Broadening Degrader Therapeutics: Keap1 PROTACs, Antimalarial Hybrids, and PLK1 Inhibition of NLRP3 Inflammasomes
Recent advances in targeted protein degradation and kinase modulation highlight therapeutic versatility across disease areas. Keap1-based degraders eliminate oncogenic KRAS and androgen receptor in cancer, antifolate-idasanutlin hybrids degrade <i>Plasmodium falciparum</i> DHFR-TS to overcome antifolate resistance, and PLK1 inhibition suppresses NLRP3 inflammasome activation to improve cardiac outcomes. Together, these innovations expand degrader and kinase-targeting strategies into oncology, infectious disease, and inflammatory cardiology.
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)
- Usona Institute (US)
- North Dakota State University (US)
Publication Details
- Journal
- ACS Medicinal Chemistry Letters
- Published
- 2025-10-10
- DOI
- https://doi.org/10.1021/acsmedchemlett.5c00596
- Primary Topic
- Peptidase Inhibition and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 0.00