Small-molecule degraders of cyclin-dependent kinase protein : a review
Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics involving the induction of protein degradation. Cyclin-dependent kinase (CDK) protein, which is involved in cycles and transcription cycles, participates in regulation of the cell cycle, transcription and splicing. Proteolysis-targeting chimeras targeting CDKs show several advantages over traditional CDK small-molecule inhibitors in potency, selectivity and drug resistance. In addition, the discovery of molecule glues promotes the development of CDK degraders. Herein, the authors describe the existing CDK degraders and focus on the discussion of the structural characteristics and design of these degraders.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:14 |
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| Enthalten in: |
Future medicinal chemistry - 14(2022), 3 vom: 09. Jan., Seite 167-185 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Yu, Bin [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 21.02.2022 Date Revised 21.02.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2021-0154 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM334753716 |
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| 520 | |a Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics involving the induction of protein degradation. Cyclin-dependent kinase (CDK) protein, which is involved in cycles and transcription cycles, participates in regulation of the cell cycle, transcription and splicing. Proteolysis-targeting chimeras targeting CDKs show several advantages over traditional CDK small-molecule inhibitors in potency, selectivity and drug resistance. In addition, the discovery of molecule glues promotes the development of CDK degraders. Herein, the authors describe the existing CDK degraders and focus on the discussion of the structural characteristics and design of these degraders | ||
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| 650 | 4 | |a Review | |
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| 650 | 4 | |a glue degraders | |
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| 650 | 4 | |a ubiquitin-proteasome system | |
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| 700 | 1 | |a Du, Zekun |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Yuming |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Zhiyu |e verfasserin |4 aut | |
| 700 | 1 | |a Bian, Jinlei |e verfasserin |4 aut | |
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