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First targeted protein degrader hits the clinic
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“Finally, a first heterobifunctional PROTAC that recruits the androgen receptor to an E3 ligase recently entered the clinic 21 .”
From Targeted protein degradation: expanding the toolbox (2019) · cites this paper as [21]
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Targeted protein degradation: expanding the toolbox
Schapira, M., Calabrese, M. F., Bullock, A. N., & Crews, C. M. (2019) · Nature Reviews Drug Discovery · doi:10.1038/s41573-019-0047-y · Cited by 960
Trends in kinase drug discovery: targets, indications and inhibitor design
Attwood, M. M., Fabbro, D., Sokolov, A. V., Knapp, S., & Schiöth, H. B. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00252-y · Cited by 850
Ferroptosis surveillance independent of GPX4 and differentially regulated by sex hormones
Liang, D., Feng, Y., Zandkarimi, F., Wang, H., Zhang, Z., Kim, J., Cai, Y., Gu, W. J., Stockwell, B. R., & Jiang, X. (2023) · Cell · doi:10.1016/j.cell.2023.05.003 · Cited by 769
“ARV-110 is a clinical stage PROTAC protein degrader selectively targetingAR.(41)Remarkably, bothENZandARV-110 inhibited endogenous MBOAT2 expression in a dose-dependent manner (Figures 5A, 5C, and S5H) and strongly sensitizedmultiple AR PCa cell lines to RSL3-induced ferroptosis, including CRPC line LnAR (Figures 5A–5…”
BackgroundLYTACs that engage the asialoglycoprotein receptor for targeted protein degradation
Ahn, G., Banik, S. M., Miller, C. L., Riley, N. M., Cochran, J. R., & Bertozzi, C. R. (2021) · Nature Chemical Biology · doi:10.1038/s41589-021-00770-1 · Cited by 665
PROTACs: An Emerging Therapeutic Modality in Precision Medicine
Nalawansha, D. A., & Crews, C. M. (2020) · Cell chemical biology · doi:10.1016/j.chembiol.2020.07.020 · Cited by 523
Metadata
- Authors
- Mullard, A.
- Corresponding author
- Mullard, Asher
- Venue
- Nature Reviews Drug Discovery
- Published
- 2019-03-06
- Volume
- 18
- Issue
- 4
- Pages
- 237-239
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W2920736663
- Cited by
- 146
- References
- 0
- Citations by year
- 2026: 7 · 2025: 8 · 2024: 15 · 2023: 18 · 2022: 16 · 2021: 28 · 2020: 32 · 2019: 20
- Type
- other
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Nature Reviews Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Prostate Cancer Treatment and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ubiquitin and proteasome pathways
- Keywords
- targeted protein degradation, PROTACs, clinical trials, protein degraders, anticancer agents, E3 ubiquitin ligase, drug development
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