Don’t Lose Your (War)head: Structure–Activity Relationships of Covalent Warheads as Substrates for GST-Catalyzed Glutathione Conjugation
values correlate closely with compound half-lives in human liver cytosol. Together, these findings establish GST susceptibility as a structurally tunable determinant of metabolic GSH conjugation and provide new principles for the optimization of TCIs.
Authors
- Jeffrey W. Keillor (ORCID: https://orcid.org/0000-0002-8133-6862)
- Lavleen Mader (ORCID: https://orcid.org/0000-0002-9519-2484)
- Jessica E. Borean (ORCID: https://orcid.org/0009-0002-6823-9686)
Institutions
- University of Ottawa (CA)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-04-30
- DOI
- https://doi.org/10.1021/acs.jmedchem.6c00826
- Primary Topic
- Sulfur Compounds in Biology
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Natural Sciences and Engineering Research Council of Canada