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BioAssay: AID 212567

Inhibition of Taq polymerase at 20 uM concentration.

Telomerase is an attractive target for the design of new anticancer drugs. We have previously described a series of 1,4- and 2, 6-difunctionalized amidoanthracene-9,10-diones that inhibit human telomerase via stabilization of telomeric G-quadruplex structures. The present study details the preparation of three further, distinct series of regioisomeric difunctionalized amidoanthracene-9,10-diones more ..
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 Tested Compounds
 Tested Compounds
All(31)
 
 
Unspecified(31)
 
 
 Tested Substances
 Tested Substances
All(31)
 
 
Unspecified(31)
 
 
 Related BioAssays
 Related BioAssays
AID: 212567
Data Source: ChEMBL (209885)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-08-25

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=DNA polymerase I, thermostable; AltName: Full=Taq polymerase 1
Description ..   
Protein Family: Polymerase I functions primarily to fill DNA gaps that arise during DNA repair, recombination and replication
Comment ..   

Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Human telomerase inhibition by regioisomeric disubstituted amidoanthracene-9,10-diones.

Abstract: Telomerase is an attractive target for the design of new anticancer drugs. We have previously described a series of 1,4- and 2, 6-difunctionalized amidoanthracene-9,10-diones that inhibit human telomerase via stabilization of telomeric G-quadruplex structures. The present study details the preparation of three further, distinct series of regioisomeric difunctionalized amidoanthracene-9,10-diones substituted at the 1,5-, 1,8-, and 2,7-positions, respectively. Their in vitro cytotoxicity and Taq DNA polymerase and human telomerase inhibition properties are reported and compared with those of their 1,4- and 2,6-isomers. Potent telomerase inhibition (telIC50 values 1.3-17.3 microM) is exhibited within each isomeric series. In addition, biophysical and molecular modeling studies have been conducted to examine binding to the target G-quadruplex structure formed by the folding of telomeric DNA. These studies indicate that the isomeric diamidoanthracene-9,10-diones bind to the human telomeric G-quadruplex structure with a stoichiometry of 1:1. Plausible G-quadruplex-ligand complexes have been identified for each isomeric family, with three distinct modes of intercalative binding being proposed. The exact mode of intercalative binding is dictated by the positional placement of substituent side chains. Furthermore, in contrast to previous studies directed toward triplex DNA, it is evident that stringent control over positional attachment of substituents is not a necessity for effective telomerase inhibition.
(PMID: 9822556)
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
1Taq inhibition activity commentTaq inhibition activity commentString
2Taq inhibition standard flagTaq inhibition standard flagInteger
3Taq inhibition qualifierTaq inhibition qualifierString
4Taq inhibition published valueTaq inhibition published valueFloat
5Taq inhibition standard valueTaq inhibition standard valueFloat
6Taq inhibition data validityTaq inhibition data validityString

Data Table (Concise)
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