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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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Items 101–144 of 144
Arbel, Y. S., Katz, B., Gabizon, R., Shraga, A., Bronstein, Y., Kamdjou, T., Levin, A. G., Perry, C., Avivi, I. M., London, N., et al. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.646971 · Cited by 16
“Taken together, PROTACs represent a very promising and powerful approach for the development of targeted therapy drugs, as was recently underscored by the first PROTAC, ARV-110, to enter clinical trials (12).”
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Drinan, S. D., Bass, J. I. F., & Bass, J. I. F. (2023) · Transcription · doi:10.1080/21541264.2023.2294623 · Cited by 15
“PROTACs function by linking a ligand targeting the protein of interest to a ligand that binds an E3 ligase, inducing proteasomal degradation of the target protein via ubiquitination (Figure 2d) [185,186].”
Pedrucci, F., Pappalardo, C., Marzaro, G., Ferri, N., Ferlin, A., & Toni, L. D. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23126630 · Cited by 14
“efficacy of as many new PROTACs in the context of neoplastic and chronic-degenerative pathologies [3,4].”
BackgroundDegradation of extracellular and membrane proteins in targeted therapy: Status quo and quo vadis
Li, Z., Ma, S., Zhang, S., Ma, Z., Du, L., & Li, M. (2023) · Drug Discovery Today · doi:10.1016/j.drudis.2023.103716 · Cited by 14
Inducing the Degradation of Disease-Related Proteins Using Heterobifunctional Molecules
Delport, A., & Hewer, R. (2019) · Molecules · doi:10.3390/molecules24183272 · Cited by 14
“Both an estrogen receptor alpha (ERα) PROTAC (ARV-471, DC50 = 2 nM) [52] and androgen receptor targeting PROTACs (AR PROTAC, DC50 1 nM [53] and ARV-110 [54]) have been developed, although their structures are nondisclosed (Table 1).”
BackgroundInfluentialTargeting Cullin-RING Ubiquitin Ligases and the Applications in PROTACs
Gong, L., Cui, D., Xiong, X., & Zhao, Y. (2020) · Advances in experimental medicine and biology · doi:10.1007/978-981-15-1025-0_19 · Cited by 13
The von Hippel–Lindau Cullin-RING E3 ubiquitin ligase regulates APOBEC3 cytidine deaminases
Scholtés, G. K., Sawyer, A. M., Vaca, C. C., Clerc, I., Roh, M., Song, C., & D’Aquila, R. T. (2021) · Translational research · doi:10.1016/j.trsl.2021.05.002 · Cited by 14
MST and TRIC Technology to Reliably Study PROTAC Binary and Ternary Binding in Drug Development
Bartoschik, T., Zoephel, A., Rumpel, K., Ciulli, A., & Heffern, C. T. R. (2021) · Methods in molecular biology · doi:10.1007/978-1-0716-1665-9_6 · Cited by 15
Engineered PROTAC-CID Systems for Mammalian Inducible Gene Regulation
Ma, D., Yuan, Q., Peng, F., Paredes, V., Zeng, H., Osikpa, E. C., Yang, Q., Peddi, A., Patel, A., Liu, M. S., et al. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c09129 · Cited by 14
Combing the Cancer Genome for Novel Kinase Drivers and New Therapeutic Targets
Torres‐Ayuso, P., & Brognard, J. (2019) · Cancers · doi:10.3390/cancers11121972 · Cited by 14
“With PROTACs entering clinical trials [120], a new era on targeting protein kinases in disease may begin.”
BackgroundPerspectives on the Development of First-in-Class Protein Degraders
Rambacher, K. M., Calabrese, M. F., & Yamaguchi, M. (2021) · Future Medicinal Chemistry · doi:10.4155/fmc-2021-0033 · Cited by 11
Reboud‐Ravaux, M. (2021) · Biologie Aujourd hui · doi:10.1051/jbio/2021007 · Cited by 10
Bioengineered ferritin-based lysosome-targeting chimera platform for tumor-targeted therapy
Zhang, S., Jin, Y., Hou, Y., Tang, G., Wang, Z., Chen, X., Yan, X., & Kelong, F. (2026) · Nature Communications · doi:10.1038/s41467-026-70383-6 · Cited by 15
Epithelial-to-mesenchymal transition as a central driver of tumor cell plasticity
Jiménez-Castaño, R., & Nieto, M. A. (2026) · Nature Cancer · doi:10.1038/s43018-026-01154-x · Cited by 14
Strategic deactivation of mRNA COVID‐19 vaccines: New applications for siRNA therapy and RIBOTACs
Hulscher, N., McCullough, P. A., & Marotta, D. E. (2024) · The Journal of Gene Medicine · doi:10.1002/jgm.3733 · Cited by 9
“95 This problem may be countered by incorporating even smaller RNase-binding ligands in the molecular structure.”
