Scaffold hopping enables direct access to more potent PROTACs with in vivo activity.

ABSTRACT: Herein we employ a scaffold hopping approach to enhance the activity of a previously reported BCR-Abl PROTAC. This represents a significant advance in the PROTAC field since it can abrogate the need to optimize the linker to access a more potent degrader. The new PROTAC demonstrates a >10 fold increase in ability to induce degradation and demonstrates in vivo activity.

SUBMITTER: Burslem GM 

PROVIDER: S-EPMC7404552 | biostudies-literature | 2020 Jun

REPOSITORIES: biostudies-literature