Molecules inducing specific cyclin-dependent kinase degradation and their possible use in cancer therapy
Cyclin-dependent kinases (CDKs) play an important role in the regulation of cell proliferation, and many CDK inhibitors were developed. However, pan-CDK inhibitors failed to be approved due to intolerant toxicity or low efficacy and the use of selective CDK4/6 inhibitors is limited by resistance. Protein degraders have the potential to increase selectivity, efficacy and overcome resistance, which provides a novel strategy for regulating CDKs. In this review, we summarized the function of CDKs in regulating the cell cycle and transcription, and introduced the representative CDK inhibitors. Then we made a detailed introduction about four types of CDKs degraders, including their action mechanisms, research status and application prospects, which could help the development of novel CDKs degraders.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2024 |
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Erschienen: |
2024 |
Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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Enthalten in: |
Future medicinal chemistry - 16(2024), 4 vom: 07. Feb., Seite 369-388 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Zheng, Mingming [VerfasserIn] |
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Links: |
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Anmerkungen: |
Date Completed 07.02.2024 Date Revised 07.02.2024 published: Print-Electronic Citation Status MEDLINE |
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doi: |
10.4155/fmc-2023-0259 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM367789094 |
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520 | |a Cyclin-dependent kinases (CDKs) play an important role in the regulation of cell proliferation, and many CDK inhibitors were developed. However, pan-CDK inhibitors failed to be approved due to intolerant toxicity or low efficacy and the use of selective CDK4/6 inhibitors is limited by resistance. Protein degraders have the potential to increase selectivity, efficacy and overcome resistance, which provides a novel strategy for regulating CDKs. In this review, we summarized the function of CDKs in regulating the cell cycle and transcription, and introduced the representative CDK inhibitors. Then we made a detailed introduction about four types of CDKs degraders, including their action mechanisms, research status and application prospects, which could help the development of novel CDKs degraders | ||
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700 | 1 | |a Chen, Weijiao |e verfasserin |4 aut | |
700 | 1 | |a Xia, Fei |e verfasserin |4 aut | |
700 | 1 | |a Yang, Huanaoyu |e verfasserin |4 aut | |
700 | 1 | |a Yuan, Kai |e verfasserin |4 aut | |
700 | 1 | |a Yang, Peng |e verfasserin |4 aut | |
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