Issue 50, 2020
From the journal:

Chemical Communications

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

George M. Burslem, ORCID logo ‡*a   Daniel P. Bondesona  and  Craig M. Crews*ab  

* Corresponding authors

a Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut, USA
E-mail: Craig.Crews@Yale.edu

b Departments of Chemistry and Pharmacology, Yale University, New Haven, CT, USA

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.

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

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Article information

DOI
https://doi.org/10.1039/D0CC02201B
Article type
Communication
Submitted
25 Mar 2020
Accepted
30 May 2020
First published
30 May 2020

Chem. Commun., 2020,56, 6890-6892

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

G. M. Burslem, D. P. Bondeson and C. M. Crews, Chem. Commun., 2020, 56, 6890 DOI: 10.1039/D0CC02201B

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