Bookmark and Share
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
_
   
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
Related Experiments
Show more
AIDNameTypeComment
1705qHTS Validation Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)Confirmatorydepositor-specified cross reference: DNA binding counterscreen
1707Counterscreen for APE1 Inhibitors: Fluorescent Dye Displacement Validation AssayConfirmatorydepositor-specified cross reference: Primary qHTS assay for APE1 inhibitors
1708Counterscreen for APE1 Inhibitors: qHTS Validation Assay for Inhibitors of Endonuclease IVConfirmatorydepositor-specified cross reference: EndoIV counterscreen
2517qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)Confirmatorydepositor-specified cross reference
2564Counterscreen for APE1 Inhibitors: Fluorescent Dye Displacement AssayConfirmatorydepositor-specified cross reference
2565Counterscreen for APE1 Inhibitors: qHTS Assay for Inhibitors of Endonuclease IVConfirmatorydepositor-specified cross reference
2572Confirmation qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)Confirmatorydepositor-specified cross reference
2573qHTS FP-Based Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)Confirmatorydepositor-specified cross reference: FP counterscreen
2741Counterscreen for APE1 Inhibitors: Confirmatory Fluorescent Dye Displacement AssayConfirmatorydepositor-specified cross reference
488940Radiotracer Incision Assay (RIA) for Inhibitors of Human Apurinic/apyrimidinic Endonuclease 1 (APE1)Confirmatorydepositor-specified cross reference
504595Inhibitors of APE1: Aqueous Solubility ProfilingOtherdepositor-specified cross reference: Aqueous Solubility
504603Inhibitors of APE1: Caco-2 Cell Permeability ProfilingOtherdepositor-specified cross reference: Caco-2 Permeability
504618Inhibitors of APE1: Efflux Ratio ProfilingOtherdepositor-specified cross reference: Efflux Ratio
504624Inhibitors of APE1: Mouse Plasma Stability ProfilingOtherdepositor-specified cross reference
504643Inhibitors of APE1: Metabolic Stability ProfilingOtherdepositor-specified cross reference: Metabolic Stability
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.
Categorized Comment - additional comments and annotations
From MLP Probe Report:
Probe count: 1
MLP Probe ML# for probe 1: ML199
PubChem Substance ID (SID) for probe 1: 99430950
PubChem Compound ID (CID) for probe 1: 46925884
Probe type for probe 1: Inhibitor
IC50/EC50 (nM) for probe 1: 6000
Target for probe 1: Ape1 (gi: 6980812)
Disease relevance for probe 1: Cancer
Anti-target for probe 1: Thiazole orange counterscreen
Fold selectivity for probe 1: >10
NCBI Book chapter link for probe 1: http://www.ncbi.nlm.nih.gov/books/NBK133448/ (ID: 3025402)
Grant number for probe 1: MH086444-01
NCBI Book chapter title for probe 1: Small Molecule Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)
Additional Information
Grant Number: MH086444-01

PageFrom: