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BioAssay: AID 2324

Probe Development Summary of Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)

The apurinic/apyrimidinic endonuclease APE1 is the primary mammalian enzyme responsible for the removal of abasic (or AP) sites in DNA and functions centrally in the base excision DNA repair (BER) pathway. Recent studies suggested a link between an overexpression of APE1 in many cancers and resistance of these tumor cells to radio- and chemotherapy. Thus, targeting APE1 could improve the efficacy of current treatment paradigms by promoting selective sensitization or protection of diseased and normal cells, respectively. ..more
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AID: 2324
Data Source: NCGC (APE1100)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-02-01
Modify Date: 2011-04-14
Target
Depositor Specified Assays
Show more
AIDNameTypeComment
504643Inhibitors of APE1: Metabolic Stability ProfilingotherMetabolic Stability
504618Inhibitors of APE1: Efflux Ratio ProfilingotherEfflux Ratio
504595Inhibitors of APE1: Aqueous Solubility ProfilingotherAqueous Solubility
504603Inhibitors of APE1: Caco-2 Cell Permeability ProfilingotherCaco-2 Permeability
1707Counterscreen for APE1 Inhibitors: Fluorescent Dye Displacement Validation AssayconfirmatoryPrimary qHTS assay for APE1 inhibitors
1708Counterscreen for APE1 Inhibitors: qHTS Validation Assay for Inhibitors of Endonuclease IVconfirmatoryEndoIV counterscreen
1705qHTS Validation Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)confirmatoryDNA binding counterscreen
2573qHTS FP-Based Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)confirmatoryFP counterscreen
2572Confirmation qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)confirmatory
2564Counterscreen for APE1 Inhibitors: Fluorescent Dye Displacement Assayconfirmatory
2741Counterscreen for APE1 Inhibitors: Confirmatory Fluorescent Dye Displacement Assayconfirmatory
504624Inhibitors of APE1: Mouse Plasma Stability Profilingother
2517qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)confirmatory
488940Radiotracer Incision Assay (RIA) for Inhibitors of Human Apurinic/apyrimidinic Endonuclease 1 (APE1)confirmatory
2565Counterscreen for APE1 Inhibitors: qHTS Assay for Inhibitors of Endonuclease IVconfirmatory
Description:
Assay Provider: David M. Wilson, III, National Institute on Aging, NIH
Screening Center PI: Austin, C.P.
Screening Center: NIH Chemical Genomics Center [NCGC]

The apurinic/apyrimidinic endonuclease APE1 is the primary mammalian enzyme responsible for the removal of abasic (or AP) sites in DNA and functions centrally in the base excision DNA repair (BER) pathway. Recent studies suggested a link between an overexpression of APE1 in many cancers and resistance of these tumor cells to radio- and chemotherapy. Thus, targeting APE1 could improve the efficacy of current treatment paradigms by promoting selective sensitization or protection of diseased and normal cells, respectively.

This assay will summarize the probe development efforts that are currently ongoing.
Protocol
Please see related BioAssays for all protocols relevant to this probe development project: AID 1705, 1707, 1708
Comment
Related BioAssays:

AID 1705: This assay is a validation screen for inhibitors of APE1.

AID 1707: This assay is an EndoIV counterscreen

AID 1708: This assay is a dna-binding counterscreen

This summary assay will be updated as additional screens are run and small molecule probes have been developed.
Additional Information
Grant Number: MH086444-01

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