54 results about "Inhibition enzyme" patented technology

Compounds of Formulas I-XLIII are identified as direct inhibitors of p97 ATPase or of the degradation of a p97-dependent ubiquitin-proteasome system (UPS) substrate. Methods and compositions are disclosed for inhibiting p97 ATPase and the degradation of a p97-dependent UPS substrate, and for identifying inhibitors thereof.

The invention relates to a competitive inhibition enzyme-linked immunosorbent assay (ELISA) method for grass carp tumor necrosis factors alpha. The method comprises the following steps of: 1, determining the concentration of coating antigens and the optimal dilution ratio of polyclonal antibodies; 2, establishing the competitive inhibition ELISA method, and coating an ELISA plate of grass carp tumor necrosis factor alpha protein to obtain antigens immobilized on the ELISA plate; mixing enzyme-labeled antibodies and an antigen mixed solution, and performing competitive binding on the solution and the antigens immobilized on the ELISA plate; washing the ELISA plate and developing the color of the substrate; and reading holes of the ELISA plate to obtain the light absorption value of each hole, calculating the inhibition rates of a standard antigen and a sample to be detected according to the read light absorption values respectively, and calculating the concentration of the sample to be detected according to the inhibition rates. The method has the advantages that a quick and efficient detection means is provided for detecting the protein expression level of the grass carp tumor necrosis factors alpha; and the method is stable, reliable and low in cost.

The invention relates to the related fields of immunology, pharmacy and medicine, discloses a method for preparing a hybridoma cell line and a monoclonal antibody based on B cell epitopes of dipeptidyl peptidase 4 (DPP-4) and an application thereof, and especially, relates to small molecular antigen peptides prepared by coupling the B epitopes of DPP-4 with intramolecular carrier peptides and quickly obtained by a synthetic method; the small molecular antigen peptides immunize mice to produce strong immune response, and can be used for preparing immune spleen lymphocytes and preparing hybrid tumor cells, antibodies and the like. The monoclonal antibody is secreted by the hybridoma cell line (having the preservation number of CCTCC No:C2017227), is a Th2 antibody, is IgG1 in the mice, inhibits the enzyme activity of DPP-4, is specifically combined with DPP-4, can develop a DPP-4 detection reagent and a DPP-4 inhibitor, can significantly reduce blood sugar, uric acid and four indexes ofcreatinine blood lipid, increases GLP-1, regulates oxidative stress and immune balance from Th1 trending to Th2, and reduces pancreatic inflammation; prepared drugs are used for preventing and treating diabetes and complications thereof, hyperuricemia, gout, kidney and liver diseases, hyperlipidemia, AS, cardiovascular diseases and Th1-related diseases.

This disclosure relates to antibodies that bind an epitope present on CD73 expressed at the surface of cells, including tumor cells, and that inhibit the enzymatic (ecto-5′ nucleotidase) activity of the CD73 enzyme. Such agents can be used for the treatment of diseases such as cancers.

The invention relates to a competitive inhibition enzyme-linked immunosorbent assay (ELISA) method for grass carp tumor necrosis factors alpha. The method comprises the following steps of: 1, determining the concentration of coating antigens and the optimal dilution ratio of polyclonal antibodies; 2, establishing the competitive inhibition ELISA method, and coating an ELISA plate of grass carp tumor necrosis factor alpha protein to obtain antigens immobilized on the ELISA plate; mixing enzyme-labeled antibodies and an antigen mixed solution, and performing competitive binding on the solution and the antigens immobilized on the ELISA plate; washing the ELISA plate and developing the color of the substrate; and reading holes of the ELISA plate to obtain the light absorption value of each hole, calculating the inhibition rates of a standard antigen and a sample to be detected according to the read light absorption values respectively, and calculating the concentration of the sample to be detected according to the inhibition rates. The method has the advantages that a quick and efficient detection means is provided for detecting the protein expression level of the grass carp tumor necrosis factors alpha; and the method is stable, reliable and low in cost.

