St. Jude Reference #SJ-21-0047
Description
LCK is an emerging therapeutic target for T-ALL. Dasatinib, a small-molecule LCK inhibitor, has significant anti-leukemia efficacy in vitro and in vivo against T-ALL. However, these effects require constant dosing of dasatinib and drug resistance is common. The PROTACs we developed showed greater potency and longer-lasting effects than dasatinib in suppressing LCK signaling and thus better cytotoxity in LCK-dependent T-ALLs.
Researchers at St. Jude created a series of Proteolytic Targeting Chimera (PROTACs) compounds that can target LCK for degradation with dasatinib as the bait/ligand. LCK kinase is an important drug target in T-ALL and these PROTACs induce T-ALL apoptosis by complete degradation of therapeutic target LCK.
Keywords
small molecule, drug, PROTAC. targeted protein degradation, Dasatinib, LCK inhibitor, leukemia, T-ALL, resistance.
Granted Patents or Published Applications
Application filed, available under confidentiality
Related Scientific References
Licensing Opportunities
We are seeking partners to commercialize these small molecules.
Contact the Office of Technology Licensing (Phone: 901-595-2342, Fax: 901-595-3148) for more information.