在癌症治疗中PRC2的药理学进展:叙述性审查
Michael S Wang1, Jonathan Sussman1, Jessica A Xu1
1Hospital of the University of Pennsylvania, HUP 3400 Spruce St., Philadelphia, PA 19104, USA.
Life (Basel, Switzerland)
|January 8, 2025
概括
聚镇压复合体2 (PRC2) 抑制剂对于癌症治疗至关重要,因为PRC2在瘤发生过程中的双重作用. 本综述强调了有希望的PRC2抑制剂用于治疗淋巴瘤和固体瘤.
科学领域:
- 表观遗传学 在表观遗传学中,表观遗传学是指表观遗传学.
- 分子生物学分子生物学
- 在瘤学瘤学.
背景情况:
- 多镇压复合体2 (PRC2) 通过H3K27甲基化对基因表达进行表观基因调节,影响色素结构和基因沉默.
- PRC2在瘤发生过程中表现出双重作用,既作为瘤基因又作为瘤抑制剂,需要细微的治疗策略.
- 针对PRC2在瘤学应用中提供了治疗漏洞和风险,推动了针对特定抑制剂开发的研究.
研究的目的:
- 进行一个结构化的文献综述,对Polycomb抑制复合体2 (PRC2) 抑制剂.
- 识别和展示具有治疗潜力的PRC2的共同因子竞争抑制剂.
- 为治疗淋巴瘤和固体瘤的有希望的PRC2抑制剂提供统一的观点.
主要方法:
- 关于PRC2及其抑制剂的科学研究的结构化文献综述.
- 对关键的PRC2抑制剂进行分析,包括Tazemetostat,GSK126,Valemetostat和UNC1999.
- 探索针对EED或SUZ12子单元的新兴PRC2抑制剂,例如EED226.
主要成果:
- 塔泽米托斯塔和GSK126对野生型和淋巴瘤相关的EZH2突变体具有很高的选择性.
- 瓦莱梅托斯塔特和UNC1999是口服生物可用,SAM竞争性EZH1/EZH2抑制剂,具有对抗药物耐药性的潜力.
- 目前正在开发针对EED或SUZ12子单元的新型PRC2抑制剂,从而扩大治疗选择.
结论:
- PRC2抑制剂代表了淋巴瘤和固体瘤的有希望的治疗途径.
- 选择性抑制PRC2组件提供了向的癌症治疗策略.
- 对各种PRC2抑制剂的持续研究对于克服治疗挑战和药物耐药性至关重要.
更多相关视频
11:04An In-House-Built and Light-Emitting-Diode-Based Photodynamic Therapy Device for Enhancing Verteporfin Cytotoxicity in a 2D Cell Culture Model
Published on: January 13, 2023
3.0K
07:25A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
13.0K
相关概念视频
Targeted Cancer Therapies
7.4K
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...
7.4K
Cancer Therapies
7.5K
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...
7.5K
Abnormal Proliferation
4.4K
Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
4.4K
Inhibition of Cdk Activity
4.6K
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...
4.6K
Treatment Resistant Cancers
3.2K
Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.2K
Combination Therapies and Personalized Medicine
4.8K
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...
4.8K
