Literature DB >> 34058637

Reviewing the toolbox for degrader development in oncology.

Joel O Cresser-Brown1, Graham P Marsh1, Hannah J Maple2.   

Abstract

The field of targeted protein degradation encompasses a growing number of modalities that achieve potent and selective knockdown of target proteins at the post-translational level. Among the most clinically advanced are bifunctional small-molecule degraders, also referred to as PROteolysis Targeting Chimeras, Degronimids, SNIPERs, or uSMITEs. Although applicable to many disease indications, oncology stands to be the first to benefit from this promising therapeutic approach, with the first investigational new drugs (INDs) filed in 2019 and a proliferation of research specifically focused on harnessing degraders for cancer treatment. In this review, we consider the toolbox of guidelines, reagents, and technologies that has evolved alongside the field to support degrader research and development.
Copyright © 2021 The Author(s). Published by Elsevier Ltd.. All rights reserved.

Entities:  

Year:  2021        PMID: 34058637     DOI: 10.1016/j.coph.2021.04.009

Source DB:  PubMed          Journal:  Curr Opin Pharmacol        ISSN: 1471-4892            Impact factor:   5.547


  2 in total

1.  Novel SMARCA Degraders for Treating Cancer.

Authors:  Ram W Sabnis
Journal:  ACS Med Chem Lett       Date:  2022-08-30       Impact factor: 4.632

2.  Bifunctional Compounds as SMARCA2 Degraders for Treating Cancer.

Authors:  Ram W Sabnis
Journal:  ACS Med Chem Lett       Date:  2021-12-10       Impact factor: 4.345

  2 in total

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