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相关概念视频

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

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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...
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M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

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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...
6.2K
Positive Regulator Molecules02:39

Positive Regulator Molecules

6.4K
Mitotic cell division results in daughter cells that exactly resemble the parent cell. However, errors in the DNA replication or distribution of genetic material may lead to genetic mutations that may be passed down to every new cell formed from the resulting abnormal cell. Propagation of such mutant cells is restricted through checkpoint mechanisms present at different stages of the cell cycle. These checkpoints involve regulator molecules that either promote or demote cell cycle events.
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Positive Regulator Molecules01:45

Positive Regulator Molecules

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To consistently produce healthy cells, the cell cycle—the process that generates daughter cells—must be precisely regulated.
133.8K
Anaphase Promoting Complex00:50

Anaphase Promoting Complex

3.3K
The stepwise destruction of specific proteins is necessary for the progression and completion of the cell cycle. Such proteins are ubiquitinated by ubiquitin ligases and then subsequently destroyed by the proteasome. The SCF (Skp1/Cullin/F-box) and the anaphase-promoting complex (APC) are two important ubiquitin ligases involved in cell cycle progression. While SCF is active throughout the cell cycle, APC gets activated during metaphase to anaphase transition. Cdc20 or Cdh1 binds to APC and...
3.3K
S-Cdk Initiates DNA Replication02:38

S-Cdk Initiates DNA Replication

5.3K
The cell cycle is a series of events leading to DNA duplication followed by the division of cell content to form two daughter cells. The cell cycle progresses in four stages—the cell increases in size (gap 1 or G1-phase), duplicates its DNA (synthesis or S-phase), prepares to divide (gap 2 or G2-phase), and divides (mitosis or M-phase).
Two states at the origin of replication
In eukaryotes, the initiation of replication occurs at many sites on the chromosomes, called the origins of...
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相关实验视频

Updated: Jan 9, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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在宏环基CDK抑制剂的近期进展.

Jiamin Zheng1, Zhisen Zhang1, Jinxin Liu2

  • 1Department of Medicinal Chemistry, Insilico Medicine Shanghai Ltd., Shanghai, China.

Future medicinal chemistry
|December 9, 2025
PubMed
概括

宏循环为开发新型环林依赖激酶 (CDK) 抑制剂提供了一个有希望的策略,有可能克服当前癌症疗法所见的耐药性和毒性问题.

关键词:
药物设计 药物设计循环林依赖的激酶.发现药物的发现.宏观循环是一个宏观循环.瘤治疗药物 瘤治疗药物

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Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics
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Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
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Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay

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相关实验视频

Last Updated: Jan 9, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics
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Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
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科学领域:

  • 药用化学 医学化学
  • 在瘤学瘤学.
  • 分子生物学分子生物学

背景情况:

  • 循环素依赖激酶 (CDK) 是细胞循环和转录的关键调节者,使它们成为癌症治疗的关键标.
  • CDK4/6抑制剂已在乳腺癌中取得成功,但耐药性和非标毒性等挑战仍然存在.
  • 基于宏循环的药物设计正在成为提高激酶抑制剂有效性和类似药物的特性的一种策略.

研究的目的:

  • 审查最近宏环化策略的进展,以开发依赖环林的激酶 (CDK) 抑制剂.
  • 突出宏循环支架如何解决当前CDK向疗法的局限性.
  • 探索CDK抑制剂从非循环到宏循环形式的结构演变.

主要方法:

  • 2015-2025年科学出版物和临床试验的文献综述.
  • 分析CDK抑制剂设计中的结构变化,重点关注宏循环化技术.
  • 评估宏环化对酶抑制活性,选择性和类似药物的特性的影响.

主要成果:

  • 宏循环化策略提高了CDK抑制剂的效力和选择性.
  • 宏循环CDK抑制剂显示出克服获得的抵抗机制的潜力.
  • 在宏环设计中观察到改善的药物动力学概况和减少的非目标效应.

结论:

  • 宏循环化代表了设计下一代CDK抑制剂的强大方法.
  • 这些新型宏环剂在改善癌症治疗结果方面具有显著的前景.
  • 进一步的研究和临床评估是有必要的,以充分实现宏环基CDK抑制剂的治疗潜力.