通过抗癌天然产品超化物/ZJ-101对内膜系统进行调节
Phillip R Sanchez1,2, Sarah A Head2, Shan Qian3
1National Center for Advancing Translational Sciences (NCATS), National Institutes of Health, Rockville, MD 20892, USA.
International journal of molecular sciences
|June 10, 2023
概括
海洋化合物ZJ-101是一种超体A模拟物,通过破坏内膜系统和抑制O-糖化,显示出强大的抗癌作用. 这种海洋天然产品类似物可能会在三阴性乳腺癌中逆转化疗抵抗.
科学领域:
- 海洋天然产品化学 海洋天然产品化学
- 癌症生物学 癌症生物学
- 药物发现 药物发现
背景情况:
- 海洋天然产品为药物开发提供了多样化的分子结构.
- 超体A是一种海洋天然产品,其作用机制尚不清楚.
- ZJ-101是一种超化物A的简化模拟物.
研究的目的:
- 研究ZJ-101.1的抗增殖和抗粘性作用.
- 阐明ZJ-101.1的作用机制.
- 探索ZJ-101在克服化学抵抗方面的潜力.
主要方法:
- 基于细胞系的测定,用于抗增殖和抗粘性活性.
- 剂量反应转录组学用于识别分子标.
- 莱克和糖基分析以研究糖基化.
- 三重阴性乳腺癌球形模型来评估化学阻力逆转.
主要成果:
- ZJ-101在癌细胞上表现出强大的抗增殖和抗粘性作用.
- 转录学揭示ZJ-101通过调节内膜系统而选择性抑制O-糖化.
- 在三阴性乳腺癌模型中,ZJ-101显示出逆转3D诱导化学抵抗的潜力.
结论:
- ZJ-101是一种海洋天然产品模拟物,具有显著的抗癌特性.
- 该机制涉及通过内膜系统破坏选择性抑制O-糖化.
- 作为克服癌症化学抵抗的协同治疗剂,ZJ-101具有前途.
相关概念视频
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
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
Receptor Downregulation in MVBs
2.1K
Multivesicular bodies (MVBs) are mature endosomes that sort ubiquitinated proteins and then fuse with lysosomes to degrade the sorted proteins. Epidermal growth factor (EGF) and its receptor (EGFR) form a complex that can be internalized through endocytosis, sorted into an MVB, and later degraded.
The EGFR can initiate signaling pathways that lead to cell proliferation, migration, and differentiation. Overexpression of EGFR stimulates cells to proliferate. Excessive EGFR...
The EGFR can initiate signaling pathways that lead to cell proliferation, migration, and differentiation. Overexpression of EGFR stimulates cells to proliferate. Excessive EGFR...
2.1K
Destabilization of Microtubules
2.8K
The destabilization of microtubules can occur during different stages of the microtubule lifecycle, such as nucleation or elongation. It can take place at either end of the microtubule or in the microtubule lattices as a whole. The lifespan of individual microtubules within a cell varies according to the cell type and stage of the cell cycle. During interphase, the lifespan of the microtubule is about 30 minutes, while during cell division, it is about 15 minutes. In axonal microtubules of...
2.8K
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
Cancer Stem Cells and Tumor Maintenance
5.0K
Early diagnosis and treatment can often cure cancer. However, even with treatment, residual cells called cancer stem cells (CSC) might remain, often causing tumor recurrence. These cancer stem cells possess the potential for self-renewal and multi-lineage differentiation and are often responsible for the therapeutic resistance displayed in most cancers.
Cancer stem cells are thought to originate from tissue-specific normal stem cells or progenitor cells. The normal stem cells usually reside in...
Cancer stem cells are thought to originate from tissue-specific normal stem cells or progenitor cells. The normal stem cells usually reside in...
5.0K


