SLCO1A2

Summary

SLCO1A2 (solute carrier organic anion transporter family member 1A2, HGNC:10956) is a protein-coding gene on chromosome 12p12.1, encoding Solute carrier organic anion transporter family member 1A2 (P46721). Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane.

This gene encodes a sodium-independent transporter which mediates cellular uptake of organic ions in the liver. Its substrates include bile acids, bromosulphophthalein, and some steroidal compounds. The protein is a member of the SLC21A family of solute carriers. Alternative splicing of this gene results in multiple transcript variants.

Source: NCBI Gene 6579 — RefSeq curated summary.

At a glance

• GWAS associations: 14
• Clinical variants (ClinVar): 89 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001386879

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10956
Approved symbol	SLCO1A2
Name	solute carrier organic anion transporter family member 1A2
Location	12p12.1
Locus type	gene with protein product
Status	Approved
Aliases	OATP, OATP1A2, OATP-A
Ensembl gene	ENSG00000084453
Ensembl biotype	protein_coding
OMIM	602883
Entrez	6579

Gene structure

Transcript identifiers

Ensembl transcripts: 22 — 17 protein_coding, 2 retained_intron, 2 nonsense_mediated_decay, 1 protein_coding_CDS_not_defined

ENST00000307378, ENST00000413682, ENST00000416627, ENST00000421287, ENST00000422327, ENST00000430803, ENST00000435179, ENST00000445053, ENST00000450590, ENST00000453443, ENST00000458504, ENST00000463718, ENST00000473830, ENST00000480394, ENST00000544020, ENST00000544290, ENST00000683939, ENST00000938257, ENST00000938258, ENST00000938259, ENST00000938260, ENST00000938261

RefSeq mRNA: 37 — MANE Select: NM_001386879 NM_001386878, NM_001386879, NM_001386880, NM_001386881, NM_001386882, NM_001386886, NM_001386887, NM_001386890, NM_001386908, NM_001386919, NM_001386920, NM_001386921, NM_001386922, NM_001386926, NM_001386927, NM_001386929, NM_001386931, NM_001386937, NM_001386938, NM_001386939, NM_001386940, NM_001386946, NM_001386947, NM_001386948, NM_001386949, NM_001386951, NM_001386952, NM_001386953, NM_001386954, NM_001386958, NM_001386959, NM_001386960, NM_001386961, NM_001386962, NM_001386963, NM_021094, NM_134431

CCDS: CCDS8686, CCDS91662

Canonical transcript exons

ENST00000683939 — 15 exons

Exon	Start	End
ENSE00001633976	21334827	21334917
ENSE00001845447	21264600	21269767
ENSE00003468168	21300348	21300569
ENSE00003469379	21318782	21318923
ENSE00003542292	21297404	21297568
ENSE00003548975	21274469	21274586
ENSE00003563568	21334588	21334709
ENSE00003570409	21292164	21292336
ENSE00003639786	21295597	21295792
ENSE00003646161	21293945	21294110
ENSE00003661566	21275360	21275424
ENSE00003662768	21301171	21301269
ENSE00003686390	21314549	21314681
ENSE00003689765	21304427	21304573
ENSE00003786950	21306882	21306988

Expression profiles

Bgee: expression breadth ubiquitous, 155 present calls, max score 94.98.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 2.6098 / max 434.1932, expressed in 153 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
130016	1.4481	82
130015	0.6795	71
130021	0.3540	63
130017	0.0585	38
130019	0.0392	28
130018	0.0272	5
130020	0.0032	1

