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2.A.60.1.5
Organic anion transporter, OATP2, OAT1B1, SLCO1B1 or OATP1B1 (LST-1) (SLC21A6) (substrates: mono- and bis-glucuronosyl bilirubin, sulfobromophthalein, taurocholate (Km = 14 μM), estrone sulfate, dehydroepiandrosterone sulfate, estradiol-17 β-D-glucuronide and other conjugated steroids (i.e., estrone 3-sulfate), leukotriene C4, eicosanoids (i.e., prostaglandin E2, thromboxane B2, leucotriene C4 and leucotriene E4), thyroid hormones (i.e., thyroxine and triiodothyronine), other organic anions, drugs, β-lactam antibiotics, ochratoxin, xenobiotics, ouabain, valsartan and pravastatin). OatP-C/1B1(SLC21A) (Hogg et al. 2015; Qi et al. 2017). The bile acid (cholic acid) uptake transporter, OatP-C (transports cholic acid without symport with GSH) (Briz et al., 2006; Degorter et al., 2012). Amino acids in TMS2 essential for estrone-3-sulfate transport have been identified (Li et al., 2012).  OATP1B1 exhibits polymorphism related to neonatal hyperbilirubinemia (Zhang et al. 2010).  Tyr258 and Trp259 in TMS6 play different roles in substrate specificity (Huang et al. 2013).  Cyclic ABP aromatic ring substituents like the chloro-phenyl-thio groups increase their ability to inhibit OATP-mediated transport (Herfindal et al. 2014).  TMS11 influences substrate binding, stability and trafficking (Hong et al. 2015).  Transports danoprevir (hepatitis C virus protease inhibitor) (Brennan et al. 2015).  Residues have been identified that are involved in modulating transport kinetics, and this participation strongly depends on the substrate used in the assay (Gruetz et al. 2016).

Accession Number:Q9Y6L6
Protein Name:OAT6 aka OATP2 aka LST1 aka OATPC
Length:691
Molecular Weight:76449.00
Species:Homo sapiens (Human) [9606]
Number of TMSs:12
Location1 / Topology2 / Orientation3: Basolateral cell membrane1 / Multi-pass membrane protein2
Substrate Monoglucuronosyl bilirubin, Bisglucuronosyl bilirubin, Sulfobromophthalein, taurocholate, Estrone sulfate, Dehydroepiandrosterone sulfate, Estradiol-17 beta-D-glucuronide, Leukotriene C4, Eicosanoids, Thyroid hormones, Organoanions, drugs, Beta-lactam antibiotics, xenobiotics, Ouabain, Valsartan, Pravastatin, Cholate

Cross database links:

NOG322696
Genevestigator: Q9Y6L6 Q9Y6L6
HEGENOM: HBG717600 HOG000231269
RefSeq: NP_006437.3   
Entrez Gene ID: 10599   
Pfam: PF07648    PF03137   
OMIM: 604843  gene
KEGG: hsa:10599    hsa:10599   

Gene Ontology

GO:0016323 C:basolateral plasma membrane
GO:0005887 C:integral to plasma membrane
GO:0005624 C:membrane fraction
GO:0015347 F:sodium-independent organic anion transmembr...
GO:0015711 P:organic anion transport
GO:0015347 F:sodium-independent organic anion transmembrane transporter activity
GO:0015721 P:bile acid and bile salt transport
GO:0008206 P:bile acid metabolic process
GO:0043252 P:sodium-independent organic anion transport

References (18)

[1] “Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1.”  Abe T.et.al.   10358072
[2] “A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters.”  Hsiang B.H.et.al.   10601278
[3] “A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.”  Koenig J.et.al.   10644574
[4] “Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide.”  Koenig J.et.al.   10779507
[5] “Complete sequencing and characterization of 21,243 full-length human cDNAs.”  Ota T.et.al.   14702039
[6] “Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans.”  Tirona R.G.et.al.   11477075
[7] “A naturally occurring mutation in the SLC21A6 gene causing impaired membrane localization of the hepatocyte uptake transporter.”  Michalski C.et.al.   12196548
[8] “Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis.”  Nozawa T.et.al.   12130747
[9] “Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1.”  Abe T.et.al.   10358072
[10] “A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters.”  Hsiang B.H.et.al.   10601278
[11] “A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.”  Koenig J.et.al.   10644574
[12] “Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide.”  Koenig J.et.al.   10779507
[13] “Complete sequencing and characterization of 21,243 full-length human cDNAs.”  Ota T.et.al.   14702039
[14] “The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).”  The MGC Project Teamet.al.   15489334
[15] “Complete OATP1B1 and OATP1B3 deficiency causes human Rotor syndrome by interrupting conjugated bilirubin reuptake into the liver.”  van de Steeg E.et.al.   22232210
[16] “Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans.”  Tirona R.G.et.al.   11477075
[17] “A naturally occurring mutation in the SLC21A6 gene causing impaired membrane localization of the hepatocyte uptake transporter.”  Michalski C.et.al.   12196548
[18] “Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis.”  Nozawa T.et.al.   12130747

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FASTA formatted sequence
1:	MDQNQHLNKT AEAQPSENKK TRYCNGLKMF LAALSLSFIA KTLGAIIMKS SIIHIERRFE 
61:	ISSSLVGFID GSFEIGNLLV IVFVSYFGSK LHRPKLIGIG CFIMGIGGVL TALPHFFMGY 
121:	YRYSKETNIN SSENSTSTLS TCLINQILSL NRASPEIVGK GCLKESGSYM WIYVFMGNML 
181:	RGIGETPIVP LGLSYIDDFA KEGHSSLYLG ILNAIAMIGP IIGFTLGSLF SKMYVDIGYV 
241:	DLSTIRITPT DSRWVGAWWL NFLVSGLFSI ISSIPFFFLP QTPNKPQKER KASLSLHVLE 
301:	TNDEKDQTAN LTNQGKNITK NVTGFFQSFK SILTNPLYVM FVLLTLLQVS SYIGAFTYVF 
361:	KYVEQQYGQP SSKANILLGV ITIPIFASGM FLGGYIIKKF KLNTVGIAKF SCFTAVMSLS 
421:	FYLLYFFILC ENKSVAGLTM TYDGNNPVTS HRDVPLSYCN SDCNCDESQW EPVCGNNGIT 
481:	YISPCLAGCK SSSGNKKPIV FYNCSCLEVT GLQNRNYSAH LGECPRDDAC TRKFYFFVAI 
541:	QVLNLFFSAL GGTSHVMLIV KIVQPELKSL ALGFHSMVIR ALGGILAPIY FGALIDTTCI 
601:	KWSTNNCGTR GSCRTYNSTS FSRVYLGLSS MLRVSSLVLY IILIYAMKKK YQEKDINASE 
661:	NGSVMDEANL ESLNKNKHFV PSAGADSETH C