41 results about "Deoxyuridine" patented technology

The invention discloses a synthesis method of 2 '-fluoro-2'-deoxyguanosine. According to the method, thymine nucleoside phosphorylase and purine nucleoside phosphorylase are used as biocatalysts, and 2 '-fluoro-2'-deoxyuridine and guanine are used as substrates to synthesize the 2 '-fluoro-2'-deoxyguanosine. Compared with a chemical method, the production cost is greatly reduced; meanwhile, the synthesis method can effectively solve the problem that the product is difficult to separate.

The invention relates to a novel method for preparing 5-fluoro-2 '-deoxyuridine-5'-O-[1-naphthyl (benzyloxy-L-alanine)] phosphate (NUC-3373) and a derivative of the NUC-3373. The NUC-3373 produced according to the method is more stable than NUC-3373 produced according to other methods. # imgabs0 #

The invention discloses a reagent and a method for improving the tolerance of a PCR inhibitor and application, and belongs to the technical field of molecular biology. According to the invention, the thermosensitive uracil DNA glycosidase and the deoxyuridine triphosphate are combined and used as the PCR antiinhibitor to be applied to DNA amplification of a whole blood sample, and experiments prove that the composition can improve the endurance capacity of a PCR reaction system to a whole blood inhibitor, reduce the false negative rate and improve the accuracy and reliability of detection. Meanwhile, the method for carrying out PCR reaction by using the composition is simple to operate, low in cost and high in nucleic acid detection sensitivity. Therefore, the reagent and the method have a good application prospect in detection of nucleic acid extracted from a whole blood sample.

The invention discloses pyridine DPP fluorophore extension type deoxyuridine as well as a preparation method and application thereof, and belongs to the field of biological medicine and detection. The invention provides a uridine analogue modified by a fluorescent chromophore DPP derivative with a structure shown in the specification, and pyridine DPP fluorophore extension type deoxyuridine has excellent fluorescent property, can be used as a fluorescent probe, and is widely applied to the fields of biochemistry, medicine and the like.

The invention relates to methods and pharmaceutical compositions for use of a deoxyuridine 5'-triphosphate nucleotidohydrolase (DUT) inhibitor for the treatment of resistant HRD cancer, particularly resistant BRCA-associated cancer.

To provide a method for producing 5-fluoro-2' - deoxyuridine-5' -O - [1-naphthyl (benzyloxy-L-alaninyl)] phosphate (NUC-3373) and a method for producing 3' - deoxyadenosine-5' -O - [phenyl (benzyloxy-L-alaninyl)] phosphate (NUC-7738).SOLUTION: A compound of Formula (IIa) or (IIb) is reacted with a compound of Formula (IIIa) or (IIIb), respectively, in presence of a base (B1) and the protecting groups are removed from the resulting compound of Formula (IVa) or (IVb) to provide NUC-3373 or NUC-7738.SELECTED DRAWING: None

The invention discloses a method for rapidly detecting MTHFR (Methylene Tetrahydrofolate Reductase) gene polymorphism based on a complementary probe technology, which comprises the following steps: S1, acquiring a sample: extracting genome DNA (Deoxyribose Nucleic Acid) from a sample to be detected as an amplification template; s2, preparing a reaction system: adding the genome DNA, the upstream primer, the downstream primer, the C probe, the T probe, uracil-N-glycosylase, DNA polymerase, deoxyribonucleoside triphosphate and deoxyuridine triphosphate of the sample to be detected into the reaction system; s3, carrying out PCR (Polymerase Chain Reaction) amplification reaction under the conditions that the temperature is 90-98 DEG C, and the time is 5-20 minutes; performing denaturation at the temperature of 90-98 DEG C for 10-50 seconds; the temperature is 55-69 DEG C, and annealing is conducted for 60-120 s; the temperature is 68-72 DEG C, and extension is carried out for 15-300 s; carrying out 35 to 40 cycles; and S, genotype judgment. A test result is the same as a first-generation sequencing test result, which shows that the detection method of the scheme has relatively high accuracy. Meanwhile, compared with a sequencing method, the method has the advantages that a series of complex follow-up treatment does not need to be carried out on a PCR product, PCR amplification and detection are synchronously carried out, the detection time is greatly shortened, and the detection cost is reduced.