Top tissues by expression

251 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
C1 segment of cervical spinal cord	UBERON:0006469	94.98	gold quality
spinal cord	UBERON:0002240	92.01	gold quality
corpus callosum	UBERON:0002336	91.75	gold quality
amygdala	UBERON:0001876	91.22	gold quality
cranial nerve II	UBERON:0000941	91.04	gold quality
putamen	UBERON:0001874	90.01	gold quality
substantia nigra	UBERON:0002038	88.83	gold quality
hypothalamus	UBERON:0001898	87.50	gold quality
midbrain	UBERON:0001891	87.21	gold quality
caudate nucleus	UBERON:0001873	87.04	gold quality
Ammon’s horn	UBERON:0001954	86.04	gold quality
Brodmann (1909) area 9	UBERON:0013540	85.61	gold quality
diaphragm	UBERON:0001103	85.31	gold quality
nucleus accumbens	UBERON:0001882	85.27	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	84.55	gold quality
prefrontal cortex	UBERON:0000451	84.14	gold quality
right frontal lobe	UBERON:0002810	83.89	gold quality
type B pancreatic cell	CL:0000169	83.87	silver quality
olfactory bulb	UBERON:0002264	83.68	silver quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	83.03	gold quality
telencephalon	UBERON:0001893	81.72	gold quality
medial globus pallidus	UBERON:0002477	81.65	gold quality
cingulate cortex	UBERON:0003027	81.50	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	81.16	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.15	gold quality
anterior cingulate cortex	UBERON:0009835	81.13	gold quality
temporal lobe	UBERON:0001871	80.55	gold quality
CA1 field of hippocampus	UBERON:0003881	80.24	silver quality
frontal cortex	UBERON:0001870	79.72	gold quality
cerebral cortex	UBERON:0000956	79.37	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-HCAD-35	yes	85.00
E-ANND-3	yes	5.80
E-ENAD-17	no	73.26
E-MTAB-7606	no	11.77

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): HNF1A, NR1I2

miRNA regulators (miRDB)

155 targeting SLCO1A2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-450A-1-3P	100.00	69.33	1837
HSA-MIR-4795-3P	100.00	74.62	4024
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-5692B	100.00	71.32	2622
HSA-MIR-5692C	100.00	71.32	2622
HSA-MIR-4668-3P	100.00	68.74	2635
HSA-MIR-3924	100.00	72.09	2394
HSA-MIR-4510	100.00	66.60	2050
HSA-MIR-6129	100.00	66.46	2080
HSA-MIR-6130	100.00	66.69	2012
HSA-MIR-6133	100.00	66.48	2064
HSA-MIR-4747-5P	100.00	67.90	2681
HSA-MIR-5196-5P	100.00	67.98	2761
HSA-MIR-4282	99.99	75.36	6408
HSA-MIR-4789-3P	99.99	70.75	2484
HSA-MIR-548N	99.98	71.94	4170
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-520D-5P	99.98	73.34	4883
HSA-MIR-524-5P	99.98	73.43	4882
HSA-MIR-12136	99.98	72.81	5713
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-548AT-5P	99.96	70.83	2666
HSA-MIR-3658	99.96	73.87	4379
HSA-LET-7C-3P	99.95	73.42	2862
HSA-MIR-128-3P	99.95	71.17	2484
HSA-MIR-216A-3P	99.95	71.19	2505
HSA-MIR-1236-3P	99.94	68.04	1695

Literature-anchored findings (GeneRIF, showing 40)

• SLCO1A2 polymorphisms may be an important yet unrecognized contributor to inter-individual variability in drug disposition and central nervous system entry of substrate drugs. (PMID:15632119)
• a potentially important role for OATP-A in the absorption and disposition of saquinovir in vivo. (PMID:15832500)
• Review summarizes current knowledge on the functional and phenotypic consequences of genetic variation in intestinally, hepatically and renally expressed members of the organic anion-transporting polypeptide (OATP) family. (PMID:18466105)
• the interplay between a xenobiotic nuclear receptor PXR and OATP1A2 that could contribute to the pathogenesis of breast cancer. (PMID:19010908)
• Antiretroviral protease inhibitors, but not non-nucleoside reverse transcriptase inhibitors, are substrates for OATP1A2, OATP1B1 and OATP1B3. (PMID:20051929)
• Is present in high frequencies in the finnish population (PMID:20560925)
• data suggest that among the many known transporters common variations of PXR, SLCO1A2, SLCO1B1, SLCO1B3, and SLCO2B1 do not contribute to breast carcinogenesis (PMID:20635135)
• By using the presence of bilirubin as a phenotype, variants rs6742078 (UGT1A1; P = .003), rs4149056 (SLCO1B1; P = .003), and rs4149000 (SLCO1A2; P = .015) were associated with gallstone composition (PMID:20837016)
• protein kinase C(PKC) regulates the transport function of OATP1A2 by modulating protein internalization; this effect of PKC is mediated in part by clathrine-dependent pathways (PMID:21133891)
• Compared with the adult cerebral cortex, mRNAs encoding OATP1A2, OATP1C1, OATP3A1 variant 2, OATP4A1, LAT2 and CD98 were reduced in fetal cortex at different gestational ages, whilst mRNAs encoding MCT8, MCT10, OATP3A1 variant 1 and LAT1 were similar. (PMID:21486766)
• Although imatinib is indicated as a substrate for OATP1A2, this transporter by itself is unlikely to contribute substantially to the absorption profiles of imatinib in humans. (PMID:21508937)
• SLCO1A2 polymorphisms significantly affect imatinib pharmacokinetics. (PMID:21633340)
• Digoxin inhibited the uptake of probe substrates of OATP1B1 (IC(50) of 47 muM), OATP1B3 (IC(50) > 8.1 muM), and OATP2B1 (IC(50) > 300 muM), but not OATP1A2 in transfected cell lines. (PMID:21849517)
• Data suggest that inhibition of OATP1A2 in intestinal mucosa at least partially explains effects of grapefruit juice (or grapefruit juice components such as the flavonoid naringin) on pharmacokinetics of aliskiren, an antihypertensive agent. (PMID:22124880)
• The expression of OATP1A2 and OATP1B3 in placenta decreased in, and may be involved in the pathophysiology of, intrahepatic cholestasis of pregnancy. OATP1A2 was localized to the vasculo-syncytial membrane and apical surface of syncytiotrophoblasts. (PMID:22203093)
• SLCO1A2 promoter variant 1 was strongly induced by vitamin D receptor. (PMID:22474172)
• Hydrophilic anti-migraine triptans are substrates for OATP1A2, a transporter expressed at human blood-brain barrier. (PMID:22509823)
• results suggest that enhanced OATP1A2 expression is associated with adaptive cell growth of prostate cancer cells under androgen-depleted conditions (PMID:22864060)
• Human OATP1A/1B transporters play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutics methotrexate and paclitaxel (PMID:23243220)
• Five novel single nucleotide polymorphisms (SNIP)S in the coding exons of SLCO1A2 gene transporter have been identified. (PMID:23918469)
• Combined high OATP1A2/high OCT6 may be a potential predictor of response to anthracycline/taxane-based chemotherapy in breast cancer (PMID:24671357)
• PDZK1 and NHERF1 regulate the transport function of OATP1A2 by modulating protein internalization via a clathrin-dependent pathway and by enhancing protein stability. (PMID:24728453)
• human OATP1B1, OATP1B3 and OATP1A2 can transport docetaxel in vivo. (PMID:24825069)
• analysis of how the transmembrane domain 6 of the human organic anion transporting polypeptide 1A2 (OATP1A2) influences transporter substrate binding, protein trafficking, and quality control (PMID:25387129)
• Report OATP1A2 expression in human retinal pigmented epithelial cells and suggest role in cellular uptake of all-trans retinol. (PMID:25560245)
• Genetic polymorphisms and function of the OATP1A2 and its clinical relevance in drug disposition (PMID:25924632)
• data provide the implication of UGT1A1 and SLCO1A2 in sickle cell anemia-related cholelithiasis. (PMID:26146896)
• important roles for OATP1A/1B in transporter-mediated uptake and disposition of doxorubicin, are reported. (PMID:27777271)
• OATP1A2, OATP1B1, and OATP2B1 can mediate cellular uptake of ochratoxin A, which could aggravate OTA toxicity. (PMID:28532671)
• SLCO1A2 and SLCO1B1 gene treatment over time interactions were associated with gametocytemia clearance rate. (PMID:28975866)
• These results indicate that the SLCO1A2 rs4149009 G > A polymorphism might affect MTX pharmacokinetics by interfering with the function of miRNAs. (PMID:29306656)
• The binding site may be responsible in part for the suppression effect of TNFalpha towars SLCO1A2 expression. (PMID:29549185)
• Our findings uncover novel associations of progressive supranuclear palsy with SLCO1A2 (rs11568563) and DUSP10 (rs6687758) variants (PMID:29986742)
• In the regulation of the function and expression of OATP1A2. (PMID:30348897)
• Association between SLCO1A2 genetic variation and methotrexate toxicity in human rheumatoid arthritis treatment. (PMID:32304147)
• Reabsorption of bile acids regulated by FXR-OATP1A2 is the main factor for the formation of cholesterol gallstone. (PMID:32597704)
• SLC46A1 Haplotype with Predicted Functional Impact has Prognostic Value in Breast Carcinoma. (PMID:33387348)
• Pharmacogenomics of celiprolol - evidence for a role of P-glycoprotein and organic anion transporting polypeptide 1A2 in celiprolol pharmacokinetics. (PMID:34585840)
• Upregulation of OATP1A2 in human oesophageal squamous cell carcinoma cells via the HDAC6-GCN5/PCAF-H3K9Ac axis. (PMID:34823432)
• Comparison of the transport kinetics of fexofenadine and its pH dependency among OATP1A2 genetic variants. (PMID:36116173)

