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The transcriptional repressor REV-ERB as a novel target for disease

Amaia Uriz-Huarte1, Amrita Date1, Heather Ang2

  • 1Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, White City Campus, Wood Lane, London W12 0BZ, UK.

Bioorganic & Medicinal Chemistry Letters
|August 3, 2020
PubMed

Insights

Nuclear receptor REV-ERB regulates key physiological processes and is a potential drug target. Developing higher quality synthetic ligands is crucial for validating REV-ERB

Area of Science:

  • Molecular biology
  • Pharmacology
  • Endocrinology

Background:

  • REV-ERB, a nuclear receptor, influences circadian rhythms, immunity, and metabolism.
  • It presents a promising yet challenging target for therapeutic intervention in various diseases.

Purpose of the Study:

  • To review the function and regulation of REV-ERB.
  • To explore its role in human diseases.
  • To highlight the medicinal chemistry of synthetic REV-ERB ligands.

Main Methods:

  • Literature review of REV-ERB function, modulation, and disease involvement.
  • Focus on synthetic ligand medicinal chemistry and development.

Main Results:

  • REV-ERB's broad physiological roles are established.
  • Synthetic ligands show potential but require improvement.
  • Higher quality ligands are needed for target validation.

Conclusions:

  • REV-ERB is a significant target for drug development.
  • Advancements in synthetic ligand chemistry are essential for therapeutic success.
  • Further research is needed to fully exploit REV-ERB's potential.
Keywords:
Drug developmentREV-ERBTranscription factor

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