Recent advances in regulating the cell cycle through inhibiting CDKs for cancer treatment.
10.1016/S1875-5364(25)60846-6
- Author:
Weijiao CHEN
1
;
Xujie ZHUANG
1
;
Yuanyuan CHEN
1
;
Huanaoyu YANG
1
;
Linhu SHEN
1
;
Sikai FENG
1
;
Wenjian MIN
2
,
3
;
Kai YUAN
3
,
4
;
Peng YANG
5
Author Information
1. State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
2. State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China. Electronic address: min1218xx@
3. com.
4. State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China. Electronic address: cpuyk1993@
5. State Key Laboratory of Natural Medicines and Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 211198, China. Electronic address: pengyang@cpu.edu.cn.
- Publication Type:Review
- Keywords:
CDK inhibitor;
Cell cycle;
Cyclin-dependent kinase (CDK);
Resistance
- MeSH:
Humans;
Cell Cycle/drug effects*;
Protein Kinase Inhibitors/chemistry*;
Cyclin-Dependent Kinases/metabolism*;
Neoplasms/genetics*;
Antineoplastic Agents/pharmacology*;
Animals;
Breast Neoplasms/enzymology*;
Cyclin-Dependent Kinase 4/metabolism*
- From:
Chinese Journal of Natural Medicines (English Ed.)
2025;23(3):286-298
- CountryChina
- Language:English
-
Abstract:
The inhibition of cyclin-dependent kinases (CDKs) is considered a promising strategy for cancer treatment due to their role in cell cycle regulation. However, CDK inhibitors with no selectivity among CDK families have not been approved. A CDK inhibitor with high selectivity for CDK4/6 exhibited significant treatment effects on breast cancer and has become a heavy bomb on the market. Subsequently, resistance gradually decreased the efficacy of selective CDK4/6 inhibitors in breast cancer treatment. In this review, we first introduce the development of selective CDK4/6 inhibitors and then explain the role of CDK2 activation in inducing resistance to CDK4/6 inhibitors. Moreover, we focused on the development of CDK2/4/6 inhibitors and selective CDK2 inhibitors, which will aid in the discovery of novel CDK inhibitors targeting the cell cycle in the future.