Cross-species orthologs

12 orthologs

Organism	Symbol	Gene ID
mus_musculus	Slco1a4	ENSMUSG00000030237
mus_musculus	Slco1a1	ENSMUSG00000041698
mus_musculus	Slco1a5	ENSMUSG00000063975
mus_musculus	Slco1a6	ENSMUSG00000079262
mus_musculus	Slco1a8	ENSMUSG00000079263
mus_musculus	Slco1a7	ENSMUSG00000084927
rattus_norvegicus	Slco1a8	ENSRNOG00000010388
rattus_norvegicus	Slco1a6	ENSRNOG00000030894
rattus_norvegicus	Slco1a1	ENSRNOG00000036984
rattus_norvegicus	Slco1a5	ENSRNOG00000047493
rattus_norvegicus	Slco1a5	ENSRNOG00000086993
drosophila_melanogaster	Oatp30B	FBGN0032123

Paralogs (10): SLCO4A1 (ENSG00000101187), SLCO1B3 (ENSG00000111700), SLCO1B1 (ENSG00000134538), SLCO2B1 (ENSG00000137491), SLCO5A1 (ENSG00000137571), SLCO1C1 (ENSG00000139155), SLCO4C1 (ENSG00000173930), SLCO2A1 (ENSG00000174640), SLCO3A1 (ENSG00000176463), SLCO6A1 (ENSG00000205359)

Protein

Protein identifiers

Solute carrier organic anion transporter family member 1A2 — P46721 (reviewed: P46721)

Alternative names: OATP-A, Organic anion-transporting polypeptide 1, Sodium-independent organic anion transporter, Solute carrier family 21 member 3

All UniProt accessions (12): P46721, B4DJE6, C9IYW8, C9JCA7, C9JG34, C9JHU9, C9JSB7, C9JTF6, C9JUW6, C9K059, F5GXY6, F5H060

UniProt curated annotations — full annotation on UniProt →

Function. Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane. Responsible for intestinal absorption of bile acids. Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision. Involved in the uptake of clinically used drugs. Capable of thyroid hormone transport (both T3 or 3,3’,5’-triiodo-L-thyronine, and T4 or L-tyroxine). Also transports prostaglandin E2. Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells. May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons. May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel. Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment. Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions. May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier.

Subcellular location. Cell membrane. Basal cell membrane.

Tissue specificity. Higher expression in the brain than in liver and kidney. Expressed in brain neurons in both cortex and hippocampus. Expressed in placental trophoblasts. Also expressed in lung and testes at lower levels. Expressed in the eye (at protein level). Expressed in the retina in the outer and inner nuclear layers, the inner plexiform layer and the ganglion cell layer. Expressed in liver and prostate. In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed in Leydig cells and within the tubules. Expressed in fetal brain and liver.

Activity regulation. Transport activity is inhibited by the grapefruit juice component naringin.

Domain organisation. A conserved histidine residue in the third TMD (His-107) may play an essential role in the pH sensitivity of SLCO1A2/OATP1A2-mediated substrate transport.

Similarity. Belongs to the organo anion transporter (TC 2.A.60) family.

Isoforms (2)

UniProt ID	Names	Canonical?
P46721-1	OATP1a	yes
P46721-2	OATP1b

RefSeq proteins (37): NP_001373807, NP_001373808, NP_001373809, NP_001373810, NP_001373811, NP_001373815, NP_001373816, NP_001373819, NP_001373837, NP_001373848, NP_001373849, NP_001373850, NP_001373851, NP_001373855, NP_001373856, NP_001373858, NP_001373860, NP_001373866, NP_001373867, NP_001373868, NP_001373869, NP_001373875, NP_001373876, NP_001373877, NP_001373878, NP_001373880, NP_001373881, NP_001373882, NP_001373883, NP_001373887, NP_001373888, NP_001373889, NP_001373890, NP_001373891, NP_001373892, NP_066580, NP_602307 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002350	Kazal_dom	Domain
IPR004156	OATP	Family
IPR020846	MFS_dom	Domain
IPR036058	Kazal_dom_sf	Homologous_superfamily
IPR036259	MFS_trans_sf	Homologous_superfamily

Pfam: PF03137, PF07648

Catalyzed reactions (Rhea), 12 shown:

