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
Target
Depositor Specified Assays
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| AID | Name | Type | Comment |
|---|---|---|---|
| 504643 | Inhibitors of APE1: Metabolic Stability Profiling | other | Metabolic Stability |
| 504618 | Inhibitors of APE1: Efflux Ratio Profiling | other | Efflux Ratio |
| 504595 | Inhibitors of APE1: Aqueous Solubility Profiling | other | Aqueous Solubility |
| 504603 | Inhibitors of APE1: Caco-2 Cell Permeability Profiling | other | Caco-2 Permeability |
| 1707 | Counterscreen for APE1 Inhibitors: Fluorescent Dye Displacement Validation Assay | confirmatory | Primary qHTS assay for APE1 inhibitors |
| 1708 | Counterscreen for APE1 Inhibitors: qHTS Validation Assay for Inhibitors of Endonuclease IV | confirmatory | EndoIV counterscreen |
| 1705 | qHTS Validation Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) | confirmatory | DNA binding counterscreen |
| 2573 | qHTS FP-Based Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) | confirmatory | FP counterscreen |
| 2572 | Confirmation qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) | confirmatory | |
| 504624 | Inhibitors of APE1: Mouse Plasma Stability Profiling | other | |
| 2564 | Counterscreen for APE1 Inhibitors: Fluorescent Dye Displacement Assay | confirmatory | |
| 2741 | Counterscreen for APE1 Inhibitors: Confirmatory Fluorescent Dye Displacement Assay | confirmatory | |
| 2565 | Counterscreen for APE1 Inhibitors: qHTS Assay for Inhibitors of Endonuclease IV | confirmatory | |
| 2517 | qHTS Assay for Inhibitors of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1) | confirmatory |
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.
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.
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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