Small molecules that can be used for targeted protein degradation of CK1alpha, IKZF1 and IKZF3 (SJ-21-0048)

St. Jude Reference #SJ-21-0048

Description

Researchers at St. Jude created small molecules that target protein degradation 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).                                                                                     

Pictured below is the leading compound in this series SJ7095 with proteomics data to point to its selectivity in degradation of CK1a and IKZF1/3. The structure of this compound was disclosed at the ACS meeting in Chicago on Aug. 22, 2022.

Keywords

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

Related scientific references

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

Licensing opportunities

Please contact us if you are interested in licensing and developing this technology to be more shelf stable.. Contact: chad.riggs@stjude.org

Contact the Office of Technology Licensing (Phone: 901-595-2342, Fax: 901-595-3148) for more information.