27274-31-3Relevant articles and documents
Synthetic analogues of glycosylphosphatidylinositol-anchored proteins and their behavior in supported lipid bilayers
Paulick, Margot G.,Wise, Amber R.,Forstner, Martin B.,Groves, Jay T.,Bertozzi, Carolyn R.
, p. 11543 - 11550 (2007)
Positioned at the C-terminus of many eukaryotic proteins, the glycosylphosphatidylinositol (GPI) anchor is a posttranslational modification that anchors the modified proteins in the outer leaflet of the plasma membrane. GPI-anchored proteins play vital ro
Chain extender as well as preparation method and application thereof
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Paragraph 0038; 0041; 0043; 0046; 0048; 0051, (2022/01/20)
The invention relates to a chain extender. The chain extender is 3-(2-(2, 3-dihydroxy propyl) sulfo) ethyoxyl) propyl 3-(3-(tert-butyl)-4-hydroxy-5-methyl phenyl) propionate (GL), and the structural formula of the chain extender is shown in the specification. The prepared chain extender GL has an excellent toughening effect; the elongation at break of a polyurethane elastomer prepared from the GL reaches 1531.1594%, the toughness reaches 12.315% MJ/m , the repairing efficiency reaches 103.62% after the polyurethane elastomer is repaired for 6 h at the normal temperature, and the repairing efficiency reaches 125.53% after the polyurethane elastomer is repaired for 2 h at the temperature of 80 DEG C. The prepared chain extender GL can be compounded with other reinforced chain extenders so as to be used, and the tensile strength and toughness of the polyurethane elastomer are further improved synergistically.
Non-natural amino acid and application thereof Recombinant protein and recombinant protein conjugate comprising same
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Paragraph 0094; 0098; 0099-0100, (2021/10/27)
The invention provides a non-natural amino acid. A compound represented by formula (I) or an enantiomer thereof. The invention also provides application of the non-natural amino acid. Further, the present invention also provides a protein conjugate comprising the recombinant protein and of the non-natural amino acid prepared from the recombinant protein. The non-natural amino acid provided by the invention is simple and convenient to prepare, good in safety, not prone to inactivation when inserted into a protein, high in coupling ratio with a coupling part, good in stability of the obtained conjugate, and capable of being applied to various fields, especially in preparation of recombinant protein or recombinant protein conjugate.
Fenton-Inspired C-H Functionalization: Peroxide-Directed C-H Thioetherification
Groendyke, Brian J.,Modak, Atanu,Cook, Silas P.
, p. 13073 - 13091 (2019/10/10)
Substoichiometric iron mediates the thioetherification of unactivated aliphatic C-H bonds directed by resident silylperoxides. Upon exposure to a catalytic amount of iron(II) triflate, TIPS-protected peroxides bearing primary, secondary, and tertiary C-H sites undergo chemoselective thioetherification of remote C-H bonds with diaryl disulfides. The reaction demonstrates a broad substrate scope and functional group tolerance without the use of any noble metal additives. Mechanistic experiments suggest that the reaction proceeds through 1,5-H atom abstraction by a hydroxyl radical generated with iron.
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
Zoppi, Vittoria,Hughes, Scott J.,Maniaci, Chiara,Testa, Andrea,Gmaschitz, Teresa,Wieshofer, Corinna,Koegl, Manfred,Riching, Kristin M.,Daniels, Danette L.,Spallarossa, Andrea,Ciulli, Alessio
, p. 699 - 726 (2019/01/11)
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive for degradation. We describe a probe-quality degrader for a ligase-target pair deemed unsuitable: the von Hippel-Lindau (VHL) and BRD9, a bromodomain-containing subunit of the SWI/SNF chromatin remodeling complex BAF. VHL-based degraders could be optimized from suboptimal compounds in two rounds by systematically varying conjugation patterns and linkers and monitoring cellular degradation activities, kinetic profiles, and ubiquitination, as well as ternary complex formation thermodynamics. The emerged structure-activity relationships guided the discovery of VZ185, a potent, fast, and selective degrader of BRD9 and of its close homolog BRD7. Our findings qualify a new chemical tool for BRD7/9 knockdown and provide a roadmap for PROTAC development against seemingly incompatible target-ligase combinations.