• prostaglandin E2(out) = prostaglandin E2(in) (RHEA:50984)
• taurocholate(out) = taurocholate(in) (RHEA:71703)
• 3,3’,5’-triiodo-L-thyronine(out) = 3,3’,5’-triiodo-L-thyronine(in) (RHEA:71815)
• L-thyroxine(out) = L-thyroxine(in) (RHEA:71819)
• estrone 3-sulfate(out) = estrone 3-sulfate(in) (RHEA:71835)
• dehydroepiandrosterone 3-sulfate(out) = dehydroepiandrosterone 3-sulfate(in) (RHEA:71839)
• tauroursodeoxycholate(out) = tauroursodeoxycholate(in) (RHEA:71843)
• glycoursodeoxycholate(out) = glycoursodeoxycholate(in) (RHEA:71847)
• glycocholate(out) = glycocholate(in) (RHEA:71851)
• taurochenodeoxycholate(out) = taurochenodeoxycholate(in) (RHEA:71855)
• glycochenodeoxycholate(out) = glycochenodeoxycholate(in) (RHEA:71859)
• taurodeoxycholate(out) = taurodeoxycholate(in) (RHEA:71863)

UniProt features (45 total): topological domain 13, transmembrane region 12, sequence variant 8, glycosylation site 4, disulfide bond 3, splice variant 3, chain 1, domain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P46721-F1	79.97	0.45

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Disulfide bonds (3): 439–469, 445–465, 454–486

Glycosylation sites (4): 124, 135, 412, 419

Function

Pathways and Gene Ontology

Reactome pathways

11 pathways

ID	Pathway
R-HSA-159418	Recycling of bile acids and salts
R-HSA-879518	Organic anion transport by SLCO transporters
R-HSA-9793528	Ciprofloxacin ADME
R-HSA-1430728	Metabolism
R-HSA-194068	Bile acid and bile salt metabolism
R-HSA-382551	Transport of small molecules
R-HSA-425397	Transport of vitamins, nucleosides, and related molecules
R-HSA-425407	SLC-mediated transmembrane transport
R-HSA-556833	Metabolism of lipids
R-HSA-8957322	Metabolism of steroids
R-HSA-9748784	Drug ADME

MSigDB gene sets: 136 (showing top): GOBP_SODIUM_INDEPENDENT_ORGANIC_ANION_TRANSPORT, GAUSSMANN_MLL_AF4_FUSION_TARGETS_A_UP, GOBP_ORGANIC_ACID_TRANSPORT, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, MARTIN_VIRAL_GPCR_SIGNALING_DN, GOBP_ORGANIC_ANION_TRANSPORT, MODULE_71, GOBP_BILE_ACID_AND_BILE_SALT_TRANSPORT, WANG_CISPLATIN_RESPONSE_AND_XPC_DN, GOBP_MONOCARBOXYLIC_ACID_TRANSPORT, GOCC_APICAL_PLASMA_MEMBRANE, FOXJ2_02, GOBP_LIPID_LOCALIZATION, MODULE_95, GOBP_TRANSMEMBRANE_TRANSPORT

GO Biological Process (8): xenobiotic metabolic process (GO:0006805), monoatomic ion transport (GO:0006811), obsolete organic anion transport (GO:0015711), bile acid and bile salt transport (GO:0015721), sodium-independent organic anion transport (GO:0043252), lipid transport (GO:0006869), obsolete organic cation transport (GO:0015695), transmembrane transport (GO:0055085)

GO Molecular Function (6): obsolete organic anion transmembrane transporter activity (GO:0008514), obsolete organic cation transmembrane transporter activity (GO:0015101), bile acid transmembrane transporter activity (GO:0015125), obsolete sodium-independent organic anion transmembrane transporter activity (GO:0015347), transmembrane transporter activity (GO:0022857), protein binding (GO:0005515)

GO Cellular Component (5): plasma membrane (GO:0005886), basal plasma membrane (GO:0009925), basolateral plasma membrane (GO:0016323), apical plasma membrane (GO:0016324), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-8 pathways:

