Discovery and design of molecular glue enhancers of CDK12-DDB1 interactions for targeted degradation of cyclin K

The CDK12 inhibitor SR-4835 promotes the proteasomal degradation of cyclin K, contingent on the presence of CDK12 and the CUL4-RBX1-DDB1 E3 ligase complex. The inhibitor displays molecular glue activity, which correlates with its enhanced ability to inhibit cell growth. This effect is achieved by fa...

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Veröffentlicht in:	RSC chemical biology 2024-10, Vol.6 (1), p.36-55
Hauptverfasser:	Ghosh, Pompom, Schmitz, Maximilian, Pandurangan, Thiyagamurthy, Zeleke, Solomon Tadesse, Chan, Sean Chin, Mosior, John, Sun, Luxin, Palve, Vinayak, Grassie, Dylan, Anand, Kanchan, Frydman, Sylvia, Roush, William R, Schönbrunn, Ernst, Geyer, Matthias, Duckett, Derek, Monastyrskyi, Andrii
Format:	Artikel
Sprache:	eng
Schlagworte:	Chemistry
Online-Zugang:	Volltext
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