A single-mercapto double-cetyl the ether gathers glycol [...] glycolipid synthesis method (by machine translation)
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Paragraph 0062-0065, (2019/11/04)
The invention discloses a single mercapto double-cetyl [...] glycol [...] glycolipid synthesis method, characterized in that the 2, 3, 4, 6 - O - acetyl - α - D - pyran mannose the heat stability of the polyurethane in the [...][...] benzoic acid with thr
Stereoselective Synthesis of Molecular Square and Granny Knots
Leigh, David A.,Pirvu, Lucian,Schaufelberger, Fredrik
supporting information, p. 6054 - 6059 (2019/04/26)
We report on the stereoselective synthesis of both molecular granny and square knots through the use of lanthanide-complexed overhand knots of specific handedness as three-crossing "entanglement synthons". The composite knots are assembled by combining two entanglement synthons (of the same chirality for a granny knot; of opposite handedness for a square knot) in three synthetic steps: first, a CuAAC reaction joins together one end of each overhand knot. Ring-closing olefin metathesis (RCM) then affords the closed-loop knot, locking the topology. This allows the lanthanide ions necessary for stabilizing the entangled conformation of the synthons to subsequently be removed. The composite knots were characterized by 1H and 13C NMR spectroscopy and mass spectrometry and the chirality of the knot stereoisomers compared by circular dichroism. The synthetic strategy of combining building blocks of defined stereochemistry (here overhand knots of λ- or Δ-handed entanglement) is reminiscent of the chiron approach of using minimalist chiral synthons in the stereoselective synthesis of molecules with multiple asymmetric centers.
Stapling of two PEGylated side chains increases the conformational stability of the WW domain via an entropic effect
Xiao, Qiang,Bécar, Natalie A.,Brown, Nathaniel P.,Smith, Mason S.,Stern, Kimberlee L.,Draper, Steven R.E.,Thompson, Katherine P.,Price, Joshua L.
supporting information, p. 8933 - 8939 (2018/12/10)
Hydrocarbon stapling and PEGylation are distinct strategies for enhancing the conformational stability and/or pharmacokinetic properties of peptide and protein drugs. Here we combine these approaches by incorporating asparagine-linked O-allyl PEG oligomers at two positions within the β-sheet protein WW, followed by stapling of the PEGs via olefin metathesis. The impact of stapling two sites that are close in primary sequence is small relative to the impact of PEGylation alone and depends strongly on PEG length. In contrast, stapling of two PEGs that are far apart in primary sequence but close in tertiary structure provides substantially more stabilization, derived mostly from an entropic effect. Comparison of PEGylation + stapling vs. alkylation + stapling at the same positions in WW reveals that both approaches provide similar overall levels of conformational stability.
TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
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Paragraph 1461, (2018/05/24)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
NOVEL TRIAZINE COMPOUND, ALL-SOLID-STATE POLYMER ELECTROLYTE COMPOSITION AND USE THEREOF
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Paragraph 0123; 0139-0142, (2018/04/12)
The present invention relates to a novel triazine compound represented by chemical formula 1, an all-solid-state polymer electrolyte composition comprising the same as a cross-linking agent and uses thereof. More specifically, the triazine compound effectively inhibits crystallization of a plasticizer at a low temperature (room temperature) to show significantly improved ion conductivity, and can realize significantly improved electrochemical stability and excellent battery properties, thereby being usefully used as an all-solid-state polymer electrolyte composition such as a lithium-polymer secondary battery, a dye-sensitized solar cell, etc.COPYRIGHT KIPO 2018
