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BioAssay: AID 475771

Inhibition of amino acid transport system xc- in human SNB19 cells assessed as [3H]L-glutamate uptake at 500 uM after 24 hrs by liquid scintillation counting

A panel of amino acid analogs and conformationally-restricted amino acids bearing a sulfonic acid were synthesized and tested for their ability to preferentially inhibit the obligate cysteine-glutamate transporter system x(c)(-) versus the vesicular glutamate transporter (VGLUT). Several promising candidate molecules were identified: R/S-4-[4'-carboxyphenyl]-phenylglycine, a biphenyl substituted analog of 4-carboxyphenylglycine and 2-thiopheneglycine-5-sulfonic acid both of which reduced glutamate uptake at system x(c)(-) by 70-75% while having modest to no effect on glutamate uptake at VGLUT. ..more
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 Tested Compounds
 Tested Compounds
All(18)
 
 
Unspecified(18)
 
 
 Tested Substances
 Tested Substances
All(18)
 
 
Unspecified(18)
 
 
 Related BioAssays
 Related BioAssays
AID: 475771
Data Source: ChEMBL (626634)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-09-27
Modify Date: 2014-08-23

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Cystine/glutamate transporter; AltName: Full=Amino acid transport system xc-; AltName: Full=Calcium channel blocker resistance protein CCBR1; AltName: Full=Solute carrier family 7 member 11; AltName: Full=xCT
Description ..   
Protein Family: Transmembrane amino acid transporter protein
Comment ..   

Gene:SLC7A11     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system x(c)(-) over the vesicular glutamate transporter.

Abstract: A panel of amino acid analogs and conformationally-restricted amino acids bearing a sulfonic acid were synthesized and tested for their ability to preferentially inhibit the obligate cysteine-glutamate transporter system x(c)(-) versus the vesicular glutamate transporter (VGLUT). Several promising candidate molecules were identified: R/S-4-[4'-carboxyphenyl]-phenylglycine, a biphenyl substituted analog of 4-carboxyphenylglycine and 2-thiopheneglycine-5-sulfonic acid both of which reduced glutamate uptake at system x(c)(-) by 70-75% while having modest to no effect on glutamate uptake at VGLUT.
(PMID: 20303751)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
BAO: Assay Format: cell-based format
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Drug uptake activity commentDrug uptake activity commentString
2Drug uptake standard flagDrug uptake standard flagInteger
3Drug uptake qualifierDrug uptake qualifierString
4Drug uptake published valueDrug uptake published valueFloat%
5Drug uptake standard valueDrug uptake standard valueFloat%

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