316-46-1Relevant articles and documents
ROOM-TEMPERATURE REACTIONS OF CsSO4F WITH ORGANIC MOLECULES CONTAINING HETEROATOMS
Stavber, Stojan,Zupan, Marko
, p. 487 (1983)
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Synthesis and properties of the monoesters of 5-fluorouridine with 4-carboxybutyric acid and their conjugates with chitosan
Onishi,Machida,Nagai
, p. 340 - 343 (1995)
The mixture of 2'-O-(4-carboxybutyryl)-5-fluorouridine (2'-glu-FUR) and 3'-O-(4-carboxybutyryl)-5-fluorouridine (3'-glu-FUR), named (glu-FUR(I)), and 5'-O-(4-carboxybutyryl)-5-fluorouridine (5'-glu-FUR), named glu-FUR(II), were easily obtained from the reaction of 5-fluorouridine (FUR) with glutaric anhydride. In addition, the chitosan-glu-FUR(I) conjugate and the chitosan-glu-FUR(II) conjugate were prepared. The obtained compounds were investigated regarding their in vitro characteristics. Equilibrium between 2'-glu-FUR and 3'-glu-FUR was suggested to be attained quickly in a 1/15 M phosphate buffer of pH 7.4. Glu-FUR(II) was found to be introduced into chitosan more easily than glu-FUR(I). For every compound, chemical hydrolysis was accelerated at weakly basic pH and a gradual regeneration of FUR was observed at physiological pH.
Thermodynamic Reaction Control of Nucleoside Phosphorolysis
Kaspar, Felix,Giessmann, Robert T.,Neubauer, Peter,Wagner, Anke,Gimpel, Matthias
supporting information, p. 867 - 876 (2020/01/24)
Nucleoside analogs represent a class of important drugs for cancer and antiviral treatments. Nucleoside phosphorylases (NPases) catalyze the phosphorolysis of nucleosides and are widely employed for the synthesis of pentose-1-phosphates and nucleoside analogs, which are difficult to access via conventional synthetic methods. However, for the vast majority of nucleosides, it has been observed that either no or incomplete conversion of the starting materials is achieved in NPase-catalyzed reactions. For some substrates, it has been shown that these reactions are reversible equilibrium reactions that adhere to the law of mass action. In this contribution, we broadly demonstrate that nucleoside phosphorolysis is a thermodynamically controlled endothermic reaction that proceeds to a reaction equilibrium dictated by the substrate-specific equilibrium constant of phosphorolysis, irrespective of the type or amount of NPase used, as shown by several examples. Furthermore, we explored the temperature-dependency of nucleoside phosphorolysis equilibrium states and provide the apparent transformed reaction enthalpy and apparent transformed reaction entropy for 24 nucleosides, confirming that these conversions are thermodynamically controlled endothermic reactions. This data allows calculation of the Gibbs free energy and, consequently, the equilibrium constant of phosphorolysis at any given reaction temperature. Overall, our investigations revealed that pyrimidine nucleosides are generally more susceptible to phosphorolysis than purine nucleosides. The data disclosed in this work allow the accurate prediction of phosphorolysis or transglycosylation yields for a range of pyrimidine and purine nucleosides and thus serve to empower further research in the field of nucleoside biocatalysis. (Figure presented.).
SYNTHESIS AND STRUCTURE OF HIGH POTENCY RNA THERAPEUTICS
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, (2019/01/15)
This invention provides expressible polynucleotides, which can express a target protein or polypeptide. Synthetic mRNA constructs for producing a protein or polypeptide can contain one or more 5′ UTRs, where a 5′ UTR may be expressed by a gene of a plant. In some embodiments, a 5′ UTR may be expressed by a gene of a member of Arabidopsis genus. The synthetic mRNA constructs can be used as pharmaceutical agents for expressing a target protein or polypeptide in vivo.
