St. Jude Reference #SJ-21-0028, #SJ-21-0048
Researchers at St. Jude created small molecules that target protein degradation (PROTACs) of CK1alpha, IKZF1 and IKZF3 that can be used for the treatment of blood and solid tumor cancers. These compounds indicate greater potency over existing small molecules (lenalidomide). Additional compounds act through the modulation of cereblon, and all may be used for treating cancers, both hematological malignancies and solid tumors.
small molecule, drug, PROTAC. targeted protein degradation, CK1alpha, IKZF1, IKZF3, hematological cancer, solid tumor, lenalidomide
Granted patents or published applications
Application filed, available under confidentiality
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Gocho, Y., Liu, J., Hu, J. et al. Network-based systems pharmacology reveals heterogeneity in LCK and BCL2 signaling and therapeutic sensitivity of T-cell acute lymphoblastic leukemia. Nat Cancer 2, 284–299 (2021). https://doi.org/10.1038/s43018-020-00167-4
Lisa J. Alcock, Yunchao Chang, Jamie A. Jarusiewicz, Marisa Actis, Stanley Nithianantham, Anand Mayasundari, Jaeki Min, Dylan Maxwell, Jeremy Hunt, Brandon Smart, Jun J. Yang, Gisele Nishiguchi, Marcus Fischer, Charles G. Mullighan, and Zoran Rankovic, “Development of Potent and Selective Janus Kinase 2/3 Directing PG–PROTACs,” ACS Medicinal Chemistry Letters 2022 13 (3), 475-482, DOI: 10.1021/acsmedchemlett.1c00650 https://pubs.acs.org/doi/full/10.1021/acsmedchemlett.1c00650
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