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

Erscheinungsjahr:

2024

Erschienen:

2024

Enthalten in:

Zur Gesamtaufnahme - volume:16

Enthalten in:

Future medicinal chemistry - 16(2024), 4 vom: 07. Feb., Seite 369-388

Sprache:

Englisch

Beteiligte Personen:

Zheng, Mingming [VerfasserIn]
Zhang, Xiao-Yu [VerfasserIn]
Chen, Weijiao [VerfasserIn]
Xia, Fei [VerfasserIn]
Yang, Huanaoyu [VerfasserIn]
Yuan, Kai [VerfasserIn]
Yang, Peng [VerfasserIn]

Links:

Volltext

Themen:

Antineoplastic Agents
CDKs
Cancer
Cyclin-Dependent Kinase 2
Cyclin-Dependent Kinase 4
Cyclin-Dependent Kinase 6
Cyclin-Dependent Kinases
Degraders
EC 2.7.11.22
Journal Article
Molecular glue
PROTAC
Protein Kinase Inhibitors
Review

Anmerkungen:

Date Completed 07.02.2024

Date Revised 07.02.2024

published: Print-Electronic

Citation Status MEDLINE

doi:

10.4155/fmc-2023-0259

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM367789094