相关实验视频

Updated: Jul 28, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

作为癌症治疗的有效策略,表皮生长因子受体PROTACs:一篇综述

Chao Wang¹, Yujing Zhang², Wujun Chen¹

¹The Affiliated Hospital of Qingdao University, Cancer Institute, Qingdao University, Qingdao 266071, Shandong, China; Qingdao Cancer Institute, Qingdao University, Qingdao 266071, Shandong, China.

Biochimica et biophysica acta. Reviews on cancer

|May 28, 2023

概括

蛋白酶向的嵌合体 (PROTACs) 通过降解表皮生长因子受体 (EGFR) 为癌症治疗提供了一种新的方法. 与传统EGFR抑制剂相比,这些PROTACs显示出更好的疗效和克服耐药性.

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:

皮表皮生长因子受体 (EGFR) 是癌症中关键的瘤原体标,调解关键的细胞过程.
目前的EGFR抑制剂,包括TKI和mAbs,由于耐药性和癌症异质性而面临限制.
在EGFR的催化结构域的变化对传统的向疗法构成重大挑战.

研究的目的:

为提供针对EGFR用于癌症治疗的PROTACs开发的全面概述.
为了突出 PROTACs 与传统 EGFR 抑制剂的优势.
讨论以EGFR为目标的PROTAC领域的挑战和未来机会.

主要方法:

审查最近在异种功能EGFR PROTACs的设计和应用方面的进展.
使用野生类型 (WT) 和突变EGFR TKI的PROTACs的分析.
基于细胞抑制,功效和毒性,PROTAC与传统EGFR抑制剂的比较.

主要成果:

PROTACs利用细胞内蛋白质破坏途径,绕过由占用驱动的小分子的限制.
与传统的EGFR TKI相比,EGFR PROTACs表现出优异的细胞抑制和功效.
PROTACs表现出改善的毒性概况和对抗耐药癌症模型的增强有效性.

结论:

PROTACs代表了一种有希望的新兴疗法,用于向癌症中的EGFR.
针对EGFR的PROTACs的开发提供了一种克服现有的治疗局限性的战略.
对EGFR PROTAC的进一步研究具有促进癌症治疗的巨大潜力.

关键词:

癌症癌症癌症癌症癌症治疗治疗癌症治疗欧洲农业基金会 (EGFR) 是一个基金.这就是 PROTACs.这就是TKI.

更多相关视频

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

Therapeutic Gene Delivery and Transfection in Human Pancreatic Cancer Cells using Epidermal Growth Factor Receptor-targeted Gelatin Nanoparticles

Therapeutic Gene Delivery and Transfection in Human Pancreatic Cancer Cells using Epidermal Growth Factor Receptor-targeted Gelatin Nanoparticles

Published on: January 4, 2012

相关概念视频

Mitogens and the Cell Cycle

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...

Targeted Cancer Therapies

Targeted Cancer Therapies

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...

Transducer Mechanism: Enzyme-Linked Receptors

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:

Combination Therapies and Personalized Medicine

Combination Therapies and Personalized Medicine

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...

Cancer Therapies

Cancer Therapies

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...