A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agents
Brilliant N Marak1, Jayanta Dowarah1, Laldingluaia Khiangte1
1Department of Chemistry, School of Physical Sciences, Mizoram University, Aizawl, 796004, Mizoram, India.
Abstract:
Cancer is one of the major leading causes of death worldwide despite many breakthroughs in the development of novel anticancer drugs. The heterodimer CDK-Cyclin complex plays an essential role in regulating cellular processes. For example, epigenetics, neuronal activity, gene transcription, metabolism, DNA repair, angiogenesis, and hematopoiesis. Consequently, CDKs are often deregulated and over-expressed, causing an uncontrolled proliferation in tumors. Due to their active role in cell cycle regulation and transcription activity, CDKs are conceived as promising targets to overcome cell proliferation. Therefore, designing and developing efficient Cyclic Dependent Kinase inhibitors is progressively becoming a credible solution in treating cancers. This review article emphasized the recent developments of cyclic dependent Kinase inhibitors with insights into their structure-activity relationship, molecular docking, and mechanism of action.
Insights
Novel anticancer drugs targeting Cyclin-Dependent Kinases (CDKs) are crucial for cancer treatment. This review highlights recent developments in CDK inhibitors, focusing on their structure-activity relationships and mechanisms.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Cancer remains a leading global cause of death despite advances in anticancer drug development.
- Cyclin-Dependent Kinase (CDK)-Cyclin complexes are vital regulators of cellular processes, including cell cycle, gene transcription, and DNA repair.
- Deregulation and overexpression of CDKs contribute to uncontrolled tumor cell proliferation, making them attractive therapeutic targets.
Purpose of the Study:
- To review recent advancements in the development of Cyclin-Dependent Kinase (CDK) inhibitors for cancer therapy.
- To provide insights into the structure-activity relationships (SAR) of these inhibitors.
- To discuss the molecular docking and mechanisms of action of novel CDK inhibitors.
Main Methods:
- Literature review of recent scientific publications on CDK inhibitors.
- Analysis of structure-activity relationships based on published data.
- Summary of molecular docking studies and proposed mechanisms of action.
Main Results:
- Several novel CDK inhibitors have been developed, showing promising efficacy in preclinical studies.
- Structure-activity relationship studies have identified key molecular features for potent and selective CDK inhibition.
- Molecular docking and mechanistic studies elucidate how these inhibitors interact with CDK targets.
Conclusions:
- Cyclin-Dependent Kinase inhibitors represent a credible and evolving strategy for cancer treatment.
- Understanding SAR and molecular interactions is key to designing more effective and targeted anticancer therapies.
- Continued research into CDK inhibitors holds significant potential for overcoming cancer cell proliferation.
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