2. Academic Validation
  3. Scaffold hopping enables direct access to more potent PROTACs with in vivo activity

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

  • Chem Commun (Camb). 2020 Jun 23;56(50):6890-6892. doi: 10.1039/d0cc02201b.
George M Burslem 1,  Daniel P Bondeson 1,  Craig M Crews 2
Affiliations

Affiliations

  • 1 Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut, USA. Craig.Crews@Yale.edu.
  • 2 Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut, USA. Craig.Crews@Yale.edu and Departments of Chemistry and Pharmacology, Yale University, New Haven, CT, USA.
PMID: 32519703 DOI: 10.1039/d0cc02201b
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.

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