Affiliation:
1. Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo 113-0033, Japan
2. National Institute of Health Sciences, Kawasaki 210-9501, Japan
3. Graduate School of Medical Life Science, Yokohama City University, Yokohama 230-0045, Japan
Abstract
Transcription factors (TFs) and RNA-binding proteins (RBPs) have long been considered undruggable, mainly because they lack ligand-binding sites and are equipped with flat and narrow protein surfaces. Protein-specific oligonucleotides have been harnessed to target these proteins with some satisfactory preclinical results. The emerging proteolysis-targeting chimera (PROTAC) technology is no exception, utilizing protein-specific oligonucleotides as warheads to target TFs and RBPs. In addition, proteolysis by proteases is another type of protein degradation. In this review article, we discuss the current status of oligonucleotide-based protein degraders that are dependent either on the ubiquitin–proteasome system or a protease, providing a reference for the future development of degraders.
Funder
Japan Society for the Promotion of Science
Japan Agency for Medical Research and Development
Princess Takamatsu Cancer Research Fund
Terumo Foundation for Life Sciences and Arts
Takeda Science Foundation
Naito Foundation
Sumitomo Foundation
the Novartis Foundation (Japan) for the Promotion of Science
Japan Foundation of Applied Enzymology
Kobayashi Foundation for Cancer Research
Foundation for the Promotion of Cancer Research in Japan
Tokyo Biochemical Research Foundation
Cited by
2 articles.
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