The Rise of Degrader Drugs

Authors

Mingxing Teng
Nathanael S Gray

Language

English

Publication Date

8-17-2023

Journal

Cell Chemical Biology

DOI

10.1016/j.chembiol.2023.06.020

PMID

37494935

Abstract

The cancer genomics revolution has served up a plethora of promising and challenging targets for the drug discovery community. The field of targeted protein degradation (TPD) uses small molecules to reprogram the protein homeostasis system to destroy desired target proteins. In the last decade, remarkable progress has enabled the rational development of degraders for a large number of target proteins, with over 20 molecules targeting more than 12 proteins entering clinical development. While TPD has been fully credentialed by the prior development of immunomodulatory drug (IMiD) class for the treatment of multiple myeloma, the field is poised for a "Gleevec moment" in which robust clinical efficacy of a rationally developed novel degrader against a preselected target is firmly established. Here, we endeavor to provide a high-level evaluation of exciting developments in the field and comment on steps that may realize the full potential of this new therapeutic modality.

Keywords

Humans, Proteins, Proteolysis, Multiple Myeloma, Drug Discovery, Genomics

Published Open-Access

yes

Recommended Citation

Mingxing Teng and Nathanael S Gray, "The Rise of Degrader Drugs" (2023). Faculty and Staff Publications. 5675.
https://digitalcommons.library.tmc.edu/baylor_docs/5675