430430-57-2Relevant academic research and scientific papers
NOVEL AUTOPHAGY-TARGETING CHIMERA (AUTOTAC) COMPOUND, AND COMPOSITION FOR PREVENTING, ALLEVIATING, OR TREATING DISEASES THROUGH TARGET PROTEIN DEGRADATION COMPRISING SAME
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, (2021/06/03)
The present invention relates to a novel AUTOTAC chimeric compound in which a new p62 ligand and a target-binding ligand are connected by a linker, a stereoisomer, hydrate, solvate or prodrug thereof, and a pharmaceutical or food composition for the prevention or treatment of diseases by degrading the target protein including the same as an active ingredient. They can target specific proteins to adjust their concentrations, and can also deliver drugs and other small molecule compounds to lysosomes. The AUTOTAC chimeric compound according to the present invention can be usefully used as a pharmaceutical composition for the prevention, amelioration or treatment of various diseases by selectively eliminating specific proteins.
IRAK DEGRADERS AND USES THEREOF
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, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
Photoactivable nonsymmetrical bifunctional linkers for protein immobilization on attenuated total reflectance FTIR optical devices
Hammaecher, Catherine,Joris, Bernard,Goormaghtigh, Erik,Marchand-Brynaert, Jacqueline
, p. 7952 - 7959 (2014/01/06)
The photosensitive 4-azido-2,3,5,6-tetrafluoro-1-benzoyl core has been connected to maleimide-, chloroacetyloxy-, or succinimidyl carbonate motifs through various spacers to furnish a series of bifunctional linkers. One linker (7a) has been used for the construction of a biosensor for β-lactam antibiotic detection by attenuated total reflectance FTIR (ATR-FTIR) spectroscopy. Linkers featuring a photosensitive aryl azide motif at one end and a function reactive toward nucleophiles at the other end are described. One linker is used for the construction of a biosensor for β-lactam antibiotic detection by attenuated total reflectance FTIR spectroscopy. Copyright
LDV peptidomimetics equipped with biotinylated spacer-arms: Synthesis and biological evaluation on CCRF-CEM cell line
Gérard, Estelle,Meulle, Aline,Feron, Olivier,Marchand-Brynaert, Jacqueline
, p. 586 - 590 (2012/03/26)
The tripeptide Leu-Asp-Val (LDV) is known to bind α4β 1 integrin in leukemia cells. Here we have synthesized a LDV peptidomimetic equipped with a biotin-conjugated spacer-arm. Compound 9 acts as an inhibitor of the α4β1 integrin in an adhesion assay using fluorescently labeled, α4β 1 integrin-expressing leukemia CCRF-CEM cells. Furthermore, when bound to neutravidin-coated plates, compound 9 could capture CCRF-CEM cells. Such biotin-conjugated LDV peptidomimetic may thus represent a novel tool for biotechnological applications using avidin interaction for leukapheresis or leukemia cell targeting.
Modular synthesis of bifunctional linkers for materials science
Moreau, Julie,Marchand-Brynaert, Jacqueline
, p. 1641 - 1644 (2011/05/03)
A practical synthesis of α,ω-bifunctional linkers is described that is based on three building blocks, namely, thioctic acid, a spacer-arm of seven ethylene glycol units, and a functional motif dedicated to the selective immobilization of purposely tagged proteins. Such representative motifs are biotin, haloacetamide, maleimide, and nitrilotriacetic acid derivatives. The building blocks are connected through alkyl, amide, and/or carbamate linkages. Copyright
Synthesis of N-propynyl analogues of peptide nucleic acid (PNA) monomers and their use in the click reaction to prepare N-functionalized PNAs
Howarth, Nicola M.,Ricci, Jennyfer
, p. 9588 - 9594 (2011/12/14)
Application of the click reaction for coupling a 2-(2-aminoethoxy)ethoxy (AEE) function to thyminyl, cytosinyl and adeninyl peptide nucleic acid (PNA) monomer analogues bearing a N-propynyl group, in place of the original N-2-aminoethyl moiety, has been explored. The N-propynyl PNA analogues were prepared from glycine ethyl ester hydrochloride and the structure of the thyminyl derivative was confirmed by X-ray diffraction. These monomers were employed in click reactions with Boc-protected AEE azide to afford the corresponding triazolyl-linked PNA-AEE conjugates in yields ranging from 64 to 76%. [1,4]-Regiochemistry was verified from a NOESY correlation experiment.
