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Protac Synthesis 1


  • ミリグラムからグラムスケール、さらにそれ以上まで迅速にスケールアップ可能な合成能力
  • 創薬のニーズに対応し新規リンカーを開発する能力
  • Homo-PROTAC、Partial-PROTAC、および、SNIPERの実績
  • 新規化合物の結合強度と物理化学的性状を最適化する能力
  • 迅速なターゲットエンゲージメントのためのPartial-PROTACとリンカーの自社ライブラリー
  • 合成化学と統合的な創薬サポート
  • in vitro, in vivoプロファイリング、DMPK、おおよび、毒性試験を含むバイオロジーサポート

E3リガーゼリガンドと標的結合リガンドのリンクに必要な多種多様なリンカーも合成しています。それらは、ほとんど全ての標的との結合に有効なように設計されたPEGリンカー、–NH2, –CO2H, –N3, –C≡CH, –CHO, –X および –OH等の官能基を含む炭素鎖ベースのリンカーを含みます。

Protac Synthesis 2

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Protac Synthesis 3


弊社PROTACの創薬化学を補完するものとして、タンパク質分解に関わるバイオロジーの豊富な経験と共に、多様なアッセイ系、DMPKおよび毒性試験を含む包括的なin vitroバイオロジーサポートを提供致しております。


  • TR-FRET生化学的アッセイ(EnVision Xcite)
  • 標的タンパク質分解を評価するためのセルベースアッセイ(Hi-Bit、Nano-Bitその他) DC50値の計算を含みます。
  • 初期ADME試験(例えば、透過性、溶解性、ミクロソーム代謝安定性)
  • げっ歯類によるPK試験
  • Xenograft 試験およびその他PDモデル
  • 毒性試験
  • タンパク質三元複合体の分析
  • 詳細な情報はこちら

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Target Protein degradation is a process in which the protein of interest is degraded using E3 ubiquitin ligase and a chemical linker by polyubiquitination followed by proteasome degradation.

High target selectivity demonstrates high potencies, less toxic ,and minimizing the risk of developing resistance.

A targeting ligand (warhead) for the protein of interest and a ligand that recruits an E3 ubiquitin ligase connected via a carefully-chosen chemical linker (PROTAC). The resulting compound can induce formation of a ternary complex (the target, degradation compound and E3 ligase). The design of degrader compounds is critical to form an effective ternary complex.

The addition of ubiquitin to a substrate protein is called ubiquitination. Ubiquitination of target proteins involves a three-step enzymatic process, i.e., Activation, conjugation, and Ligation. Finally, polyubiquitinated proteins are recognized by the proteasome then degrades into small peptides by proteolysis.

Cellular Permeability and Target Affinity are the important factors to decide the effective binding of PROTAC with target protein and ubiquitination. These parameters play a crucial role in the designing of PROTAC molecules.

PROTACs regulate protein function by degrading target proteins instead of inhibiting them, providing more sensitivity to drug-resistant targets and a greater chance of affecting nonenzymatic functions. PROTACs have been proven to show better selectivity compared to classic inhibitors. It has attracted great attention both from academia and industry.

Catalytic in nature, targeted degradation and selectivity provide a niche for PROTAC applications in cancer diseases and immune disorders, viral infections, and neurodegenerative diseases.

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