一个洞察力thymidylate合成酶抑制剂作为抗癌药物:一个解释性审查
Aratrika Sen1, Dipanjan Karati2
1Department of Pharmaceutical Technology, School of Pharmacy, Techno India University, Kolkata, 700091, West Bengal, India.
Naunyn-Schmiedeberg's archives of pharmacology
|March 6, 2024
概括
乙基胺酸合成酶 (TS) 对于DNA合成至关重要,其失调驱动癌症. 抑制TS是一种有前途的治疗策略,可以减缓癌症的进展并提高化疗的有效性.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 在瘤学瘤学.
背景情况:
- 癌症是一种复杂的疾病,是由分子变化驱动的.
- 乙基胺酸合成酶 (TS) 对于DNA合成至关重要,它将dUMP转化为dTMP.
- 失调的TS活性与各种癌症有关,包括乳腺癌,结肠癌,肺癌和卵巢癌.
研究的目的:
- 审查胺酸合成酶 (TS) 在癌症发展和进展中的作用.
- 探索TS的调节机制,包括microRNA的参与.
- 评估在癌症治疗中针对TS的治疗潜力.
主要方法:
- 在癌症中对胺酸合成酶 (TS) 的研究的文献综述.
- 分析涉及TS的分子相互作用和信号通路.
- 通过微RNAs (miRNAs) 检查TS调节.
- 评估TS抑制作为一种抗癌策略.
主要成果:
- TS过度表达或突变有助于不受控制的细胞增殖和瘤发生.
- 微RNAs (miRNAs) 可以通过准其信使RNA来调节TS活动.
- 抑制TS显示在减缓癌细胞分裂和生长方面具有前途.
- 新型抗叶酸TS抑制剂对更广泛的瘤,包括肺癌,显示出有效性.
- 转基因抑制剂可以使癌症组织对化疗和放射治疗敏感.
结论:
- 乙基酸合成酶 (TS) 是癌症发展中的关键酶,也是一个可行的治疗点.
- 用小分子抑制剂,特别是新型抗叶剂向TS,为癌症治疗提供了一个有希望的策略.
- 抑制TS可以提高常规疗法 (如化疗和放射治疗) 的有效性.
- 对TS的分子机制和抑制策略的进一步研究是改善癌症治疗的必要条件.
相关概念视频
Inhibition of Cdk Activity
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...
Targeted Cancer Therapies
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 specific...
There are several types of targeted therapies against specific...
Combination Therapies and Personalized Medicine
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...
Targeted Cancer Therapies
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 specific...
There are several types of targeted therapies against specific...
Tumor Immunotherapy
Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...


