Acyclic Glutarimide PROTAC Precursors Enable Controlled Protein Degradation and Expand Cereblon Ligand Space
Targeted protein degradation continues to reshape therapeutic strategy, yet the structural constraints of cereblon (CRBN) ligand chemistry limit broader application. Patent application WO 2026/043898 A1 discloses acyclic glutarimide-based precursors that undergo in situ cyclization to generate active degraders. This prodrug-like strategy enables temporally controlled CRBN engagement, enhances conjugation compatibility, and expands the degrader design space across oncology and related indications.
Authors
- Anna C. Renner (ORCID: https://orcid.org/0000-0003-4971-9609)
- Robert B. Kargbo (ORCID: https://orcid.org/0000-0002-5539-6343)
Institutions
- Dakota State University (US)
- North Dakota State University (US)
Publication Details
- Journal
- ACS Medicinal Chemistry Letters
- Published
- 2026-04-14
- DOI
- https://doi.org/10.1021/acsmedchemlett.6c00172
- Primary Topic
- Protein Degradation and Inhibitors
- Type
- article
- Field-Weighted Citation Impact
- 0.00