A Nimbolide-Based Kinase Degrader Preferentially Degrades Oncogenic BCR-ABL
B. Tong, J. N. Spradlin, L. F. T. Novaes, E. Zhang, X. Hu, M. Moeller, S. M. Brittain, L. M. McGregor, J. M. McKenna, J. A. Tallarico, M. Schirle, T. J. Maimone, D. K. Nomura
This paper develops a PROTAC molecule, BT1, that selectively degrades BCR-ABL over c-ABL in leukemia cells using nimbolide as an E3 ligase recruiter, showing additional anti-proliferative effects.
bioRxiv · Apr 2, 2020Biochemistry