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BioAssay: AID 598686

Inhibition of human recombinant 5-lipoxygenase expressed in Escherichia coli BL21 assessed as enzyme product formation measured up to 30 uM in presence of 13(S)-HpODE

5-Lipoxygenase (5-LO) and microsomal prostaglandin E# synthase (mPGES)-1 are key enzymes in the biosynthesis of leukotrienes and prostaglandin (PG)E#, respectively, and are considered as valuable targets for the treatment of inflammatory diseases. Here, we present the identification of 2-mercaptohexanoic acid derivatives as dual inhibitors of 5-LO and mPGES-1. The lead compound more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
AID: 598686
Data Source: ChEMBL (748837)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-02-15
Modify Date: 2014-05-25

Data Table ( Complete ):           View Active Data    View All Data
Target
Sequence: RecName: Full=Arachidonate 5-lipoxygenase; Short=5-LO; Short=5-lipoxygenase
Description ..   
Protein Family: Lipoxygenase
Comment ..   

Gene:ALOX5     Related Protein 3D Structures     More BioActivity Data..
BioActive Compound: 1
Description:
Title: Identification of 2-mercaptohexanoic acids as dual inhibitors of 5-lipoxygenase and microsomal prostaglandin E# synthase-1.

Abstract: 5-Lipoxygenase (5-LO) and microsomal prostaglandin E# synthase (mPGES)-1 are key enzymes in the biosynthesis of leukotrienes and prostaglandin (PG)E#, respectively, and are considered as valuable targets for the treatment of inflammatory diseases. Here, we present the identification of 2-mercaptohexanoic acid derivatives as dual inhibitors of 5-LO and mPGES-1. The lead compound 2(4-(3-biphenyloxypropoxy)phenylthio)hexanoic acid (21) inhibits human 5-LO and mPGES-1 in cell-free assays with an IC## = 3.5 and 2.2 muM, respectively, and suppresses 5-LO in intact cells with even a higher potency (IC##=0.9 muM). Compound 21 (10 muM) neither significantly inhibited the related 12- or 15-LOs nor cyclooxygenase-1 and -2 or cytosolic phospholipase A#. Based on the selective and potent inhibition of 5-LO and mPGES-1, further assessment of these 2-mercaptohexanoic acids in preclinical models of inflammation are warranted.
(PMID: 21570310)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Target Type: Target is a single protein chain

Protein Target Class: enzyme reductase

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat
5Inhibition standard valueInhibition standard valueFloat

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