黄素的化学修饰增加了它对低喉癌的功效
Linlin Zhang1, Lei Cheng2, Zhemeng Chen2
1Shanghai Minhang District Dental Clinic, Shanghai, China.
Journal of drug targeting
|August 14, 2023
概括
一种新型的黄素类似物,L42H17,通过抑制NFκB通路,有效向下腺癌. 这种化合物在临床前模型中显示出显著的抗癌作用,显示出未来治疗开发的前景.
科学领域:
- 在瘤学瘤学.
- 分子生物学分子生物学
- 药物发现 药物发现 药物发现
背景情况:
- 低癌呈现出不良预后,NFκB通路过活化与其进展有关.
- 开发针对性治疗下癌的向疗法仍然是一个临床挑战.
研究的目的:
- 开发一种新型治疗剂,以向喉癌中NFκB通路.
- 为了评估一种修饰的黄素化合物的抗癌潜力,L42H17.
主要方法:
- 化学修饰黄素以产生L42H17,一种单碳烯类同类物.
- 评估L42H17对NFκB信号传递,细胞循环和低喉癌细胞的亡的影响.
- 在患者衍生瘤异种移植 (PDTX) 模型中评估L42H17的疗效.
主要成果:
- L42H17显示增强了与MD2的结合,并抑制了TNF-α诱导的NFκB激活.
- 该化合物通过非活化cdc2-cyclin B1复合体来诱导G2-M细胞循环停止.
- 在PDTX模型中,L42H17促进了亡,并在PDTX模型中显示出显著的抗癌疗效.
结论:
- L42H17是一种有前途的候选药物,用于治疗下喉癌.
- 用L42H17准NFκB通路提供了一个潜在的治疗策略.
相关概念视频
Cancer Therapies
7.7K
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...
7.7K
Mutagenicity and Carcinogenicity
1.3K
Mutagenicity and carcinogenicity refer to the ability of drugs to cause genetic defects and induce cancer, respectively. The International Agency for Research on Cancer (IARC) classifies agents into four groups based on their carcinogenic potential. Group 1 agents are known human carcinogens; group 2A agents are probably carcinogenic to humans; group 3 agents lack data to support their role in carcinogenesis; and group 4 includes agents for which data support that they are not likely to be...
1.3K
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
315
Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
Two synthetic agonists of THC,...
315
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
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
199
Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy. SP binds and activates...
199
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


