862778-54-9Relevant articles and documents
Development of an ON/OFF switchable fluorescent probe targeting His tag fused proteins in living cells
Okitsu, Koyo,Misawa, Takashi,Shoda, Takuji,Kurihara, Masaaki,Demizu, Yosuke
, p. 3417 - 3422 (2017)
The fluorescent labeling of target proteins is useful for analyzing their functions and localization in cells, and several fluorescent probes have been developed. However, the fusion of tags such as green fluorescent protein (GFP) to target proteins occas
Development of a Small Hybrid Molecule That Mediates Degradation of His-Tag Fused Proteins
Okitsu, Koyo,Hattori, Takayuki,Misawa, Takashi,Shoda, Takuji,Kurihara, Masaaki,Naito, Mikihiko,Demizu, Yosuke
, p. 576 - 582 (2018)
In recent years, the induction of target-protein degradation via the ubiquitin-proteasome system (UPS) mediated by small molecules has attracted attention, and this approach has applications in pharmaceutical development. However, this technique requires a ligand for the target protein that can be incorporated into tailor-made molecules, and there are many proteins for which such ligands have not been found. In this study, we developed a protein-knockdown method that recognizes a His-tag fused to a protein of interest. This strategy theoretically allows comprehensive targeting of proteins of interest by a particular molecule recognizing the tag. As expected, our hybrid molecule 10 [SNIPER(CH6)] efficiently degraded His-tagged CRABP-II and Smad2 in cells. This system provides an easy method to determine the susceptibility of proteins of interest to UPS-mediated degradation. Furthermore, we hope that this method will become an efficient tool to analyze the function of the UPS.
High-Affinity Copolymers Inhibit Digestive Enzymes by Surface Recognition
Gilles, Patrick,Wenck, Kirstin,Stratmann, Inga,Kirsch, Michael,Smolin, Daniel A.,Schaller, Torsten,De Groot, Herbert,Kraft, Arno,Schrader, Thomas
, p. 1772 - 1784 (2017/06/19)
This account presents a general method for the construction of polymeric surface binders for digestion enzymes. Two prominent parts, namely, the modification of the copolymer composition and the screening assay for the most powerful inhibitors are both am