瘤学中的OXPHOS向药物:新的视角
Balaraman Kalyanaraman1, Gang Cheng1, Micael Hardy2
1Department of Biophysics, Medical College of Wisconsin, Milwaukee, WI, USA.
Expert opinion on therapeutic targets
|September 22, 2023
概括
针对线粒体的药物显示出对癌症治疗的希望. 基于三酸 (TPP+) 的药物选择性地向癌细胞线粒体,以最小的毒性抑制增殖,提供一种新的治疗策略.
科学领域:
- 线粒体医学是指线粒体医学.
- 癌症治疗方法 癌症治疗方法
- 药物开发 药物开发
背景情况:
- 针对线粒体的药物正在成为有前途的抗瘤疗法.
- 一些针对线粒体的药物已观察到临床毒性.
- 开发改性天然化合物和FDA批准的药物,具有增强的治疗指数是一个关键的战略.
研究的目的:
- 讨论针对线粒体的改性天然化合物和FDA批准的药物作为癌症治疗的替代策略.
- 突出基于三酸 (TPP+) 的药物在癌症治疗中的潜力.
- 强调需要对这些新型治疗方法进行临床翻译.
主要方法:
- 基于TPP+的药物的选择性积累在癌细胞线粒体中,这是由于膜潜力的改变.
- 针对线粒体电子运输链中的氧化酸化蛋白.
- 抑制线粒体呼吸和瘤扩散.
主要成果:
- 基于TPP+的药物选择性地积聚在线粒体中,抑制瘤增殖.
- 这些药物在临床前模型和人类中表现出最小的有毒副作用.
- 基于TPP+的药物可以使癌细胞对辐射和免疫疗法的敏感.
结论:
- 基于TPP+的药物代表了一种具有抗癌潜力的新型氧化酸化抑制剂类.
- 这些药物由天然产品和FDA批准的药物合成,在临床前研究中显示出低毒性.
- 基于TPP+的OXPHOS抑制药物的临床转化对于癌症的预防和治疗是有必要的.
相关概念视频
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 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
Treatment Resistant Cancers
3.3K
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...
3.3K
Targets for Drug Action: Overview
6.3K
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
6.3K
Electron Transport Chain: Complex I and II
14.3K
The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...
ROS generation is regulated and maintained at moderate levels necessary...
14.3K
Combination Therapies and Personalized Medicine
4.9K
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...
4.9K


