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関連する概念動画

Directing Proteins to the Rough Endoplasmic Reticulum01:34

Directing Proteins to the Rough Endoplasmic Reticulum

17.9K
The organelle-specific signaling sequences direct proteins synthesized in the cytosol to their final destination like ER, mitochondria, peroxisomes, etc. Some of the proteins directed to ER are then trafficked via vesicles to other organelles within the cell or the extracellular environment through the Golgi complex. For example, the rough ER synthesizes soluble proteins for transportation to the lysosomes or secretion out of the cell. It can also synthesize transmembrane proteins that can...
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Protein-protein Interfaces02:04

Protein-protein Interfaces

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Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a...
14.8K
Protein and Protein Structure02:15

Protein and Protein Structure

88.9K
Proteins are one of the most abundant organic molecules in living systems and have the most diverse range of functions of all macromolecules. Proteins may be structural, regulatory, contractile, or protective. They may serve in transport, storage, or membranes; or they may be toxins or enzymes. Their structures, like their functions, vary greatly. They are all, however, amino acid polymers arranged in a linear sequence.
A protein's shape is critical to its function. For example, an enzyme...
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Protein Folding01:22

Protein Folding

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Overview
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Directing Effect of Substituents: meta-Directing Groups01:09

Directing Effect of Substituents: meta-Directing Groups

6.0K
Substituents on the benzene ring that direct an incoming electrophile to undergo substitution at the meta position are called meta directors. All meta directors either have a positive charge on the atom directly bonded to the ring or a partial positive charge. These groups function by withdrawing electrons from the ring through inductive and resonance effects. Consider the carbocation intermediates formed upon the addition of an electrophile on nitrobenzene at the...
6.0K
Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

9.7K
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.
These groups modify specific amino acids in a protein....
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Updated: Feb 12, 2026

Targeting Cysteine Thiols for in Vitro Site-specific Glycosylation of Recombinant Proteins
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システイン誘導型タンパク質ターゲティング用のモジュラービニルフォスフォナミデート.

Christian E Stieger1,2, Charlotte Völkel1,3, Mathias B Bertelsen1

  • 1Leibniz-Forschungsinstitut für Molekulare Pharmakologie (FMP), Robert-Rössle-Straße 10, 13125 Berlin, Germany.

Journal of the American Chemical Society
|February 10, 2026
PubMed
まとめ

ビニルフォスフォナミデート (VPA) は,コヴァレンント阻害剤開発の選択性を向上させる新しいシステイン電極である. これらの化合物は,標的外効果の減少を示し,PROTACsを介して標的タンパク質の分解を可能にします.

さらに関連する動画

Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry
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Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry

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Author Spotlight: A Selective Luciferase-Based Assay for Monitoring ATG4B 27 Activity in Cells
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Author Spotlight: A Selective Luciferase-Based Assay for Monitoring ATG4B 27 Activity in Cells

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関連する実験動画

Last Updated: Feb 12, 2026

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11:25

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Synthesis of Protein Bioconjugates via Cysteine-maleimide Chemistry
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科学分野:

  • 薬用化学 薬用化学について
  • 化学生物学 化学生物学とは
  • ドラッグ・ディスカバリー・ディスカバリー・ドラッグ・ディスカバリー・ドラッグ・ディスカバリー

背景:

  • システイン残留を標的とする共振性阻害剤は,薬剤発見とプロテオミクスにおいて不可欠である.
  • クロロアセタミドやアクリラミドのような既存の電ophilesは,選択性の制限があります.

研究 の 目的:

  • 選択性システイン電愛体の新しいクラスとして,ビニルフォスフォナミデート (VPA) を導入する.
  • VPAの反応性,選択性,およびコヴァレンント阻害剤およびPROTACの開発における有用性を評価する.

主な方法:

  • グルタチオンおよびヒト細胞溶解酸でVPAの反応性を評価した.
  • VPA機能化されたアファチニブおよびイブルーチニブ誘導体を開発した.
  • ゲルベースの活動ベースのタンパク質プロファイリング (ABPP) と質量スペクトロメトリーベースのアクティビティベースのタンパク質プロファイリング (ABPP) を利用しました.
  • VPAベースのタンパク質分解標的キメラ (PROTAC) を構築しました.

主要な成果:

  • VPAは,従来の電化分子よりも低い内在的反応性を表しています.
  • VPAデリバティブは,限られた非特異的反応性と,オフターゲットの関与の減少を示した.
  • VPA機能化された薬は,阻害剤の効率性を維持した.
  • 標的型タンパク質分解のためのVPAベースのPROTACが成功裏に開発されました.

結論:

  • VPAは,システイン誘導コヴァラント変異のための選択的およびモジュール型の電ophilic クラスを表します.
  • VPAは,好ましい反応性プロファイルを持つ共振性阻害剤を開発するための化学的空間を拡大します.
  • VPAは,PROTACの開発を通じて,標的型タンパク質分解戦略を容易にする.