生細胞内の疾患関連タンパク質を 減少させる低分子創薬手法の開発

Minoru Ishikawa, Yuichi Hashimoto

研究成果: Article査読

抄録

New therapeutic modalities are great interests in pharmaceutical researchers. We believe that induction of selective degradation of target proteins by small molecules could become a new therapeutic modality of drug discovery. And we speculated that formation of an artificial (nonphysiological) complex of cIAP1 (cellular inhibitor of apoptosis protein 1) and a target protein would be induced by a hybrid small molecule composed of a cIAP1 ligand linked to a ligand of the target protein, and this would lead to cIAP1-mediated ubiquitination and subsequent proteasomal degradation of the target protein. This review article summarizes advances in chemical protein knockdown, that is, the small hybrid molecules induce decrease of the target proteins in living cells. This article also describes that this technology is capable of degrading receptors, enzymes, substrate binding proteins, and aggregation-prone proteins.

寄稿の翻訳タイトルDegradation of disease related proteins in living cells by small molecules
本文言語Japanese
ページ(範囲)402-413
ページ数12
ジャーナルYuki Gosei Kagaku Kyokaishi/Journal of Synthetic Organic Chemistry
78
5
DOI
出版ステータスPublished - 2020

Keywords

  • Inhibitor of apoptosis protein
  • Neurodegenerative disorders
  • PROTACs
  • SNIPERs
  • Small molecule protein degrader
  • Ubiquitin proteasome system

ASJC Scopus subject areas

  • 有機化学

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