The present invention belongs to the field of organic synthesis and specifically relates to a method for synthesizing 2'-fluoro-2'-deoxyuridine and its intermediates. The method comprises the following steps: The method prepares 2'-fluoro-2'-deoxyuridine by constructing novel intermediates, namely, compounds of formula IV, III, and II. This method avoids the use of reagents such as dihydropyran, which are strong eye and skin irritants. The method results in milder reaction conditions, lower costs, simple operation, environmental friendliness, high yield, and suitability for industrial production.

The present invention belongs to the technical field of preparing functional materials for molecular recognition, adsorption and separation, and discloses a method for preparing a hydrophilic dual-receptor MOFs nanosheet surface imprinted adsorbent and its application in the selective separation of adenosine monophosphate. The present invention targets the structural characteristics of a typical nucleoside compound adenosine monophosphate (AMP) molecule, designs and synthesizes Zr-MOFs nanosheets coordinated with its specific metal ion as a matrix material, and uses 5-(2-methoxyvinyl)-2′-deoxyuridine (AcrU) as a functional monomer that undergoes specific base complementary pairing. The arrangement and orientation of the template molecules are precisely fixed through an ordered assembly strategy. Finally, the large number of double bonds modified on the surface of the Zr-MOFs nanosheets and a hydrophilic cross-linking agent are utilized to photoinitiate the construction of a stable hydrophilic dual-receptor MOFs nanosheet surface imprinted adsorbent (D-MIPs), thereby enhancing the recognition and separation effect of nucleoside compounds and achieving the selective separation and enrichment of nucleoside compounds such as AMP in biological samples such as urine and blood.

Polymer compounds useful for preparing antibody-drug conjugates are disclosed. The polymers contain a side chain-carrying deoxyuridine group. Methods associated with preparation and use of such compounds are also provided.

The embodiment of the invention provides a connecting unit for chemical modification of a nucleic acid terminal group, a solid-phase carrier and a preparation method of the solid-phase carrier, the chemical modification comprises N-acetylgalactosamine, and the method comprises the following steps: mixing L-deoxyuridine with iodine, and carrying out iodine substitution reaction to obtain 8-iodine-L-deoxyuridine; carrying out triphenyl methylation on the 8-iodine-L-deoxyuridine to protect 5 '-terminal hydroxyl, carrying out palladium catalytic coupling reaction to obtain 8-alkenyl-L-deoxyuridine ester compounds, and hydrolyzing to obtain unsaturated carboxyl modified L-deoxyuridine derivatives; the unsaturated carboxyl modified L-deoxyuridine derivative and N-acetylgalactosamine are subjected to condensation, and the connecting unit for nucleic acid end group chemical modification is obtained. The connection unit obtained by the method has better enzymolysis resistance, and the synthesis method is simple and efficient.

The invention discloses a drug delivery nano system based on ROS response as well as a preparation method and application of the drug delivery nano system. The drug delivery nano system comprises nanoparticles and a camptothecin-5-fluorodeoxyuridine prodrug, wherein the nanoparticles are formed by self-assembly of an amphiphilic high-molecular polymer HA-IR-780 with a photosensitive characteristic, and the camptothecin-5-fluorodeoxyuridine prodrug is wrapped in the nanoparticles; and the surface of the drug delivery nano system is modified with a lipid-polyethylene glycol material. When the drug delivery nano-system is applied to preparation of breast cancer drugs, the drug delivery nano-system can be enriched at a tumor site depending on the passive targeting effect of the EPR effect of the drug delivery nano-system, breast cancer chemotherapy / PDT / PTT / combined treatment can be achieved, and the effects of reducing toxicity and enhancing efficacy are achieved to a certain extent.

