SJ-21-0047 – LCK PROTAC for T-ALL Therapy

  • 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
  • These PROTACs induce T-ALL apoptosis by complete degradation of therapeutic target LCK.

Abstract

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. We are seeking partners to commercialize these small molecules.

Contact Information

Name: Scott Elmer

Email: scott.elmer@stjude.org

Phone: 901-595-2756