Targeting proteins for degradation. Nat Chem Biol. 2009;5:815-22.Schrader EK, Harstad KG, Matouschek A. Targeting proteins for degradation. Nat Chem Biol. Nature Publishing Group; 2009 Nov 1; 5(11):815-22. https://doi.org/10.1038/nchembio.250 PMID: 19841631...
Selectively targeting proteins for degradation Phthalimide-based drugs such as thalidomide, which have been successfully repurposed for the treatment of multiple myeloma, have recently been shown to bind to cereblon (CRBN; part of an ubiquitin E3 ligase complex). This promotes the recruitment of two ...
To understand the molecular functions of SAP, we purified the GFP–SAP complex from35S:GFP-SAPtransgenic plants and identified SAP-associated proteins using mass spectrometry. As shown inSupplementary Fig. 9, ASK1, ASK2 and CUL1 (Cullin1) were detected in the GFP–SAP complex. Considering that...
Proteolysis-targeting chimeras: Harnessing the ubiquitin-proteasome system to induce degradation of specific target proteins. Annu. Rev. Cancer Biol. 2018, 2... KG Coleman,CM Crews - 《Annual Review of Cancer Biology》 被引量: 3发表: 2018年 PROteolysis Targeting Chimeras: A new cutting‐edge na...
Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. A bifunctional PROTAC molecule consists of a ligand (mostly small-molecule inhibitor) of the protein of interest (POI) and a covalently
UPS is a highly conserved mechanism for degradation of both normal and misfolded proteins in eukaryotic cells, thus keeping intracellular protein homeostasis [28,29,30]. In UPS, proteins to be degraded are covalently tagged with ubiquitin (Ub, a 76-amino acid protein), and this tagging process...
It also interacts with the LC3 protein, thereby mediating degradation of ubiquitin-decorated cargo like misfolded proteins and aggregates. The LC3‒p62 interaction is viewed as a potential PPI target for autophagy intervention. Tanaka et al.91 performed a screening of ∼10,000 compounds for LC3...
p>Selective protein degradation platforms have afforded new development opportunities for therapeutics and tools for biological inquiry. The first lysosome targeting chimeras (LYTACs) targeted extracellular and membrane proteins for degradation by bridging a target protein to an endogenous lysosome targeting re...
Protein-degradation platforms such as proteolysis-targeting chimaeras (PROTACs)1,2 and others (for example, dTAGs3, Trim-Away4, chaperone-mediated autophagy targeting5 and SNIPERs6) have been developed for proteins that are typically difficult to target; however, these methods involve the ...
In addition to phosphorylation, mitosis mainly depends on the strict regulation of proteins by ubiquitination [5]. Ubiquitination is a post-translational modification, which involves tagging proteins for degradation, and is mediated by ubiquitin-activating (E1), -conjugating (E2), or -ligating (E3)...