Design and Functionalization of Molecules Towards Drug Discovery
Abstract
We performed the design, synthesis and evaluation of ligands of nuclear receptors [vitamin D receptor (VDR), retinoid receptor and a VDR mutant], stapled short helical peptides as VDR-coactivator interaction inhibitors, and estrogen receptor degradation inducers based on a protein knockdown strategy and selective estrogen receptor down-regulators. We also demonstrated the design and functionalization of helical peptides, and performed conformational analysis of peptides, as well as an in silico study on the prediction of bioactivity for the regulation of new designer drugs.
Fields of Study & Subjects
Chemical Synthesis and Analysis
Computational Drug Discovery Methods
Heterocyclic Compound Synthesis and Bioactivity
Publication details
- Journal / source
- YAKUGAKU ZASSHI
- Volume
- 146
- Issue
- 3
- Pages
- 149–155
- Publication date
- 28 February 2026
- Language
- JA