association between SLCO1A2 genetic variation and methotrexate toxicity in human rheumatoid arthritis treatment.
PMID: 32304147
J Biochem Mol Toxicol · 2020
0.90
3
The SLCO1A2 gene, encoding human organic anion-transporting polypeptide 1A2, is transactivated by the vitamin D receptor.
PMID: 22474172
Mol Pharmacol · 2012
0.80
4
Genetic modifiers of APOE-ε4-associated cognitive decline.
PMID: 41720779
Nat Commun · 2026
0.70
5
Functional analysis of novel polymorphisms in the human SLCO1A2 gene that encodes the transporter OATP1A2.
PMID: 23918469
AAPS J · 2013
0.60