Rapid synthesis of proteolysis-targeting chimeras by consecutive click assembly
Abstract An efficient strategy to access proteolysis-targeting chimeras (PROTACs) is disclosed. Consecutive click assembly of readily available functional modules enables the rapid and modular synthesis of PROTACs. In this manuscript, we demonstrate the synthesis of a range of PROTACs from an E3 ligase ligand and an epidermal growth factor receptor (EGFR) ligand, conveniently diversified with functional modules by triple-click assembly, together with the evaluation of their bioactivity.
Authors
- Yosuke Demizu (ORCID: https://orcid.org/0000-0001-7521-4861)
- Hidetomo Yokoo (ORCID: https://orcid.org/0000-0002-9354-6592)
- Gaku Orimoto
- Suguru Yoshida (ORCID: https://orcid.org/0000-0001-5888-9330)
- Maho Miyamoto
- K. Yamada
- Yuri Taninaga
Institutions
- Tokyo University of Science (JP)
- Yokohama City University Medical Center (JP)
- National Institute of Health Sciences (JP)
- Yokohama City University (JP)
Publication Details
- Journal
- Bulletin of the Chemical Society of Japan
- Published
- 2025-11-28
- DOI
- https://doi.org/10.1093/bulcsj/uoaf115
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 0.00