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[Design and Functionalization of Molecules Towards Drug Discovery].

Masaaki Kurihara1

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Yakugaku Zasshi : Journal of the Pharmaceutical Society of Japan
|March 1, 2026
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Summary

Researchers designed novel ligands targeting nuclear receptors like the vitamin D receptor (VDR) and developed helical peptides to inhibit VDR-coactivator interactions, advancing designer drug development.

Keywords:
nuclear receptor ligandprotein knockdownstapled short helical peptide

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Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Drug Discovery

Background:

  • Nuclear receptors, including the vitamin D receptor (VDR), play critical roles in cellular regulation.
  • Modulating nuclear receptor activity is a key strategy in drug development.
  • Understanding protein-protein interactions is essential for designing targeted therapeutics.

Purpose of the Study:

  • To design and synthesize novel ligands for nuclear receptors, specifically VDR, retinoid receptor, and a VDR mutant.
  • To develop stapled helical peptides as inhibitors of VDR-coactivator interactions.
  • To explore estrogen receptor degradation strategies and predict bioactivity for new designer drugs.

Main Methods:

  • Ligand design and synthesis.
  • Development of stapled short helical peptides.
  • Protein knockdown strategies and selective estrogen receptor down-regulators.
  • Conformational analysis of peptides.
  • In silico studies for bioactivity prediction.

Main Results:

  • Successful design, synthesis, and evaluation of nuclear receptor ligands.
  • Demonstrated functionalization and conformational analysis of helical peptides.
  • In silico prediction of bioactivity for potential designer drugs.
  • Exploration of VDR-coactivator interaction inhibition and estrogen receptor degradation.

Conclusions:

  • The study successfully designed and synthesized novel ligands and peptides targeting nuclear receptors.
  • The developed helical peptides show potential as VDR-coactivator interaction inhibitors.
  • In silico methods provide a valuable tool for predicting bioactivity in designer drug development.
  • This research contributes to the advancement of targeted therapeutics by modulating nuclear receptor function.