Category	Pathways
Bile acid and bile salt metabolism	1
SLC-mediated transport of organic anions	1
Drug ADME	1
Metabolism of steroids	1
SLC-mediated transmembrane transport	1
Transport of small molecules	1
Metabolism	1
Metabolism of lipids	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transport	3
plasma membrane region	3
transmembrane transport	2
metabolic process	1
cellular response to xenobiotic stimulus	1
lipid transport	1
monocarboxylic acid transport	1
organic hydroxy compound transport	1
lipid localization	1
cellular process	1
bile acid and bile salt transport	1
carboxylic acid transmembrane transporter activity	1
lipid transmembrane transporter activity	1
transporter activity	1
binding	1
membrane	1
cell periphery	1
basal part of cell	1
basal plasma membrane	1
apical part of cell	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1046 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLCO1A2	SLC10A1	Q14973	928
SLCO1A2	SLC22A7	Q9Y694	855
SLCO1A2	SLC10A2	Q12908	823
SLCO1A2	SLC22A8	Q8TCC7	776
SLCO1A2	ABCB11	O95342	774
SLCO1A2	ABCG2	Q9UNQ0	763
SLCO1A2	NR1H4	Q96RI1	749
SLCO1A2	ABCC2	Q92887	739
SLCO1A2	CYP7A1	P22680	733
SLCO1A2	SLC16A2	P36021	723
SLCO1A2	ABCC3	O15438	721
SLCO1A2	ABCC4	O15439	705
SLCO1A2	ABCB1	P08183	700
SLCO1A2	SLC22A9	Q8IVM8	691
SLCO1A2	NR0B2	Q15466	688

IntAct

128 interactions, top by confidence:

A	B	Type	Score
SHANK1	SLCO1A2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	PDZK1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	NHERF2	psi-mi:“MI:0407”(direct interaction)	0.440
MAST1	SLCO1A2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	ARHGEF12	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	GRID2IP	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	PDZD7	psi-mi:“MI:0407”(direct interaction)	0.440
TAMALIN	SLCO1A2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	FRMPD4	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	ARHGEF11	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	GOPC	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	NHERF4	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	ARHGAP21	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	APBA3	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	SCRIB	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	PALS2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	WHRN	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	SNTB1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	HTRA4	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	MPP2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	IL16	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	PICK1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	MPDZ	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1A2	DLG1	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (2): ZCCHC24 (Cross-Linking-MS (XL-MS)), SEL1L (Affinity Capture-MS)

ESM2 similar proteins: A1Z7R6, A4IF94, A4IHK6, A5D7V7, B2RYH9, F5H094, G3V0H7, O35913, O75387, O80905, O88397, P46720, P46721, P70187, P70502, P81721, Q08C75, Q0VCM6, Q28E13, Q28FF3, Q4LE88, Q4R877, Q5BK75, Q5F4B8, Q5RBM3, Q5RF58, Q5SR56, Q7Z3Q1, Q8BSM7, Q8C0T7, Q8CA03, Q8CGA3, Q8CIA9, Q8N370, Q91498, Q91514, Q91YY5, Q96MC6, Q99J94, Q99PL8

Diamond homologs: F5H094, G3V0H7, O35913, O88397, O94956, P46720, P46721, P70502, Q00910, Q5RFF0, Q6ZQN7, Q71MB6, Q8BGD4, Q8BXB6, Q8HYW2, Q8R3L5, Q91YY5, Q92959, Q96BD0, Q99J94, Q99N01, Q99N02, Q9EP96, Q9EPT5, Q9EPZ7, Q9ERB5, Q9GMU6, Q9H2Y9, Q9JHI3, Q9JJL3, Q9NPD5, Q9NYB5, Q9QXZ6, Q9QYE2, Q9QZX8, Q9UIG8, Q9Y6L6, Q8K078, Q86UG4, Q9VVH9

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 82 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	52.9×	1e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	50.4×	1e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	50.4×	1e-06
Assembly and cell surface presentation of NMDA receptors	10	47.0×	7e-13
Dopamine Neurotransmitter Release Cycle	5	46.0×	2e-06
Long-term potentiation	5	44.1×	2e-06
Neurexins and neuroligins	11	40.1×	4e-13
Protein-protein interactions at synapses	7	34.4×	8e-08

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	10	74.5×	2e-14
protein localization to synapse	6	58.9×	9e-08
receptor clustering	7	56.0×	7e-09
regulation of postsynaptic membrane neurotransmitter receptor levels	6	38.1×	8e-07
protein-containing complex assembly	9	13.1×	2e-06
cell-cell adhesion	10	13.0×	4e-07
regulation of small GTPase mediated signal transduction	5	9.2×	4e-03
chemical synaptic transmission	7	6.9×	2e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

89 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	79
Likely benign	0
Benign	2

Top pathogenic / likely-pathogenic (0)

SpliceAI

4159 predictions. Top by Δscore:

