Jove
Visualize
联系我们
JoVE
x logofacebook logolinkedin logoyoutube logo
关于 JoVE
概览领导团队博客JoVE 帮助中心
作者
出版流程编辑委员会范围与政策同行评审常见问题投稿
图书馆员
用户评价订阅访问资源图书馆顾问委员会常见问题
研究
JoVE JournalMethods CollectionsJoVE Encyclopedia of Experiments存档
教育
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab Manual教师资源中心教师网站
使用条款与条件
隐私政策
政策

相关概念视频

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

7.8K
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...
7.8K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

4.9K
The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
4.9K
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

5.7K
Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
5.7K

您也可能阅读

相关文章

通过共同作者、期刊和引用图与本文相关的文章。

排序
Same author

Trends in psychotropic use among older adults with dementia in Korean long-term care hospitals across the COVID-19 pandemic: a national longitudinal study.

Frontiers in public health·2026
Same author

Erratum to "'Site-specific enrichment of highly sialylated N-glycans in an erythropoietin-hybrid Fc fusion protein" [Eur. J. Pharm. Biopharm. 226 (2026) 115147].

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V·2026
Same author

Limited Cross-Neutralization of Emerging SARS-CoV-2 BA.3.2.2 After LP.8.1-Updated Vaccination.

Journal of medical virology·2026
Same author

Differential Wound Healing Potential of Tonsil Parenchymal and Epithelial Mesenchymal Stromal Cell-Derived Exosomes.

Tissue engineering and regenerative medicine·2026
Same author

Site-specific enrichment of highly sialylated N-glycans in an erythropoietin-hybrid Fc fusion protein.

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V·2026
Same author

Clinical outcomes associated with Korean medicine home-visit care for patients with cognitive impairment: a multi-center retrospective observational study.

Scientific reports·2026

相关实验视频

Updated: Sep 9, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
05:33

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

Published on: November 9, 2020

10.1K

基于N-Degron的PROTAC针对PLK1:对于宫癌的潜在治疗策略

Pethaiah Gunasekaran1,2, Sang Chul Shin3, Yeon Sil Hwang2

  • 1Division of Magnetic Resonance, Korea Basic Science Institute (KBSI), Ochang, Cheongju 28119, Republic of Korea.

Pharmaceutics
|August 28, 2025
PubMed
概括

一种新型的PROTAC分子NC1在宫癌细胞中有效降解波罗样激酶1 (PLK1),在临床前模型中显示它有望克服化学抵抗并抑制瘤生长.

关键词:
在 N-degronN端规则路径其他:这里是 PROTAC抗癌药物

更多相关视频

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

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

Published on: May 15, 2019

13.3K
Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.4K

相关实验视频

Last Updated: Sep 9, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
05:33

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

Published on: November 9, 2020

10.1K
Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
10:44

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

Published on: May 15, 2019

13.3K
Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.4K

科学领域:

  • 癌症学
  • 分子生物学
  • 药物发现

背景情况:

  • 宫癌对全球健康构成重大挑战.
  • 目前的化疗选择因耐药性而受到限制,需要新的治疗策略.
  • 在宫癌中,波洛样酶1 (PLK1) 过度表达,是潜在的治疗点.

研究的目的:

  • 开发一种针对PLK1的新型蛋白质分解向化学分子 (PROTAC).
  • 研究这种PROTAC在降解PLK1及其对子宫癌细胞的影响的疗效.
  • 在临床前模型中评估PROTAC的治疗潜力.

主要方法:

  • 开发一种新型的PROTAC,NC1,通过N端规则路径向PLK1蛋白.
  • 在HeLa细胞中评估PLK1蛋白耗尽.
  • 使用异热定位热量计 (ITC) 测定PBD-NC1复合物的结构分析和结合亲和度.
  • 在体外评估细胞活力,细胞循环停止和亡诱导.
  • 在HeLa异种移植小鼠模型中对瘤生长抑制的体内评估.

主要成果:

  • 在 HeLa 细胞中,PROTAC NC1 成功诱导了 PLK1 蛋白的降解.
  • 结构研究证实了NC1和PLK1PBD之间的关键结合相互作用,ITC确定结合亲和度为6. 06μM.
  • 在实验室中,NC1显示出显著的抗癌作用,包括细胞活力降低 (IC50为5. 23μM),G2/ M阶段停止和亡诱导.
  • 在体内研究表明,NC1抑制了小鼠模型中的瘤生长.

结论:

  • 针对PLK1的基于N-degron的PROTAC是一种有前途的癌症治疗策略.
  • 开发的PROTAC,NC1显示出克服宫癌化学抵抗的显著潜力.
  • 这项研究支持开发用于未来宫癌治疗策略的新型PLK1向PROTAC.