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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Cites
Items 201–218 of 218
Selective Downregulation of JAK2 and JAK3 by an ATP-Competitive pan-JAK Inhibitor
Field, S. D., Arkin, J., Li, J., & Jones, L. H. (2017) · ACS Chemical Biology · doi:10.1021/acschembio.7b00116 · Cited by 21
Dalal, K., Morin, H., Ban, F., Shepherd, A., Fernández, M., Tam, K. J., Li, H., Leblanc, E., Lack, N. A., Prinz, H., et al. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.08.059 · Cited by 18
Du, Y., Khuri, F. R., & Fu, H. (2008) · Current Chemical Genomics · doi:10.2174/1875397300802010040 · Cited by 17
Edgar, K. A., Hanan, E. J., Staben, S. T., Schmidt, S., Hong, R., Song, K. W., Young, A. E., Hamilton, P., Arrazate, A., de la Cruz, C., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-156 · Cited by 15
Self-citationFluorescent Proteins for Flow Cytometry
Hawley, T. S., Hawley, R. G., & Telford, W. G. (2017) · Current Protocols in Cytometry · doi:10.1002/cpcy.17 · Cited by 14
Govek, S. P., Bonnefous, C., Julien, J. D., Nagasawa, J. Y., Kahraman, M., Lai, A. G., Douglas, K. L., Aparicio, A. M., Darimont, B. D., Grillot, K. L., et al. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.12.042 · Cited by 10
General Staining and Segmentation Procedures for High Content Imaging and Analysis
Chambers, K. M., Mandavilli, B. S., Dolman, N. J., & Janes, M. S. (2017) · Methods in molecular biology · doi:10.1007/978-1-4939-7357-6_2 · Cited by 9
Omlin, A. G., Jones, R. J., van der Noll, R., Graham, J., Ong, M., Finkelman, R. D., Schellens, J. H. M., Zivi, A., Crespo, M., Clack, G., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2013.31.15_suppl.4511 · Cited by 8
Quantitative Comparisons of Large Numbers of Human Plasma Samples Using TMT10plex Labeling
Liu, P., Beer, L. A., Ky, B., Barnhart, K. T., & Speicher, D. W. (2017) · Methods in molecular biology · doi:10.1007/978-1-4939-7057-5_22 · Cited by 8
Labelling HaloTag Fusion Proteins with HaloTag Ligand in Living Cells
Duc, H. N., & Ren, X. (2017) · BIO-PROTOCOL · doi:10.21769/bioprotoc.2526 · Cited by 8
Friedman, L., Edgar, K., Song, K., Schmidt, S., Kirkpatrick, D., Phu, L. H., Nannini, M., Hong, R., Cheng, E., Crocker, L., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.sabcs16-s6-04 · Cited by 6
New developments and novel applications in high throughput and high content imaging
Calvert, M., Ward, A. M., Wright, G. D., & Bard, F. (2016) · Cytometry Part A · doi:10.1002/cyto.a.22921 · Cited by 6
A new “angle” on kinase inhibitor design: Prioritizing amphosteric activity above kinase inhibition
Meyerowitz, J., Weiss, W. A., & Gustafson, W. C. (2015) · Molecular & Cellular Oncology · doi:10.4161/23723556.2014.975641 · Cited by 5
Attaching Suspension Cells to Slides Using a CytocentrifugePreprint
Harlow, E., & Lane, D. P. (2006) · Cold Spring Harbor Protocols · doi:10.1101/pdb.prot4291 · Cited by 4
Fluorescent Proteins and Engineered Cell Lines
Thomas, N. (2006) · Humana Press eBooks · doi:10.1385/1-59745-217-3:165 · Cited by 4
Pushing the boundaries of high content imaging
Wright, G. D., Ward, A. M., Bard, F., & Calvert, M. (2017) · Cytometry Part A · doi:10.1002/cyto.a.23063 · Cited by 3
Song, K. W., Edgar, K. A., Kirkpatrick, D. S., Phu, L., Schmidt, S., Nannini, M., Hong, R., Cheng, E., Crocker, L., Young, A. E., et al. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-146 · Cited by 3
Attaching Suspension Cells to Slides Using Chemical LinkersPreprint
Harlow, E., & Lane, D. P. (2006) · Cold Spring Harbor Protocols · doi:10.1101/pdb.prot4292 · Cited by 1
Research works printed but not linked: 2
- Towbin, 1989, Immunoblotting in the Clinical Laboratory, J. Clin. Chem. Clin. Biochem., 27, 495
- Buchser, 2004, Assay Development Guidelines for Image-Based High Content Screening, High Content Analysis and High Content Imaging
Cited by
Sorted by citations
Targeting ferroptosis opens new avenues for the development of novel therapeutics
Sun, S., Shen, J., Jiang, J., Wang, F., & Min, J. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01606-1 · Cited by 674
Advances in Targeting ‘Undruggable’ transcription Factors With Small Molecules
Henley, M. J., & Koehler, A. N. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00199-0 · Cited by 409
E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones
Ishida, T., & Ciulli, A. (2020) · SLAS DISCOVERY · doi:10.1177/2472555220965528 · Cited by 404
Targeted protein degradation via intramolecular bivalent glues
Hsia, O., Hinterndorfer, M., Cowan, A. D., Iso, K., Ishida, T., Sundaramoorthy, R., Nakasone, M. A., Imrichova, H., Schätz, C., Rukavina, A., et al. (2024) · Nature · doi:10.1038/s41586-024-07089-6 · Cited by 222
Chasing molecular glue degraders: screening approaches
Domostegui, A., Nieto-Barrado, L., Perez-Lopez, C., & Mayor-Ruiz, C. (2022) · Chemical Society Reviews · doi:10.1039/d2cs00197g · Cited by 200
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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