RGD Reference Report - Transport of the sulfated, amidated bile acid, sulfolithocholyltaurine, into rat hepatocytes is mediated by Oatp1 and Oatp2. - Rat Genome Database

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Transport of the sulfated, amidated bile acid, sulfolithocholyltaurine, into rat hepatocytes is mediated by Oatp1 and Oatp2.

Authors: Meng, LJ  Wang, P  Wolkoff, AW  Kim, RB  Tirona, RG  Hofmann, AF  Pang, KS 
Citation: Meng LJ, etal., Hepatology 2002 May;35(5):1031-40.
RGD ID: 634158
Pubmed: PMID:11981753   (View Abstract at PubMed)
DOI: DOI:10.1053/jhep.2002.32667   (Journal Full-text)

The uptake of the sulfated bile acid sulfolithocholyltaurine (SLCT) was investigated in isolated rat hepatocytes and in HeLa cells transfected with complementary DNAs (cDNAs) of organic anion transporting polypeptides (Oatps) 1 and 2 cloned from rat liver. In hepatocytes, transport of SLCT was greatly reduced by bromosulfophthalein (BSP), estrone sulfate, the precursor bile acids cholyltaurine and lithocholyltaurine, and 4,4'-diisothiocyanostilbene-2-2'-disulfonic acid (DIDS). However, SLCT transport was insensitive to 4-methylumbelliferyl sulfate, harmol sulfate, digoxin, fexofenadine, and lack of sodium ion. Because the estimation of kinetic constants was enhanced with use of inhibitors, BSP (1-50 micromol/L) was added to isolated rat hepatocytes to assess the various transport components for SLCT uptake. The resulting data showed a nonsaturable pathway and at least 2 pathways of different Michaelis-Menten constants (K(m)) (70 and 6 micromol/L) and similar maximum velocities (V(max)) (1.73 and 1.2 nmol/min/mg protein) and inhibition constants of 0.63 and 10.3 micromol/L for BSP. In expression systems, SLCT was taken up by Oatp1 and Oatp2 expressed in HeLa cells with similar K(m) values (12.6 +/- 6.2 and 14.6 +/- 1.9 micromol/L). These K(m) values were comparable to that observed for the high-affinity pathway in rat hepatocytes. In conclusion, the results suggest that transport of SLCT into rat liver is mediated in part by Oatp1 and Oatp2, high-affinity pathways, a lower-affinity pathway of unknown origin, and a nonsaturable pathway that is compatible with a transport system of high K(m) and/or passive diffusion.

Gene Ontology Annotations    Click to see Annotation Detail View

Biological Process
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
bile acid and bile salt transport  IDA 634158 RGD 

Molecular Function
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
bile acid transmembrane transporter activity  IDA 634158 RGD 

Molecular Pathway Annotations    Click to see Annotation Detail View

RGD Manual Annotations

Objects Annotated

Genes (Rattus norvegicus)
Slco1c1  (solute carrier organic anion transporter family, member 1c1)

Genes (Mus musculus)
Slco1c1  (solute carrier organic anion transporter family, member 1c1)

Genes (Homo sapiens)
SLCO1C1  (solute carrier organic anion transporter family member 1C1)

Objects referenced in this article
Gene Slco1a1 solute carrier organic anion transporter family, member 1a1 Rattus norvegicus
Gene Slco1a4 solute carrier organic anion transporter family, member 1a4 Rattus norvegicus

Additional Information