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相关概念视频

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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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...
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Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

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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...
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Drug Discovery: Overview01:26

Drug Discovery: Overview

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

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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...
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Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

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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...
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Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

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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...
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相关实验视频

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A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer
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A Flow Cytometry-Based Cell Surface Protein Binding Assay for Assessing Selectivity and Specificity of an Anticancer Aptamer

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药物挑战癌症目标使用基于碎片的方法.

Stephen W Fesik1

  • 1Department of Biochemistry, Chemistry, and Pharmacology, Vanderbilt University, Nashville, Tennessee 37235 United States.

Chemical reviews
|March 5, 2025
PubMed
概括

基于碎片的药物发现识别了对挑战癌症点的配体,这些点以前被认为是无法治疗的. 这种方法可以准缺乏适合传统小分子结合口袋的蛋白质,从而推进癌症治疗方法.

科学领域:

  • 药用化学 医学化学
  • 药物发现 药物发现 药物发现
  • 在瘤学瘤学.

背景情况:

  • 许多经过验证的癌症标缺乏常规小分子抑制剂的可用药物口袋.
  • 以前无法制药的蛋白质在癌症药物开发中提出了重大挑战.
  • 基于碎片的方法为克服这些局限性提供了一个有希望的策略.

研究的目的:

  • 为提供基于碎片的连接体发现的概述.
  • 为了说明基于碎片的方法在识别对挑战性癌症标的配体中的应用.
  • 突出基于片段的方法的潜力,用于以前无法用药的蛋白质.

主要方法:

  • 基于碎片的连接体发现原则的概述.
  • 案例研究展示了基于碎片的方法的应用.
  • 识别高亲缘关系联体对困难的癌症标.

主要成果:

  • 基于碎片的方法成功地确定了对挑战性癌症标的配体.
  • 基于片段的方法对以前被认为是不可用药的蛋白质的证明有用性.
  • 通过基于片段的选发现高亲和度连接体.

结论:

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  • 基于碎片的连接体发现是有效的向困难的癌症目标.
  • 这种方法扩大了在瘤学中可用药蛋白的范围.
  • 基于碎片的方法是开发新型癌症治疗方法的宝贵工具.