Cited by 72Protein Degradation and InhibitorsChemical Synthesis and AnalysisUbiquitin and proteasome pathways

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Monomeric Targeted Protein Degraders

Hanan, Emily J., Liang, Jun, Wang, Xiaojing, Blake, Robert A., Blaquiere, Nicole, Staben, Steven T.·2020·Journal of Medicinal Chemistry

DOI 10.1021/acs.jmedchem.0c00093

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Abstract

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.

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Authors: Hanan, E. J., Liang, J., Wang, X., Blake, R. A., Blaquiere, N., & Staben, S. T.
Affiliations: Genentech (US)
Genentech, Inc. , , 1 DNA Way , , ,
Corresponding author: Staben, Steven T.
ORCID: Hanan, Emily J.
Liang, Jun
Wang, Xiaojing
Staben, Steven T.
Venue: Journal of Medicinal Chemistry
Publisher: American Chemical Society (ACS)
Published: 2020-04-30
Volume: 63
Issue: 20
Pages: 11330-11361
ISSN: 0022-2623 (ISSN-L)
1520-4804
DOI: 10.1021/acs.jmedchem.0c00093
OpenAlex: W3023538604
Cited by: 69
References: 218
Citations by year: 2026: 6 · 2025: 6 · 2024: 8 · 2023: 13 · 2022: 13 · 2021: 13 · 2020: 8
FWCI: 1.20
Type: journal article
Language: en
Open access: closed
Licence: doi.org/10.15223/policy-029 (stm-asf)
doi.org/10.15223/policy-037 (stm-asf)
doi.org/10.15223/policy-045 (stm-asf)
Locations: Journal of Medicinal Chemistry (publishedVersion)
PubMed (publishedVersion)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
Physical Sciences › Chemistry › Organic Chemistry › Chemical Synthesis and Analysis
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
Keywords: targeted protein degradation, duration of action
MeSH terms: Binding Sites, Humans, Protein Binding, Proteins, Molecular Structure, Ubiquitin-Protein Ligases, Cell Line, Tumor, Small Molecule Libraries, Drug Discovery, Proteolysis

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