In this work, complexes of cysteine proteases, namely bromelain, papain and ficin, with a graft copolymer of chitosan and poly(N,N-dimethyl amino ethyl methacrylate) were obtained. It was determined that the enzyme catalytic activity in the complexes is reduced compared to their native forms. The results of molecular docking showed that modified polysaccharide located in the catalytic pocket of cysteine proteases globules. The resulting complexes have increased stability when stored under physiological conditions, which makes them promising candidates for use in the development of treatments for wounds.
The toxicity and aggressive nature of hydrogen fluoride have resulted in development of alternative strong Lewis acid-based reagents for final deprotection and cleavage steps in Boc/Bzl peptide synthesis. The acids employed are high-boiling liquids unlike hydrogen fluoride, however most peptides could be quite easily isolated from the cleavage cocktails due to their favorable physico-chemical properties: they are usually precipitated with ether. We found that this simple procedure is not suitable for the isolation of Deltorphin II peptides and its analogues. Therefore we developed alternative isolation methods and successfully purified these peptides. The procedures developed could be utilized in purification of other hydrophibic peptides.
We report a series of orto-substituted aryliden-imidazolones and their derivatives containing styrene moiety. These compounds can be used like ligands of NanoLuc protein. Together with NanoLuc this fluorogens can be used for genetically encoded labeling in fluorescence microscopy, as demonstrated by staining HEK293 cells.
A new approach to the synthesis of Anti-Reverse Cap Analog (ARCA) of the classical structure – dimethylated guanosine dinucleotide 2mGpppG is proposed. The classical approach to obtaining consists in condensation of activated 5′-diphosphate of 7,3′-O-dimethylguanosine with 5′-guanosine monophosphate. We suggest to use a commercially available 3′-O-methylguanosine for the synthesis of 5′-monophosphate of dimethylated guanosine only, and to use an activated 5′-guanosine diphosphate in the condensation. The conditions of 3′-O-methylguanosine phosphorylation were determined to avoid the formation of a side product 3′-O-methyl-5′-deoxy-5′-chloroguanosine-3′-phosphate. ARCA was synthesized with a high yield (89% at the condensation stage). Our approach to the synthesis is easily scaled and can be used for a preparative synthesis of ARCA (several grams).
We report a series of 3-aminocoumaranones possess significant chemiluminescence under various conditions. The introduce of the electron-donor groups in the coumaranone moiety and increasing of the conjugated π-system of coumaranones allow to shift 30–40 nm of the chemiluminescence maxima to the long-wavelength region. We showed that some 3-aminocoumaranones can be used for detecting of the urease and hydrogen peroxide.
