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US 2025/0049930 A1Published application
Protac molecules targeting foxp3 and uses thereof
AssigneeCedars-Sinai Medical Center
InventorsHyung L. KIM, Yanping WANG, Shengchen SU
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Abstract
A bi-functional, proteolysis-targeting chimera (PROTAC) agent is provided for the modulation of transcriptional factor FOXP3 and associated regulatory T cells. The agent contains an inhibitory peptide of FOXP3 covalently bound through a linker to a ubiquitin ligase binding moiety. The agent binds FOXP3 and recruits an E3 ubiquitin ligase, and thereby bringing FOXP3 in proximity to the E3 ubiquitin ligase for ubiquitination and degradation of the FOXP3. Methods of preparation and use of the agent are also provided.
Claims22
A compound of chemical structure:
- E3LBM-L-FOXP3BP,
- wherein
- the E3LBM is a ubiquitin ligase binding moiety;
- the L is a bond or a chemical linker that is chemically linked to the E3LBM and the PFOX3M;
- and
- the FOXP3BP is a peptide capable of binding to Forkhead box protein P3 (FOXP3), wherein upon binding of the FOXP3 to the compound, the FOXP3 is ubiquitinated by a ubiquitin ligase;
- or a pharmaceutically acceptable salt, enantiomer, stereoisomer, solvate, polymorph, or prodrug thereof.
4 more elements
11-15. (canceled)
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Dependencies are inferred from the claim text.