Variant	Effect	Δscore
12:21292334:CAC:C	acceptor_gain	1.0000
12:21292337:C:A	acceptor_loss	1.0000
12:21295677:A:AC	donor_gain	1.0000
12:21300358:T:TA	donor_gain	1.0000
12:21300368:T:TA	donor_gain	1.0000
12:21300452:G:C	acceptor_gain	1.0000
12:21300452:G:GC	acceptor_gain	1.0000
12:21300460:C:CT	acceptor_gain	1.0000
12:21300461:A:T	acceptor_gain	1.0000
12:21301268:CC:C	acceptor_gain	1.0000
12:21301269:CC:C	acceptor_gain	1.0000
12:21304421:ACTT:A	donor_loss	1.0000
12:21304423:TTAC:T	donor_loss	1.0000
12:21304424:T:TG	donor_loss	1.0000
12:21304425:A:AC	donor_gain	1.0000
12:21304425:ACC:A	donor_loss	1.0000
12:21304426:C:CA	donor_loss	1.0000
12:21304426:C:CC	donor_gain	1.0000
12:21304571:ACT:A	acceptor_gain	1.0000
12:21304572:CTC:C	acceptor_gain	1.0000
12:21304573:TCT:T	acceptor_gain	1.0000
12:21304579:T:TC	acceptor_gain	1.0000
12:21318781:CCAAT:C	donor_gain	1.0000
12:21319744:T:TA	donor_gain	1.0000
12:21319745:C:A	donor_gain	1.0000
12:21269688:T:TA	donor_gain	0.9900
12:21292158:TTGTA:T	donor_loss	0.9900
12:21292159:TGTA:T	donor_loss	0.9900
12:21292160:GTACC:G	donor_loss	0.9900
12:21292161:TAC:T	donor_loss	0.9900

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000011150 (12:21418200 CT>C), RS1000045618 (12:21375788 C>T), RS1000051866 (12:21271144 A>G), RS1000055614 (12:21395718 G>A), RS1000069224 (12:21355596 T>A,C), RS1000075813 (12:21302041 G>A,C), RS1000079821 (12:21371814 C>T), RS1000089267 (12:21308783 C>G,T), RS1000103592 (12:21270841 T>A), RS1000122890 (12:21379213 T>A,C), RS1000131516 (12:21265904 T>C), RS1000135815 (12:21330987 T>C), RS1000145691 (12:21324452 G>T), RS1000147001 (12:21300283 A>C), RS1000165019 (12:21340774 A>G,T)

Disease associations

OMIM: gene MIM:602883 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

14 associations (top):

Study	Trait	p-value
GCST000386_4	Bilirubin levels	7.000000e-13
GCST000523_4	Methotrexate pharmacokinetics (acute lymphoblastic leukemia)	2.000000e-06
GCST001116_11	Progressive supranuclear palsy	7.000000e-08
GCST002875_10	Diisocyanate-induced asthma	7.000000e-06
GCST002883_2	AR-C124910XX levels in individuals with acute coronary syndromes treated with ticagrelor	4.000000e-13
GCST006249_107	Serum metabolite levels	1.000000e-26
GCST006249_44	Serum metabolite levels	2.000000e-11
GCST006249_58	Serum metabolite levels	9.000000e-52
GCST006249_97	Serum metabolite levels	1.000000e-11
GCST006309_6	Post bronchodilator percent predicted FEV1 in smoking	5.000000e-06
GCST006418_9	Progressive supranuclear palsy	3.000000e-08
GCST008553_5	Statin-induced myopathy (severe)	3.000000e-06
GCST012479_1	Rocuronium dose requirement in breast cancer surgery	5.000000e-11
GCST012479_2	Rocuronium dose requirement in breast cancer surgery	1.000000e-10

EFO canonical traits (5, from GWAS)

EFO ID	Trait name
EFO:0004570	bilirubin measurement
EFO:0006995	response to diisocyanate
EFO:0007020	AR-C124910XX measurement
EFO:0004314	forced expiratory volume
EFO:0600034	response to neuromuscular blocker

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1743123 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 96,632 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL374478	RIFAMPIN	4	93,834
CHEMBL437765	RIFAMYCIN	4	2,798

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

5 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs11045995	Dosage	3	rocuronium
rs3764043	Metabolism/PK	3	imatinib	Chronic myelogenous leukemia;BCR-ABL1 positive
rs3834939	Metabolism/PK	3	rocuronium
rs4149009	Metabolism/PK	3	methotrexate	Acute lymphoblastic leukemia
rs7967354	Dosage	3	rocuronium

