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BioAssay: AID 681362

TP_TRANSPORTER: uptake in Xenopus laevis oocytes

Numerous drugs and endogenous compounds are efficiently excreted from the renal proximal tubule via carrier-mediated pathways. Transepithelial excretion of organic anions occurs via their accumulative transport from the blood into the proximal tubule cells across the basolateral membrane and subsequent secretion into the urine through the apical membrane. Here we report on the isolation of a more ..
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 Tested Compounds
 Tested Compounds
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Unspecified(9)
 
 
 Tested Substances
 Tested Substances
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 Related BioAssays
 Related BioAssays
AID: 681362
Data Source: ChEMBL (838501)
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2013-11-17

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Solute carrier family 22 member 6; AltName: Full=Organic anion transporter 1; Short=rOAT1; AltName: Full=renal organic anion transporter 1; Short=rROAT1
Description ..   
Protein Family: MFS
Comment ..   

Gene:SLC22A6          More BioActivity Data..
Tested Compounds:
Description:
Title: Expression cloning and characterization of a novel multispecific organic anion transporter.

Abstract: Numerous drugs and endogenous compounds are efficiently excreted from the renal proximal tubule via carrier-mediated pathways. Transepithelial excretion of organic anions occurs via their accumulative transport from the blood into the proximal tubule cells across the basolateral membrane and subsequent secretion into the urine through the apical membrane. Here we report on the isolation of a novel complementary DNA from rat kidney that encodes a 551-amino acid residue protein (OAT1) with 12 putative membrane-spanning domains. When expressed in Xenopus laevis oocytes, OAT1 mediated sodium-independent para-aminohippurate (PAH) uptake (Km = 14.3 +/- 2.9 microM). The uptake rate of PAH was increased by the outwardly directed dicarboxylate gradient, consisting with the idea that OAT1 is an organic anion/dicarboxylate exchanger. OAT1 displayed remarkably wide substrate selectivity, covering endogenous substrates such as cyclic nucleotides, a prostaglandin and uric acid, and a variety of drugs with different structures (e.g. antibiotics, a nonsteroidal anti-inflammatory drug, diuretics, an antineoplastic drug, and a uricosuric drug). The Northern blot analysis and in situ hybridization revealed that OAT1 is exclusively expressed in the particular segment of the proximal tubule in the kidney. These data suggest that OAT1 is a multispecific organic anion transporter at the basolateral membrane of the proximal tubule. Isolation of OAT1 will facilitate elucidation of the molecular basis of drug kinetics and the development of new drugs lacking unwanted side effects.
Categorized Comment
ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: TP-search Transporter Database

ChEMBL Assay Test Type: In vitro

ChEMBL Assay Cell Type: oocytes

ChEMBL Target ID: 104148

ChEMBL Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Km*Km PubChem standard valueFloatμM
2Activity activity commentActivity activity commentString
3Activity standard flagActivity standard flagInteger
4Activity qualifierActivity qualifierString
5Activity published valueActivity published valueFloat
6Activity standard valueActivity standard valueFloat
7Km activity commentKm activity commentString
8Km standard flagKm standard flagInteger
9Km qualifierKm qualifierString
10Km published valueKm published valueFloatμM
11Km standard valueKm standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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