New Frontiers in the Discovery and Development of PROTACs
Barghout, S. H. (2022) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520622666220412132759 · Cited by 8
Design and Applications of Bifunctional Small Molecules in Biology
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From Degraders to Molecular Glues: New Ways of Breaking Down Disease‐Associated Proteins
Nagel, Y. A., Britschgi, A., & Ricci, A. (2021) · Wiley eBooks · doi:10.1002/9783527826872.ch2 · Cited by 6
Ma, C., Hanyin, S., Shen, C., Li, X., & Shen, Y. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.117625 · Cited by 7
The Expanding E3 Ligase-Ligand Landscape for PROTAC Technology
Li, Z., Huang, X., Zhao, X., Zhang, Y., & Li, P. (2025) · Targets · doi:10.3390/targets3040030 · Cited by 9
An overview of recent advancements in targeted cancer therapies and their potential clinical impact
Ahmed, S., Sakla, A. P., Jahan, K., Neshat, N., Akhter, M., Aaghaz, S., & Kamal, A. (2025) · RSC Medicinal Chemistry · doi:10.1039/d5md00740b · Cited by 6
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Targeted Management: Unlocking the Crucial Role of PROTACs in Cancer Treatment
Gupta, P., Dutta, S., Kumar, P., Kaushik, M., Ashique, S., & Bhowmick, M. (2025) · Current Drug Discovery Technologies · doi:10.2174/0115701638324854250218053353 · Cited by 5
Proteome editing using engineered proteins that hijack cellular quality control machinery
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Enhancing c-MYC degradation via 20S proteasome activation induces in vivo anti-tumor efficacyPreprint
Njomen, E., Lansdell, T. A., Vanecek, A. S., Benham, V., Bernard, M. P., Yang, Y.-T., Schall, P. Z., Isaac, D., Alkharabsheh, O. A., Al-Janadi, A., et al. (2020) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2020.08.24.265470 · Cited by 4
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Palbociclib as an Antitumor Drug: A License to Kill
Łupicka‐Słowik, A., Cossu, F., & Sieńczyk, M. (2024) · Molecules · doi:10.3390/molecules29225334 · Cited by 5
“Three main barriers that degraders have to overcome are chemical stability, solubility, and cell membrane permeability [123].”
Siepe, D. H., Picton, L. K., & García, K. C. (2022) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2022.10.31.514624 · Cited by 3
Targeted Protein Degradation: "The Gold Rush is On!"
Kotlarek, D., Pawlik, A., Sagan, M., Sowała, M., Zawiślak-Architek, A., & Walczak, M. (2020) · Technology Transfer and Entrepreneurship · doi:10.2174/2213809907666200130111436 · Cited by 2
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Exploring the Role of PROTACs for the Treatment of Breast Cancer
Pannu, A. S., Goyal, R. K., & Goswami, S. (2024) · Springer eBooks · doi:10.1007/978-981-97-5077-1_12 · Cited by 1
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CDK6 degradation hits Ph+ ALL hard
Hantschel, O. D. (2020) · Blood · doi:10.1182/blood.2020005136 · Cited by 1
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“Moreover, more than 20 PROTACs are currently undergoing clinical trials since 2019 13-16 , indicating that PROTAC technology is a promising therapeutic strategy.”
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Hulscher, N., McCullough, P. A., & Marotta, D. E. (2024) · doi:10.31219/osf.io/qxbgu · Cited by 1
Advances in Protein Degradation
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血管造影(IVR-CT)検査時のデジタルズームによる被曝線量低減の試み(第31回秋季学術大会放射線防護管理関連演題発表後抄録)
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The next frontier in drug discovery: Unveiling the pharmacological potential of proximity inducers
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Ubiquitin Receptor-Mediated, Ubiquitin-Independent Targeted Protein Degradation via 26S ProteasomesPreprint
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Expanding the E3 Ligase Landscape: From Small Molecule to Biological Targeted Protein Degradation
Zhao, X., Liu, Y., & Teng, X. (2026) · Handbook of experimental pharmacology · doi:10.1007/164_2026_842
From discovery to clinic: Medicinal chemistry strategies for PROTAC linker optimization
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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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