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BioAssay: AID 654887

Competitive inhibition of human recombinant DDX3 expressed in Escherichia coli using 50 nM double strand 18/36mer RNA substrate by PAGE analysis

Efficacy of currently approved anti-HIV drugs is hampered by mutations of the viral enzymes, leading invariably to drug resistance and chemotherapy failure. Recent data suggest that cellular co-factors also represent useful targets for anti-HIV therapy. Here we describe the identification of the first small molecules specifically designed to inhibit the HIV-1 replication by targeting the RNA more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 654887
Data Source: ChEMBL (811959)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2015-04-12

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=ATP-dependent RNA helicase DDX3X; AltName: Full=DEAD box protein 3, X-chromosomal; AltName: Full=DEAD box, X isoform; AltName: Full=Helicase-like protein 2; Short=HLP2
Description ..   
Protein Family: DEADc
Comment ..   

Gene:DDX3X     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Description:
Title: Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: towards the next generation HIV-1 inhibitors.

Abstract: Efficacy of currently approved anti-HIV drugs is hampered by mutations of the viral enzymes, leading invariably to drug resistance and chemotherapy failure. Recent data suggest that cellular co-factors also represent useful targets for anti-HIV therapy. Here we describe the identification of the first small molecules specifically designed to inhibit the HIV-1 replication by targeting the RNA binding site of the human DEAD-Box RNA helicase DDX3. Optimization of a easily synthetically accessible hit (1) identified by application of a high-throughput docking approach afforded the promising compounds 6 and 8 which proved to inhibit both the helicase and ATPase activity of DDX3 and to reduce the viral load of peripheral blood mononuclear cells (PBMC) infected with HIV-1.
(PMID: 22300661)
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
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1ID50*ID50 PubChem standard valueFloatμM
2ID50 activity commentID50 activity commentString
3ID50 standard flagID50 standard flagInteger
4ID50 qualifierID50 qualifierString
5ID50 published valueID50 published valueFloatμM
6ID50 standard valueID50 standard valueFloatμM
7ID50 data validityID50 data validityString

* Activity Concentration.

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