The application discloses a monomerized pyrimidine nucleoside phosphorylase mutant and a construction method and application thereof, and belongs to the field of enzyme engineering and biological catalysis technology.The mutant is obtained by amino acid substitution mutation of wild-type pyrimidine nucleoside phosphorylase shown in SEQ ID NO:1, and the amino acid sequence is shown in SEQ ID NO:2.The mutant is transformed into a stable monomer form by dimer interface remodeling and hinge region stabilization of the closed active conformation, the natural dimer PyNP is transformed into a stable monomer form, and the catalytic activity of the mutant to uridine, 2'-deoxyuridine and similar substrates is maintained in the monomer state.Compared with the wild-type enzyme, the mutant has lower oligomer dependence, better temperature stability, pH stability and storage stability, and can be used for biological catalytic synthesis of nucleosides and nucleoside analogs.

This invention relates to a novel process for the preparation of 5-fluoro-2′-deoxyuridine-5′—O-[1-naphthyl (benzoxy-L-alaninyl)] phosphate (NUC-3373) and derivatives thereof. The NUC-3373 made according to this process is more stable than NUC-3373 made according to alternative processes.

The invention relates to a hydantoin-containing deoxyuridine triphosphatase inhibitor and a preparation method thereof. Provided herein are dUTPase inhibitors, compositions comprising these compounds, and methods of using these compounds or compositions.

Described herein are synthetic methods for producing sequence-specific RNA oligonucleotides that eliminate impurities produced in prior art methods. In one aspect, a first amplification primer includes one or more deoxyuridine residues, wherein at least one of the one or more deoxyuridine residues is at position −1, −2, −3, −4 or −5 of the promoter region for the single-subunit, DNA-dependent RNA polymerase. The deoxyuridines are excised to provide an amplified functional template DNA which is then used to synthesize RNA which has reduced immunogenic double stranded RNA compared to controls.

The present disclosure provides pyrimidine nucleoside compounds, including torcitabine, thymidine, deoxyuridine, deoxycytidine and uridine, and methods to treat telomere biology disorders (TBDs) and aging-related diseases, including hematological disorder, liver disease, or hepatic fibrosis, comprising administering to a subject diagnosed with said telomere biology disorder a therapeutically effective amount of said compounds.

The invention discloses a fluorodeoxyuridine monophosphate prodrug as shown in a formula I, application of the prodrug in preparation of a medicine for treating liver cancer, a pharmaceutical composition containing the prodrug and pharmaceutically acceptable auxiliary materials or taraxasterol and application of the prodrug in preparation of the medicine for treating liver cancer, and belongs to the field of pharmacy. The compound is modified by specific natural amino acid residues and can be used for preparing medicines for treating liver cancer. The in-vitro and in-vivo anti-tumor activity of the compound is remarkably superior to that of the prior art, the compound has a synergistic effect when being combined with taraxasterol, the highest tumor inhibition rate reaches 91.72%, the compound is high in selectivity, good in safety and high in liver targeting performance, and a more effective new scheme is provided for liver cancer treatment.

The invention discloses a heterologous transport protein YdhP and application thereof in production of beta-thymidine from escherichia coli, and belongs to the technical field of microbial engineering. According to the present invention, by introducing the heterologous transport protein ydhP derived from Ralstania mannitolyticus, the extracellular secretion of beta-thymidine can be effectively promoted, and the intracellular feedback regulation limitation can be reduced; during shake flask fermentation, the yield of beta-thymidine is increased to 1.6 g / L (increased by about 45%), and the by-product deoxyuridine is reduced by about 50%; the yield in a 5 L fermentation tank reaches 20 g / L, which is obviously improved compared with that of a control strain (12 g / L), and an efficient and stable engineering strain and a fermentation process are provided for industrial production of beta-thymidine.

The present invention relates generally to the fields of cancer cell biology, cancer therapeutics for cancers located within in the central nervous system, thymidine analogs and cellular nucleotide excision repair mechanisms. More specifically, the invention relates to the use of EdU in methods of treating cancers located within in the central nervous system, and methods of inhibiting and / or reducing growth of a cancer or cancer cell.

