相关实验视频

Updated: Jan 16, 2026

Isolation and Screening from Soil Biodiversity for Fungi Involved in the Degradation of Recalcitrant Materials

Isolation and Screening from Soil Biodiversity for Fungi Involved in the Degradation of Recalcitrant Materials

Published on: May 16, 2022

发现一种具有持久降解活动的强大和选择性的TEAD降解剂

Linhui Cao^1,2, Jing Yang³, Yuhang Liu^1,2

¹School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, China, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, China.

Advanced science (Weinheim, Baden-Wurttemberg, Germany)

|October 5, 2025

概括

一种新的TEAD降解剂,KG-FP-003,通过破坏Hippo通路,对癌细胞表现出强有力的和选择性的活性. 这种化合物为各种癌症提供了有前途的治疗策略,包括子宫内膜癌和质母细胞瘤.

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:

TEA/ATSS (TEAD) 转录因子是Hippo途径的关键效应因子,与YAP和TAZ联合激活剂相互作用.
针对YAP-TEAD相互作用是癌症治疗的关键策略,具有重要的学术和工业利益.

研究的目的:

报告发现和描述KG-FP-003,一种新的TEAD降解剂.
与现有抑制剂相比,评估KG-FP-003的疗效和选择性.

主要方法:

KG-FP-003的特点是它在TEAD异型体中具有降解活性.
评估了乌比基-蛋白酶体系统 (UPS) 的依赖性.
评估了体外和体外治疗反应.
使用条形码细胞系查来识别敏感的癌症类型.

主要成果:

通过UPS,KG-FP-003在低纳米分子度下证明了所有TEAD异型的强大,选择性和持久的降解.
它的性能优于MYF-03-176 (LBP抑制剂) 和IAG933 (TEAD-YAP PPI抑制剂).
在体外和体内,KG-FP-003诱导了优越和持续的治疗反应.
在子宫内膜癌,质母细胞瘤,卵巢瘤和骨肉瘤中观察到过度敏感性.

结论:

KG-FP-003是TEAD异型选择性癌症疗法的一个引人注目的主要候选者.
它的潜力超越了间皮瘤,扩展到其他Hippo-dysregulated癌症.

关键词:

我们的 TEAD TEAD 团队.哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈哈化学探测器化学探测器降解剂降解剂是一种降解剂.河马的路径河马的路径

更多相关视频

Isolation of Native Soil Microorganisms with Potential for Breaking Down Biodegradable Plastic Mulch Films Used in Agriculture

Isolation of Native Soil Microorganisms with Potential for Breaking Down Biodegradable Plastic Mulch Films Used in Agriculture

Published on: May 10, 2013

Prospecting Microbial Strains for Bioremediation and Probiotics Development for Metaorganism Research and Preservation

Prospecting Microbial Strains for Bioremediation and Probiotics Development for Metaorganism Research and Preservation

Published on: October 31, 2019

相关概念视频

Bioremediation

Bioremediation

Bioremediation is the use of prokaryotes, fungi, or plants to remove pollutants from the environment. This process has been used to remove harmful toxins in groundwater as a byproduct of agricultural run-off and also to clean up oil spills.

Olefin Metathesis Polymerization: Acyclic Diene Metathesis (ADMET)

Olefin Metathesis Polymerization: Acyclic Diene Metathesis (ADMET)

Acyclic diene metathesis polymerization or ADMET polymerization involves cross-metathesis of terminal dienes, such as 1,8-nonadiene, to give linear unsaturated polymer and ethylene. As ADMET is a reversible process, the formed ethylene gas must be removed from the reaction mixture to complete the polymerization process.
Similar to cross-metathesis, ADMET also involves the formation of metallacyclobutane intermediate by [2+2] cycloaddition of one of the double bonds of a terminal diene with...

Enzyme Inhibition

Enzyme Inhibition

Inhibitors are molecules that reduce enzyme activity by binding to the enzyme. In a normally functioning cell, enzymes are regulated by a variety of inhibitors. Drugs and other toxins can also inhibit enzymes. Some inhibitors bind to the enzyme’s active site, while others inhibit enzymatic activity by binding to other sites on the protein structure.