The DOI matches its Crossref record; 218 of the 218 references it cites were found in a registry or an index.
Monomeric Targeted Protein Degraders
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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“(i) favorable drug-like properties that often fall within the Lipinski's ''rule of 5'' (Fig. 2); 35”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [35]
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Targeting ferroptosis opens new avenues for the development of novel therapeutics
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Metadata
- 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.
- 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
- 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
- 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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