在抗癌疗法中准CRAF激酶:进展和机遇
Penglei Wang1,2,3, Kyle Laster3, Xuechao Jia1,2,3
1Department of Pathophysiology, School of Basic Medical Sciences, Zhengzhou University, Zhengzhou, 450000, China.
Molecular cancer
|December 19, 2023
概括
向CRAF (RAF激酶) 对由RAS/RAF瘤基因驱动的癌症至关重要. 这篇综述探讨了CRAF.
科学领域:
- 在瘤学瘤学.
- 分子生物学分子生物学
- 癌症信号通路 癌症信号通路
背景情况:
- 在癌症中,RAS/mitogen-activated protein kinase (MAPK) 途径经常因RAS或RAF瘤基因而失调.
- 作为RAF酶家族成员的CRAF是RAS-MAPK通路和癌症进展的组成部分.
- 越来越多地认识到CRAF在通过MAPK依赖和独立机制对BRAF抑制剂的生理调节和抵抗中的作用.
研究的目的:
- 调查各种癌症中的CRAF变异及其在瘤基因驱动的恶性瘤中的独特作用.
- 总结CRAF相互作用蛋白及其在癌症特征中的调节.
- 讨论泛RAF抑制剂和组合疗法的进展,以提高RAF/RAS突变瘤的疗效和降低毒性.
主要方法:
- 关于癌症中CRAF变化,功能和相互作用的文献综述.
- 对针对CRAF和RAF抑制剂的当前治疗策略的分析.
- 探索抵抗机制和潜在的协同目标.
主要成果:
- CRAF在癌症中发挥着多方面的作用,其激酶活性和独立功能有助于瘤发生和耐药性.
- 仅针对CRAF激酶活性显示有争议的有效性;其激酶独立功能可能在KRAS突变肺癌中至关重要.
- 最近的进展包括泛RAF抑制剂和组合疗法,在RAF/RAS突变癌症中显示出有前途.
结论:
- 对CRAF的不同角色的全面理解对于开发有效的癌症治疗是必不可少的.
- 确定协同目标和阐明抵抗路径是推进组合策略的关键.
- 未来的战略应该集中在针对RAF/RAS驱动的瘤的强大和更安全的组合疗法上.
相关概念视频
Targeted Cancer Therapies
7.6K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
There are several types of targeted therapies against...
7.6K
M-Cdk Drives Transition Into Mitosis
5.6K
Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
5.6K
Inhibition of Cdk Activity
4.8K
The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
4.8K
Combination Therapies and Personalized Medicine
4.9K
Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
4.9K
Transducer Mechanism: Enzyme-Linked Receptors
2.5K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
Major types that are helpful drug targets include:
2.5K
mTOR Signaling and Cancer Progression
3.8K
The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
The mTOR pathway or the...
3.8K


