Selective degradation of target proteins by chimeric small-molecular drugs, PROTACs and SNIPERs

Minoru Ishikawa, Shusuke Tomoshige, Yosuke Demizu, Mikihiko Naito

Research output: Contribution to journalReview article

Abstract

New therapeutic modalities are needed to address the problem of pathological but undruggable proteins. One possible approach is the induction of protein degradation by chimeric drugs composed of a ubiquitin ligase (E3) ligand coupled to a ligand for the target protein. This article reviews chimeric drugs that decrease the level of specific proteins such as proteolysis targeting chimeric molecules (PROTACs) and specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein erasers (SNIPERs), which target proteins for proteasome-mediated degradation. We cover strategies for increasing the degradation activity induced by small molecules, and their scope for application to undruggable proteins.

Original languageEnglish
Article number74
JournalPharmaceuticals
Volume13
Issue number4
DOIs
Publication statusPublished - 2020 Apr

Keywords

  • Chemical protein degradation
  • PROTACs
  • SNIPERs

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science

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