Provided are a high-affinity nanoantibody targeting African swine fever virus deoxyuridine triphosphatase, and a preparation method therefor and a use thereof. The nanoantibody targeting African swine fever virus deoxyuridine triphosphatase has three complementarity determining regions CDR1, CDR2 and CDR3, wherein the amino acid sequence of CDR1 is positions 26-38 of SEQ ID No. 2, the amino acid sequence of CDR2 is positions 55-64 of SEQ ID No. 2, and the amino acid sequence of CDR3 is positions 100-113 of SEQ ID No. 2. Upon verification by ELISA, the nanoantibody can specifically bind to African swine fever virus deoxyuridine triphosphatase (dUTPase), and has relatively high affinity.

The invention discloses a bithiophene DPP derivative modified deoxyuridine as well as a synthesis method and application thereof, and belongs to the field of biological medicine and detection. The invention provides a bithiophene DPP derivative modified deoxyuridine shown in the following structure, and the compound has excellent fluorescent property, can be used as a fluorescent probe, and is widely applied in the fields of biochemistry, medicine and the like. The target product is directly generated, and other reactions such as glycosylation and hydrolysis are avoided. The method has the characteristics of relatively simple and controllable reaction conditions, no generation of by-products, high yield and the like.

The application discloses a reagent, a method and application for improving PCR inhibitor tolerance, and belongs to the technical field of molecular biology. The application combines heat-sensitive uracil DNA glycosylase and deoxyuridine triphosphate, and applies the combination as a PCR anti-inhibitor in DNA amplification of a whole blood sample. Experiments prove that the combination can improve the tolerance of a PCR reaction system to whole blood inhibitors, reduce the false negative rate, and improve the accuracy and reliability of detection. Meanwhile, the method for performing PCR reaction by using the combination is simple in operation, low in cost, and high in nucleic acid detection sensitivity. Therefore, the reagent and the method have good application prospects in the detection of nucleic acids extracted from a whole blood sample.

The invention relates to a cross-lesion synthesis driving Cas12a activity grading regulation method based on a template-activator bifunctional unit and application of the cross-lesion synthesis driving Cas12a activity grading regulation method. The invention firstly discloses a template-activator bifunctional unit which comprises (i) a T7 promoter and a complementary sequence thereof; (ii) a CRISPR array sequence; (iii) at least one DNA damage site, said site being selected from a deoxyuridine base or a purine / pyrimidine-free site. According to the construction method, the TAC unit is constructed, so that the template chain has the functions of a crRNA transcription template and an activator, exogenous activator addition and complex crRNA modification steps are avoided, experimental components are reduced, and the operation is simple and convenient; a DNA lesion mechanism is introduced, the cross-lesion synthesis characteristic of T7 RNAP for different lesion sites is fully utilized, fine hierarchical regulation and control of Cas12a activity are achieved through the synergistic effect on the template level and the template-activator level, and the regulation and control accuracy and flexibility are remarkably improved.

The invention relates to a method of producing cladribine with a purity greater than 99.9 wt.% from 2-deoxyuridine and 2-chloroadenine by using the catalytic action of high concentrations (at least 20.000 U / L) of freely dissolved transglycosidases UP (uridine phosphorylase) and PNP (purine nucleoside phosphorylase) in an enzymatic synthesis in an aqueous environment without the presence of any organic solvent.

This invention relates to pharmaceutical formulations and formulation strategies of protides (phosphoramidate derivatives of nucleosides) and, in particular, protides useful in the treatment of cancer such as NUC-3373 (5-fluoro-2′-deoxyuridine-5′-O-[1-naphthyl (benzoxy-L-alaninyl)] phosphate) and NUC-7738 (3′-deoxyadenosine-5′-O-[phenyl (benzyloxy-L-alaninyl)] phosphate). In particular, the invention relates to formulations which comprise a polar aprotic solvent, for example dimethyl acetamide (DMA).

