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Targeted protein degraders crowd into the clinic
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In the citing paper
“Although some have entered clinical trials with a primary focus on PROTAC, the diverse range of protein regulation methods has undoubtedly laid a robust foundation for developing drugs targeting previously undruggable proteins.477–479”
From Recent advances in targeting the “undruggable” proteins: from drug discovery to clinical trials (2023) · cites this paper as [478]
In the citing paper
“Indeed, this exciting technology is currently transitioning to the clinic, with several PROTACs now in clinical trials.16,31”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [31]
In the citing paper
“Chemical diversification of known glue degraders, especially IMiDs, has delivered derivatives that are even approaching the clinic.16,31”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [31]
In the citing paper
“The Helios glue degrader DKY709 (Fig. 8) from Novartis is in Phase I for solid cancers (currently tested as monotherapy and in combination with spartalizumab, an anti-PD-1).16,31”
From Chasing molecular glue degraders: screening approaches (2022) · cites this paper as [31]
In the citing paper
“Twenty years after its theoretical conception, at least 15 targeted protein degraders, among them heterobifunctional PROTACs and molecular glues, had entered the clinic by the end of 2021 (ref.30) (Tables 1,2), and many more are expected to follow.”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [30]
In the citing paper
“DT2216 is in phase I trials30”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [30]
In the citing paper
“Degrader drugs currently on the market (the IMiD class) and the overwhelming majority of newly developed PROTACs and molecular glue compounds currently in clinical trials (Tables 1,2) target various types of cancer30,163.”
From PROTAC targeted protein degraders: the past is prologue (2022) · cites this paper as [30]
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Metadata
- Authors
- Mullard, A.
- Corresponding author
- Mullard, Asher
- Venue
- Nature Reviews Drug Discovery
- Published
- 2021-03-18
- Volume
- 20
- Issue
- 4
- Pages
- 247-250
- ISSN
- 1474-1776 (ISSN-L)
- 1474-1784
- OpenAlex
- W3136448722
- Cited by
- 409
- References
- 0
- Citations by year
- 2026: 42 · 2025: 51 · 2024: 78 · 2023: 85 · 2022: 104 · 2021: 48
- Type
- other
- Language
- en
- Open access
- closed
- Locations
- Nature Reviews Drug Discovery (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, PROTACs, heterobifunctional degraders, molecular glues, clinical development, drug approval
- MeSH terms
- Drug Development, Animals, Humans, Proteins, Drug Discovery, Proteolysis
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