Quinolinones as a Novel Therapeutic Strategy in ALS

Abstract

This project investigates quinolinone analogues as a novel therapeutic strategy for ALS. We previously demonstrated that these compounds display broad efficacy in cellular and zebrafish models. This study aims (i) to identify the primary biological target, (ii) optimize formulation and delivery, and (iii) investigate efficacy and best modes of delivery of the lead molecule, ML4-10. In the first year of the project, we completed the Safety Screen analysis of ML4-10. We identified the GABAA receptor as a possible primary target and identified 3-4 possible off-target hit proteins. Using proteomics, we identified 16interacting partners of ML4-10, nine of which were localized in the nucleus, and these are currently being prioritized. We also synthesized and tested new ML4-10 analogues in disease models, including salt/prodrug forms to optimize formulation/delivery. However, ML4-10remains the most active compound to date although additional analogues are being examined.

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Document Details

Document Type
Technical Report
Publication Date
Oct 01, 2023
Accession Number
AD1213968

Entities

People

  • Belinda Abbott
  • Julie D Atkin
  • Sonam Parakh

Organizations

  • Macquarie University

Tags

DTIC Thesaurus Topics

  • Anticonvulsants
  • Australia
  • Carrier Proteins
  • Cell Physiological Processes
  • Cells
  • Chemical Synthesis
  • Chemistry
  • Dementia
  • Diseases
  • Drug Abuse
  • Lead Compounds
  • Mass Spectrometry
  • Molecules
  • Proteins
  • Proteomics
  • Spectra
  • Universities

Fields of Study

  • Biology

Readers

  • Molecular and Cellular Biochemistry
  • Neuroscience
  • Oncology

Technology Areas

  • Biotechnology
  • Biotechnology - Cancer Biotech