67319-28-2Relevant articles and documents
Live-Cell Protein Modification by Boronate-Assisted Hydroxamic Acid Catalysis
Adamson, Christopher,Kajino, Hidetoshi,Kanai, Motomu,Kawashima, Shigehiro A.,Yamatsugu, Kenzo
, p. 14976 - 14980 (2021/09/29)
Selective methods for introducing protein post-translational modifications (PTMs) within living cells have proven valuable for interrogating their biological function. In contrast to enzymatic methods, abiotic catalysis should offer access to diverse and new-to-nature PTMs. Herein, we report the boronate-assisted hydroxamic acid (BAHA) catalyst system, which comprises a protein ligand, a hydroxamic acid Lewis base, and a diol moiety. In concert with a boronic acid-bearing acyl donor, our catalyst leverages a local molarity effect to promote acyl transfer to a target lysine residue. Our catalyst system employs micromolar reagent concentrations and affords minimal off-target protein reactivity. Critically, BAHA is resistant to glutathione, a metabolite which has hampered many efforts toward abiotic chemistry within living cells. To showcase this methodology, we installed a variety of acyl groups inE. colidihydrofolate reductase expressed within human cells. Our results further establish the well-known boronic acid-diol complexation as abona fidebio-orthogonal reaction with applications in chemical biology and in-cell catalysis.
Polyethylene glycol monomethyl ether statin compound and preparation method thereof
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Paragraph 0018, (2018/04/21)
The invention relates to a polyethylene glycol monomethyl ether statin compound and a preparation method thereof. The method mainly comprises the following steps: 1) activating an end group of polyethylene glycol monomethyl ether; and 2) connecting the activated polyethylene glycol monomethyl ether statin compound by amino acid or oligopeptide to obtain the polyethylene glycol monomethyl ether statin compound. The polyethylene glycol monomethyl ether statin compound has a structure: mPEG-(A)i-(statins)j, wherein mPEG is polyethylene glycol monomethyl ether and has a structure as shown in the specification, n is an integer ranging from 1 to 24, A is amino acid or oligopeptide, i is an integer ranging from 1 to 6, statins are statin compounds, and j is an integer ranging from 1 to 6. The load rate of a drug is increased by the statin compounds modified by polyethylene glycol. Due to the modification of polyethylene glycol, the absorption of the drum is improved, the acting time is prolonged, the curative effect is enhanced, and toxic or side effects are avoided.
PEPTIDIC LINKERS AND CRYPTOPHYCIN CONJUGATES, USEFUL IN THERAPY, AND THEIR PREPARATION
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, (2018/12/02)
The present disclosure relates to compounds of formula (I): RCG1-L-P (I) wherein RCG1 represents a reactive chemical group being reactive towards a chemical group present on a polypeptide such as an antibody; P represents H, OH or an activated O; and L represents a specific linker. The disclosure also relates to cryptophycin payloads, as well as to cryptophycin conjugates, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these conjugates.
Dissociative reactions of benzonorbornadienes with tetrazines: Scope of leaving groups and mechanistic insights
Xu,Galindo-Murillo,Cheatham,Franzini
supporting information, p. 9855 - 9865 (2017/12/12)
Bioorthogonal dissociative reactions boast diverse potential applications in chemical biology and drug delivery. The reaction of benzonorbornadienes with tetrazines to release amines from carbamate leaving groups was recently introduced as a bioorthogonal bond-cleavage reaction. The present study aimed at investigating the scope of leaving groups that are compatible with benzonorbornadienes. Synthesis of several benzonorbornadienes with different releasable groups is reported, and the reaction of these molecules with tetrazine was found to be rapid and afforded high release yields. The tetrazine-induced release of molecules proceeds in a cascade of steps including inverse-electron demand cycloaddition and cycloreversion reactions that form unstable isoindoles/isobenzofuran intermediates and spontaneously eliminate a leaving group of interest. In the case of oxygen-bridged BNBDs at room temperature, we observed the formation of an unproductive byproduct.
ONIUM SALT, LIQUID COMPOSITION CONTAINING SAID ONIUM SALT AND CELLULOSE, AND CELLULOSE RECOVERY METHOD
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Paragraph 0128; 0129; 0130; 0131; 0132; 0133, (2016/02/19)
The invention relates to an onium salt, a liquid composition containing the onium salt and cellulose, and a method for recovering cellulose. The invention makes it possible to provide an onium salt having an extremely high ability to dissolve cellulose at temperatures of 100° C. or lower. It also makes it possible to provide a liquid composition containing this onium salt and cellulose, as a composition suitable for the recovery of cellulose, and a method for recovering cellulose efficiently by using such a liquid composition containing the onium salt and cellulose.
METHOD OF SYNTHESIZING A SUBSTANTIALLY MONODISPERSED MIXTURE OF OLIGOMERS
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, (2011/06/10)
The present invention relates to methods of synthesizing oligomeric compounds, and more particularly, to methods of synthesizing oligomer compounds comprising polyethylene glycol moieties. The present invention provides improved methods for synthesizing oligomers comprising polyethylene glycol moieties. Methods according to embodiments of the present invention may utilize reaction conditions that are milder, efficacious than those taught by conventional methods.
Oligo(p-phenylene-ethynylene)s with backbone conformation controlled by competitive intramolecular hydrogen bonds
Hu, Wei,Yan, Qifan,Zhao, Dahui
supporting information; experimental part, p. 7087 - 7094 (2011/07/09)
A series of conjugated oligo(p-phenylene-ethynylene) (OPE) molecules with backbone conformations (that is, the relative orientations of the contained phenylene units) controlled by competitive intramolecular hydrogen bonds to be either co-planar or random
