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Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines

Nat Commun. 2024-01; 
Gisele Nishiguchi , Lauren G Mascibroda , Sarah M Young , Elizabeth A Caine , Sherif Abdelhamed , Jeffrey J Kooijman , Darcie J Miller , Sourav Das , Kevin McGowan , Anand Mayasundari , Zhe Shi , Juan M Barajas , Ryan Hiltenbrand , Anup Aggarwal , Yunchao Chang , Vibhor Mishra , Shilpa Narina , Melvin Thomas , Allister J Loughran , Ravi Kalathur , Kaiwen Yu , Suiping Zhou , Xusheng Wang , Anthony A High , Junmin Peng , Shondra M Pruett-Miller , Danette L Daniels , Marjeta Urh , Anang A Shelat , Charles G Mullighan , Kristin M Riching , Guido J R Zaman , Marcus Fischer , Jeffery M Klco , Zoran Rankovic
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Custom Vector Construction … Human full-length CK1α (StrepII-CK1α) was synthesized and cloned into the pFastBac1 vector (Genscript) and expressed in High-Five insect cells using the Bac-to-Bac baculovirus … Get A Quote

摘要

Molecular-glue degraders are small molecules that induce a specific interaction between an E3 ligase and a target protein, resulting in the target proteolysis. The discovery of molecular glue degraders currently relies mostly on screening approaches. Here, we describe screening of a library of cereblon (CRBN) ligands against a panel of patient-derived cancer cell lines, leading to the discovery of SJ7095, a potent degrader of CK1α, IKZF1 and IKZF3 proteins. Through a structure-informed exploration of structure activity relationship (SAR) around this small molecule we develop SJ3149, a selective and potent degrader of CK1α protein in vitro and in vivo. The structure of SJ3149 co-crystalized in complex with CK1... More

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