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Chemistries of bifunctional PROTAC degraders
Chemical Society Reviews, 2022Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic strategy using small molecules to induce ubiquitin-dependent degradation of proteins.
Chaoguo Cao +4 more
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Bifunctional Molecules beyond PROTACs
Journal of Medicinal Chemistry, 2020Heterobifunctional molecules, which recruit E3 ligases to ubiquitinate a target protein of interest, have found wide application as both biological tools and molecules with the potential to have clinical effects. In their recent paper, Yamazoe et al. report a heterobifunctional molecule that recruits the phosphatase PP1 to promote the dephosphorylation
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Targeted protein degradation by PROTACs
Pharmacology & Therapeutics, 2017Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases driven by the aberrant expression of a disease-causing protein. PROTAC molecules are bifunctional small molecules that simultaneously bind a target protein and an E3-ubiquitin ligase, thus causing ubiquitination and degradation of the ...
Taavi K, Neklesa +2 more
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Progress in the controllability technology of PROTAC
European Journal of Medicinal ChemistryProteolysis-targeting chimaera (PROTAC) technology functions by directly targeting proteins and catalysing their degradation through an event-driven mode of action, a novel mechanism with significant clinical application prospects for various diseases.
Xin He, Zhibing Weng, Yi Zou
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Efficient PROTAC-ing: combinational use of PROTACs with signaling pathway inhibitors
Trends in Biochemical SciencesTargeted protein degradation is an innovative therapeutic modality for the degradation of disease-causing proteins. In a recent report combining high-throughput screening of small-molecule compounds and biochemical analyses, Mori et al. identified certain inhibitors of cellular pathways, such as PARylation and proteostatic pathways, which enhance ...
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