作为癌症治疗的单碳基黄素类似物
Takashi MaruYama1, Hiroyuki Yamakoshi2, Yoshiharu Iwabuchi2
1Department of Organ Anatomy, Tohoku University Graduate School of Medicine.
Biological & pharmaceutical bulletin
|May 31, 2023
概括
与黄相比,新的黄相似物显示出增强的抗瘤作用. 这些单碳化合物通过抑制关键转录因子和激活细胞死亡途径来抑制瘤细胞的生长,为癌症治疗提供了潜在的潜力.
科学领域:
- 自然产品 化学 化学
- 癌症生物学 癌症生物学
- 药理学 药理学是指药理学的学科.
背景情况:
- 黄素表现出抗炎和潜在的抗瘤特性.
- 高剂量要求限制了黄素对癌症的临床疗效.
- 开发黄素类似物旨在改善治疗效果.
研究的目的:
- 合成和评估新型的黄素对抗瘤活性增强的类似物.
- 调查这些类型的抗瘤作用背后的机制.
- 在癌症治疗中讨论单碳基库尔库明类型的临床潜力.
主要方法:
- 合成了50多种库尔库类型,专注于单碳基结构.
- 在各种瘤细胞系中抑制生长的评估.
- 涉及转录活性测试 (NF-κB,STAT3) 和caspase-3激活的机制研究.
- 对瘤细胞代谢的分析.
主要成果:
- 与黄素相比,单碳基黄素类似物显示出优异的瘤细胞生长抑制.
- 观察到主要转录因子的抑制,包括核因子kappa B (NF-κB) 和信号转换器和转录激活器3 (STAT3).
- 激活caspase-3和调节瘤细胞代谢被确定为作用机制.
- 在临床前评估中,类似的药物显示出有前途.
结论:
- 单碳基库尔库明类似物代表了一类具有增强抗瘤活性的有前途的化合物.
- 这些类似物通过准多个癌症途径,提供了潜在的治疗策略.
- 对于癌症治疗,需要对单碳基曲素类型的进一步临床研究.
相关概念视频
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
Drugs that Stabilize Microtubules
2.1K
Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
2.1K
Targeted Cancer Therapies
7.7K
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...
7.7K
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
Cancer Therapies
7.8K
Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
7.8K
Drugs that Destabilize Microtubules
2.0K
Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
2.0K


