Development of target protein-selective degradation inducer for protein knockdown

Yukihiro Itoh, Minoru Ishikawa, Risa Kitaguchi, Shinichi Sato, Mikihiko Naito, Yuichi Hashimoto

Research output: Contribution to journalArticlepeer-review

50 Citations (Scopus)

Abstract

Our previous technique for inducing selective degradation of target proteins with ester-type SNIPER (Specific and Nongenetic Inhibitor-of-apoptosis- proteins (IAPs)-dependent Protein ERaser) degrades both the target proteins and IAPs. Here, we designed a small-molecular amide-type SNIPER to overcome this issue. As proof of concept, we synthesized and biologically evaluated an amide-type SNIPER which induces selective degradation of cellular retinoic acid binding protein II (CRABP-II), but not IAPs. Such small-molecular, amide-type SNIPERs that induce target protein-selective degradation without affecting IAPs should be effective tools to study the biological roles of target proteins in living cells.

Original languageEnglish
Pages (from-to)3229-3241
Number of pages13
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number10
DOIs
Publication statusPublished - 2011 May 15
Externally publishedYes

Keywords

  • CRABP-II
  • IAPs
  • Protein degradation inducer
  • Protein knockdown

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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