Anti-Schistosoma japonicum thioredoxin glutathione reductase Sj ? The invention relates to a TGR single-region antibody and a preparation method thereof, which belong to the technical fields of molecular biology, immunology and pharmacy of biotechnology. The present invention provides an anti- Sj ? Recombinant phage display library of single-region antibody of TGR protein, anti- Sj ? Single region antibody of TGR protein and preparation method thereof, described anti Sj ? TGR single domain antibody can be combined with Sj ? TGR protein specifically binds, and / or has inhibitory Sj The TGR enzyme activity can be used to prepare new drugs for treating schistosomiasis or targeted carriers of therapeutic drugs. The invention lays a good foundation for the development of new schistosomiasis therapeutic drugs and new treatment methods, and has important significance for controlling the prevalence of schistosomiasis.

The invention provides a method for designing a DPP-IV (dipeptidyl peptidase-IV) inhibitory peptide by a computer-aided drug, the DPP-IV inhibitory peptide and application of the DPP-IV inhibitory peptide. The method comprises the steps of establishing a database and dividing the database into an internal training set and an external test set; constructing the structure of the polypeptide in the database; carrying out molecular docking on the polypeptide and DPP-IV to select a conformation with the highest score; carrying out superposition by taking the tripeptide IPI as a template molecule and taking a peptide bond as a public skeleton; manually adjusting the bond angle of each peptide to improve the model fitting degree, wherein the training set is an established target model, and the test set is used for testing the prediction capability of the model; calculating the pIC50 of the peptide in the test set by using the training set, and comparing the calculated pIC50 of the peptide with the pIC50 obtained by the experiment; then exporting an equipotential diagram of the training set to guide the design of the DPP-IV inhibitory peptide; and finally obtaining the novel DPP-IV inhibitory peptide. The novel peptide designed and obtained by the invention has very high activity of inhibiting DPP-IV enzyme.

The present invention encompasses assays to identify compounds that inhibit the enzymatic activity of MIF which catalyzes the tautomerization of MIF-substrates, such as D-dopachrome to DHICA. In general, the assay is conducted in vitro by adding, mixing or combining MIF and a suitable substrate in the presence or absence of a test compound, and measuring the tautomerization of the substrate. The test compounds that inhibit tautomerization in the assay are identified as MIF inhibitors.

The invention relates to a competitive inhibition enzyme-linked immunoassay (ELISA) method of grass carp interleukin 10 (IL-10). The method comprises the following steps of: immunizing a New Zealand white rabbit by utilizing grass carp interleukin 10 proteins which is expressed in a recombined way as an immunogen to obtain a polyclonal antibody; marking the antibody by utilizing horseradish peroxidase; and finally, establishing the competitive inhibition ELISA method by taking the recombined grass carp interleukin IL-10 protein as a covered antigen, wherein the competitive inhibition ELISA method can be used for the protection detection of the grass carp interleukin 10. The detection range of the ELISA method is 0.1-100 ng / mL. By utilizing the polyclonal antibody and the competitive inhibition ELISA method, the cost is low, and the stability and the repeatability are good. The conventional method is that the competitive inhibition ELISA method is firstly established to detect protection expression of the grass carp interleukin 10.

The invention provides a compound WXSA-082B based on inhibiting histone demethylase, further provides a preparation method thereof. Tests shown that the compound can enable H3K4me3 protein level in human gastric carcinoma cell BGC-823 to increase obviously, has obvious RBP2 enzyme activity inhibiting effect, and can reduce the transfer ability of the human gastric carcinoma cell BGC-823. The compound provided by the invention can be applied to preparation of anti-gastric carcinoma drugs serving as a gastric carcinoma inhibitor. The structure of the compound is as follows: (the structure is shown in the description).

A C6 compound as histone methyltransferase NSD3 activity inhibitor and its pharmaceutical use are disclosed. C6 has a chemical structure represented by formula I. Chemical name is 6-Amino-9-(2-(naphthalen-1-Yloxy) ethyl)-9H-Purine-8-Thiol; At least one of that compound C6 or its hydrate, pharmaceutically acceptable salt, tautomers, stereoisomer. And precursor compounds is used as an active ingredient for preparing an antineoplastic drug. The pharmaceutical use of the compound C6 or its hydrate, the pharmaceutically acceptable salt, the tautomers, the stereoisomers. And the precursor compoundsare described. Experiments show that the compound C6 of the invention can effectively inhibit the NSD3 enzyme activity. And the IC50 value of the enzyme level is 17.97 +-2. 75[mu]mol / L. And significantly inhibited the proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650. The compound of the invention has the effect of inhibiting tumor cell proliferation. And is expected tobe used as an active ingredient for preparing an anti-tumor drug. And has pharmaceutical prospect.