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An Improved Method for P2X7R Antagonist Screening.

Rômulo José Soares-Bezerra1, Natiele Carla da Silva Ferreira1, Anael Viana Pinto Alberto1

  • 1Laboratory of Cellular Communication, Oswaldo Cruz Institute, FIOCRUZ, Rio de Janeiro, Brazil.

Plos One
|May 21, 2015
PubMed
Summary
This summary is machine-generated.

A new high-throughput screening (HTS) assay effectively identifies antagonists for the P2X7 receptor (P2X7R), a target for diseases like rheumatoid arthritis and Alzheimer's. This validated method offers reliable drug discovery for P2X7R-related conditions.

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Drug Discovery

Background:

  • The P2X7 receptor (P2X7R) is activated by extracellular ATP, particularly at inflammation sites, forming a pore permeable to molecules up to 900 Da.
  • P2X7R is implicated in diseases such as leukemia, rheumatoid arthritis, and Alzheimer's disease, making it a therapeutic target.
  • Selective P2X7R antagonists are sought for treating diseases associated with its overactivation.

Purpose of the Study:

  • To validate a high-throughput screening (HTS) method for identifying P2X7R antagonists.
  • To assess the reliability and suitability of the developed HTS assay using in vitro protocols.

Main Methods:

  • Generation of dose-response curves for the agonist ATP and antagonists Brilliant Blue G (BBG) and oxidized ATP (OATP).
  • Calculation of EC50 and IC50 values to confirm assay performance against known literature data.
  • Assessment of assay robustness using the Z-factor for propidium iodide (PI) and lucifer yellow (LY) uptake.
  • Evaluation of inter-operator variability and reproducibility.

Main Results:

  • EC50 for ATP and IC50 values for BBG and OATP were consistent with published data.
  • High Z-factor values (0.635 for PI uptake, 0.867 for LY uptake) indicate a robust assay.
  • The assay demonstrated no inter-operator variation and high reproducibility.
  • The spectrophotometry-based method is suitable for multiwell plate evaluation of P2X7R activity.

Conclusions:

  • The validated HTS assay provides a selective and reliable method for evaluating P2X7R activity.
  • This assay can be instrumental in screening chemical and natural product libraries for novel P2X7R antagonists or agonists.
  • The developed method facilitates efficient drug discovery for P2X7R-related diseases.