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BioAssay: AID 362522

Activity of human recombinant iNOS expressed in Escherichia coli

Anaerobic reduction of anticancer prodrugs is a promising route to achieve targeting and selectivity in anticancer drug design. Most reductive prodrug activations involve simple electron transfer from a flavoprotein and are not amenable to specific targeting. Here, we report that the N-oxide AQ4N is reduced by a nitric oxide synthase. This reduction involves interaction with the heme iron atom in the active site and is thus subject to specific protein constraints. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 362522
Data Source: ChEMBL (510551)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-26
Modify Date: 2014-05-25

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Nitric oxide synthase, inducible; AltName: Full=Hepatocyte NOS; Short=HEP-NOS; AltName: Full=Inducible NO synthase; Short=Inducible NOS; Short=iNOS; AltName: Full=NOS type II; AltName: Full=Peptidyl-cysteine S-nitrosylase NOS2
Description ..   
Protein Family: NOS_oxygenase_euk
Comment ..   

Gene:NOS2     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Reductive heme-dependent activation of the n-oxide prodrug AQ4N by nitric oxide synthase.

Abstract: Anaerobic reduction of anticancer prodrugs is a promising route to achieve targeting and selectivity in anticancer drug design. Most reductive prodrug activations involve simple electron transfer from a flavoprotein and are not amenable to specific targeting. Here, we report that the N-oxide AQ4N is reduced by a nitric oxide synthase. This reduction involves interaction with the heme iron atom in the active site and is thus subject to specific protein constraints.
(PMID: 18681417)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Km*Km PubChem standard valueFloatμM
2Km activity commentKm activity commentString
3Km standard flagKm standard flagInteger
4Km qualifierKm qualifierString
5Km published valueKm published valueFloatμM
6Km standard valueKm standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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