PharmGKB variants

13 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs3764043	SLCO1A2	3	2.00	1	imatinib
rs4148977	SLCO1A2		0.00	0
rs4148978	SLCO1A2		0.00	0
rs4148981	SLCO1A2		0.00	0
rs10841795	SLCO1A2		0.00	0
rs11568563	SLCO1A2		0.00	0
rs45502302	SLCO1A2		0.00	0
rs3834939	SLCO1A2	3	2.00	1	rocuronium
rs750165758	SLCO1A2		0.00	0
rs4149000	SLCO1A2		0.00	0
rs7967354	SLCO1A2	3	0.00	1	rocuronium
rs11045995	IAPP, SLCO1A2	3	0.00	1	rocuronium
rs4149009	SLCO1A2	3	0.50	1	methotrexate

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: transporter — SLCO family of organic anion transporting polypeptides

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
rifamycin	Inhibition	4.96	pKi
rifampicin	Inhibition	4.29	pKi

ChEMBL bioactivities

10 potent at pChembl≥5 of 12 total, top 10 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.62	IC50	237	nM	CHEMBL6162249
6.38	IC50	420	nM	CHEMBL6146403
6.38	IC50	422	nM	CHEMBL6171119
6.15	IC50	710	nM	CHEMBL6150561
6.00	IC50	991	nM	CHEMBL6172851
6.00	IC50	1010	nM	CHEMBL6151074
5.92	IC50	1200	nM	CHEMBL6161464
5.88	IC50	1320	nM	CHEMBL6163420
5.66	IC50	2180	nM	CHEMBL6161472
5.10	IC50	7930	nM	CHEMBL6161092

CTD chemical–gene interactions

53 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
estrone sulfate	increases uptake, decreases activity, decreases uptake, increases transport, decreases reaction (+1 more)	5
Valproic Acid	affects cotreatment, increases expression, affects expression, decreases expression	5
naringin	increases transport, decreases reaction, increases uptake	3
Calcitriol	increases expression	2
Methotrexate	decreases reaction, increases import, affects response to substance	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Okadaic Acid	decreases expression	2
trospium chloride	increases metabolic processing, decreases activity	1
testosterone enanthate	affects expression	1
methylmercuric chloride	decreases expression	1
7-hydroxymethotrexate	decreases reaction, increases import	1
sodium arsenite	affects methylation	1
ochratoxin A	increases uptake	1
imidazopyrazole	affects expression	1
zearalenol	decreases activity	1
artemisinin	decreases reaction, increases uptake	1
perfluorodecanoic acid	decreases reaction, increases import	1
diosmetin	decreases reaction, increases uptake	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	increases expression, affects cotreatment, decreases expression	1
3-iodothyronamine	affects uptake	1
lithocholic acid acetate	increases expression	1
dorsomorphin	affects cotreatment, decreases expression, increases expression	1
theaflavin-3,3’-digallate	affects expression	1
Rosuvastatin Calcium	decreases reaction, increases uptake	1
Resveratrol	affects cotreatment, decreases expression	1
Vorinostat	increases expression	1
Methanol	decreases activity, decreases uptake	1
Benzo(a)pyrene	affects methylation	1
Carbamazepine	increases expression	1
Carmustine	decreases expression	1

ChEMBL screening assays

70 unique, capped per target: 60 functional, 9 admet, 1 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1743150	ADMET	Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP1A2	Membrane transporters in drug development. — Nat Rev Drug Discov
CHEMBL2075956	Functional	TP_TRANSPORTER: uptake in Xenopus laevis oocytes	Organic anion transporting polypeptides expressed in liver and brain mediate uptake of microcystin. — Toxicol Appl Pharmacol
CHEMBL6109875	Binding	Inhibition of OATP1A2 (unknown origin) transfected in human A-431 cells assessed as inhibition of SR101 uptake preincubated for 5 mins followed by SR101 addition and measured after 10 mins by fluorescence based analysis	Functional and structural polypharmacology of indazole-based privileged ligands to tackle the undruggability of membrane transporters. — Eur J Med Chem

Cellosaurus cell lines

3 cell lines: 3 cancer cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_D4UN	HuH7-SLCO1A2-KO-c4	Cancer cell line	Male
CVCL_D4UP	HuH7-SLCO1A2-KO-c5	Cancer cell line	Male
CVCL_XT43	HAP1 SLCO1A2 (-)	Cancer cell line	Male

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.