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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.
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Covalently Linked Protein Regulators02:04

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Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
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Transducer Mechanism: Enzyme-Linked Receptors01:27

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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.
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The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
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The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
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Cyclic Adenosine Monophosphate (cAMP) is an essential second messenger that activates protein kinase A (PKA) and regulates various biological processes. A single epinephrine molecule binds to GPCR and activates several heterotrimeric G proteins, each stimulating multiple adenylyl cyclase, amplifying the signal, and synthesizing large numbers of cAMP molecules. Small changes in cAMP concentration affect PKA activity. The binding of four cAMP molecules induces a conformational change in PKA,...
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Updated: Jun 14, 2025

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs
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针对表观遗传蛋白质的PROTACs

Chao Zhang1, Yuna He2, Xiuyun Sun1

  • 1Changping Laboratory, Beijing 102206, China.

Acta materia medica
|September 2, 2024
PubMed
概括
此摘要是机器生成的。

像PROTACs这样的表观遗传蛋白质降解剂提供了针对引起疾病的蛋白质的新方法,有可能在表观遗传疗法中克服药物耐药性.

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相关实验视频

Last Updated: Jun 14, 2025

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Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes

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科学领域:

  • 分子生物学分子生物学
  • 遗传学 是一个遗传学.
  • 药理学 药理学是指药理学的学科.

背景情况:

  • 表观遗传学涉及遗传的基因功能变化,而不会改变DNA序列.
  • 作者,读者和擦拭者的表观遗传调节对于发展和稳定至关重要.
  • 表观遗传蛋白是药物开发的关键目标,但耐药性是一个挑战.

研究的目的:

  • 审查针对表观遗传调节器的新型降解剂 (编写器,阅读器,擦拭器).
  • 探索表观遗传蛋白质降解剂的新应用.
  • 针对表观遗传标的 PROTAC 领域的挑战,并提出解决方案.

主要方法:

  • 对最近开发的表观遗传蛋白质降解剂的文献综述.
  • 对针对表观遗传点的蛋白质分解向化体 (PROTACs) 的分析.
  • 讨论该领域的挑战和未来方向.

主要成果:

  • 针对表观遗传编写者,读者和擦拭器的各种降解剂的摘要.
  • 确定这些降解剂的新兴应用.
  • 讨论PROTAC技术当前的局限性和潜在的进步.

结论:

  • 表观遗传蛋白质降解剂在克服药物耐药性方面表现有前途.
  • PROTACs提供了一种策略,用于向以前无法药物治疗的表观遗传蛋白.
  • 对于表观遗传性疾病的治疗,在PROTAC开发中的持续创新至关重要.