Monomeric Targeted Protein Degraders

The discovery and development of targeted protein degraders have become important areas of research in the field of medicinal chemistry. Inducing degradation of a target protein presents several advantages relative to simple inhibition including a potential for extended duration of action and more p...

Full description

Saved in:
Bibliographic Details
Published inJournal of medicinal chemistry Vol. 63; no. 20; pp. 11330 - 11361
Main Authors Hanan, Emily J, Liang, Jun, Wang, Xiaojing, Blake, Robert A, Blaquiere, Nicole, Staben, Steven T
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 22.10.2020
Subjects
Binding Sites
Cell Line, Tumor
Drug Discovery - methods
Humans
Molecular Structure
Protein Binding
Proteins - antagonists & inhibitors
Proteolysis - drug effects
Small Molecule Libraries - chemistry
Small Molecule Libraries - pharmacology
Ubiquitin-Protein Ligases
Online AccessGet full text

Cover

More Information
Summary:The discovery and development of targeted protein degraders have become important areas of research in the field of medicinal chemistry. Inducing degradation of a target protein presents several advantages relative to simple inhibition including a potential for extended duration of action and more profound pharmacology. While engineered heterodimeric molecules have recently been a major focus within industry and academia, this Perspective highlights examples of targeted protein degradation observed for smaller, monomeric molecules. Methods and tools for evaluating protein degradation as well as a discussion of physical properties of monomeric vs engineered heterodimeric degraders are presented.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-3
content type line 23
ObjectType-Review-1
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.0c00093