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Recent progress of SRC family kinase inhibitors as anticancer agents
Xin Cao1, Qi-Dong You, Zhi-Yu Li
1Jiangsu Key Laboratory of Carcinogenesis and Intervention, Department of Medicinal Chemistry, China Pharmaceutical University, No. 24, Tongjiaxiang Rd, Nanjing 210009, Jiangsu Province, PR China.
Abstract:
Src family of protein tyrosine kinases (SFKs) play key roles in regulating signal transduction in cellular processes. However, hyper-activated SFKs lead to uncontrolled cell proliferation and cancers. Many SFKs inhibitors were designed and synthesized as anticancer agents in the past several years and great progress has been made. Herein, some predominant examples of SFKs inhibitors recently developed are reviewed and special attentions are paid to the most important ATP binding site inhibitors.
Insights
Src family of protein tyrosine kinases (SFKs) are crucial for cell signaling but their hyper-activation causes cancer. Recent advancements have yielded promising SFKs inhibitors, particularly targeting the ATP binding site for cancer therapy.
Area of Science:
- Biochemistry
- Molecular Biology
- Oncology
Background:
- Src family of protein tyrosine kinases (SFKs) regulate critical cellular signaling pathways.
- Aberrant SFK activity is implicated in uncontrolled cell proliferation and the development of various cancers.
Purpose of the Study:
- To review recently developed inhibitors targeting Src family of protein tyrosine kinases (SFKs).
- To highlight inhibitors specifically designed to target the ATP binding site of SFKs.
Main Methods:
- Literature review of predominant SFKs inhibitors.
- Focus on recent advancements in inhibitor design and development.
Main Results:
- Significant progress has been made in the design and synthesis of SFKs inhibitors.
- Several potent inhibitors targeting the ATP binding site have emerged.
Conclusions:
- SFKs inhibitors represent a promising therapeutic strategy for cancer treatment.
- Targeting the ATP binding site is a key approach for developing effective SFKs inhibitors.
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