The invention relates to the technical field of biology, in particular to a preparation and purification method of 2 '-fluoro-2'-deoxyguanosine. The invention discloses a preparation and purification method of 2 '-fluoro-2'-deoxyguanosine.The preparation method comprises the following steps that 2, 6-diaminopurine and 2 '-fluoro-2'-deoxyuridine generate 2 '-fluoro-2, 6-diaminopine-2'-deoxynucleoside under the catalysis of thymine nucleoside phosphorylase and purine nucleoside phosphorylase, filtering is conducted, and the 2 '-fluoro-2, 6-diaminopine-2'-deoxyguanosine is obtained. Then adenosine deaminase is added for catalysis, and 2 '-fluoro-2'-deoxyguanosine is generated; biosynthesis of the 2 '-fluoro-2'-deoxyguanosine is divided into two stages, the intermediate 2 '-fluoro-2, 6-diaminopine-2'-deoxynucleoside is synthesized firstly, and then deamination is performed to form the 2 '-fluoro-2'-deoxyguanosine, so that the problem that the conversion rate is extremely low when guanine with low solubility is taken as a substrate is solved.

According to the invention, an amplification-free, high-sensitivity and high-specificity monomolecular biosensing platform is constructed. According to the single-molecule biosensing platform, the clickchemistry-based multi-fluorophore nucleic acid probe is designed and synthesized by taking DNA (Deoxyribose Nucleic Acid) of orientia tsutsugamushi as a model target. 5-ethynyl-2 '-deoxyuridine triphosphate is introduced into the probe through a polymerase chain reaction, so that the probe carries a plurality of alkynyl modification sites and is further connected with a large number of Cy5 fluorophores, signals are greatly enhanced, and the photobleaching problem is effectively relieved. Meanwhile, random optical reconstruction microscopy is introduced to serve as a detection reading mode, the random flicker characteristic of fluorescent molecules is utilized, tens of thousands of single molecule events are positioned and counted, and signals are further amplified. The application successfully develops a simple, rapid, high-sensitivity and high-specificity single-molecule detection platform, provides an effective tool for the detection of low-abundance biomarkers, and has wide application prospects in the fields of early diagnosis of diseases and the like.

The invention discloses a lactobacillus fermentation lysate as well as a preparation method and application thereof, and the lactobacillus fermentation lysate mainly comprises the following components accounting for the relative content of the lactobacillus fermentation lysate: 53-62% of carbohydrate and carbohydrate conjugate; 2-11% of nucleoside, nucleotide and derivatives thereof; 5-10% of amino acid, polypeptide and analogues thereof; 20-22% of organic acid and derivatives thereof; wherein the nucleoside, the nucleotide and the derivatives of the nucleoside and the nucleotide comprise one or more of NAD (Nicotinamide Adenine Dinucleotide), guanosine diphosphate, 2 '-deoxyuridine-5'-triphosphate, acetyl coenzyme A, cytidine monophosphate, deoxyguanosine, guanosine and adenosine. The lactobacillus fermentation lysate has the effects of maintaining skin health and repairing aged cells, and also has the potential of whitening skin cells. In addition, the lactobacillus fermentation lysate also has the effects of promoting microcirculation, enhancing mitochondria, enhancing immunity and regulating rhythm.

The application relates to the technical field of deoxyuridine intermediate synthesis, and specifically discloses a new type of 2'-methoxy uridine compound containing 4'-methyl or 4'-alkynyl and a synthesis method thereof. The synthesis method of the new type of 2'-methoxy uridine compound containing 4'-methyl or 4'-alkynyl comprises the following steps: taking 2'-methoxy uridine as raw material to synthesize an intermediate 9 containing two TBSO groups; the intermediate 9 is subjected to an oxidation reaction, a Seyferth-Gilbert carbon increase reaction and TBSO group deprotection to obtain an intermediate 12; the intermediate 9 is reacted with thiophosgene phenyl ester, then methyl intermediate 14 is generated under the condition of TMSS and AIBN, and then the TBSO group deprotection is carried out to obtain an intermediate 15; the new type of 2'-methoxy uridine compound containing 4'-methyl or 4'-alkynyl provided by the application can be used for the synthesis of a drug intermediate and the research on biological activity, and has the advantages of high product stability.