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BioAssay: AID 624611

Specific activity of expressed human recombinant UGT1A8

In vertebrates, the glucuronidation of small lipophilic agents is catalyzed by the endoplasmic reticulum UDP-glucuronosyltransferases (UGTs). This metabolic pathway leads to the formation of water-soluble metabolites originating from normal dietary processes, cellular catabolism, or exposure to drugs and xenobiotics. This classic detoxification process, which led to the discovery nearly 50 years more ..
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 Tested Compounds
 Tested Compounds
All(112)
 
 
Unspecified(112)
 
 
 Tested Substances
 Tested Substances
All(113)
 
 
Unspecified(113)
 
 
 Related BioAssays
 Related BioAssays
AID: 624611
Data Source: ChEMBL (774047)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-26

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=UDP-glucuronosyltransferase 1-8; Short=UDPGT 1-8; Short=UGT1*8; Short=UGT1-08; Short=UGT1.8; AltName: Full=UDP-glucuronosyltransferase 1-H; Short=UGT-1H; Short=UGT1H; AltName: Full=UDP-glucuronosyltransferase 1A8; Flags: Precursor
Description ..   
Protein Family: GT1_Gtf_like
Comment ..   

Gene:UGT1A8     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Human UDP-glucuronosyltransferases: metabolism, expression, and disease.

Abstract: In vertebrates, the glucuronidation of small lipophilic agents is catalyzed by the endoplasmic reticulum UDP-glucuronosyltransferases (UGTs). This metabolic pathway leads to the formation of water-soluble metabolites originating from normal dietary processes, cellular catabolism, or exposure to drugs and xenobiotics. This classic detoxification process, which led to the discovery nearly 50 years ago of the cosubstrate UDP-glucuronic acid (19), is now known to be carried out by 15 human UGTs. Characterization of the individual gene products using cDNA expression experiments has led to the identification of over 350 individual compounds that serve as substrates for this superfamily of proteins. This data, coupled with the introduction of sophisticated RNA detection techniques designed to elucidate patterns of gene expression of the UGT superfamily in human liver and extrahepatic tissues of the gastrointestinal tract, has aided in understanding the contribution of glucuronidation toward epithelial first-pass metabolism. In addition, characterization of the UGT1A locus and genetic studies directed at understanding the role of bilirubin glucuronidation and the biochemical basis of the clinical symptoms found in unconjugated hyperbilirubinemia have uncovered the structural gene polymorphisms associated with Crigler-Najjar's and Gilbert's syndrome. The role of the UGTs in metabolism and different disease states in humans is the topic of this review.
(PMID: 10836148)
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloatpm/min/mg
5Activity standard valueActivity standard valueFloatpm/min/mg

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
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