32 results about "Inhibition enzyme" patented technology

Provided are: a compound defined by chemical formula 1; a stereoisomer thereof; a tautomer thereof; and pharmaceutically acceptable salts of the compound, the stereoisomer, and the tautomer. The compound according to the present invention can inhibit the activity of the USP1 enzyme. In chemical formula 1, R1 to R4 and [the symbol A in chemical formula 1] are as defined in the present specification.

The application belongs to the field of medicine, and particularly relates to application of CZC-54252 in preparation of a drug for treating esophageal squamous cell carcinoma. The results of the application show that CZC-54252 can efficiently inhibit expression of RSK4 enzyme, and can efficiently inhibit proliferation, invasion and migration of esophageal squamous cell carcinoma cells. In combination with Afatinib, the proliferation of an esophageal squamous cell carcinoma erlotinib-resistant strain can be significantly inhibited, and the results provide an effective technical means for treatment and prognosis of esophageal squamous cell carcinoma patients.

The invention discloses an S3B polypeptide taking SHP2 as an action target and application of the S3B polypeptide in treatment of tumors and inflammations. The amino acid sequence of the polypeptide is RLLREEEYVAPPRGPLPTLQVVPL, the amino acid sequence of a cell-penetrating peptide contained in the polypeptide is TAT: YGRKKRRQRRR, the polypeptide can enter cells after being wrapped by lipidosome, the effects of inhibiting proliferation, migration, growth and the like of tumor cells are achieved by inhibiting QPCTL enzyme activity and promoting SHP2 protein degradation, and then the purpose of treating diseases such as tumors is achieved. The invention provides a certain reference for treating SHP2 related tumors or immune inflammatory diseases and developing a novel SHP2 degradation drug.

The invention provides a casein source blood sugar reducing peptide and application thereof. According to the invention, through research and analysis on protein hydrolysate, two polypeptides with DPP-IV inhibitory activity are found, and the amino acid sequences of the polypeptides are respectively APFPEV and FPEVF. After high-purity polypeptide is obtained through a chemical synthesis method, a liquid chromatograph-mass spectrometer is used for characterization, the effect of the polypeptide is verified through a DPP-IV inhibition experiment, experimental results find that the two polypeptides can effectively inhibit DPP-IV enzyme and are high in inhibition activity, the IC50 value of the polypeptide APFPEV is 224.67 mu M, the IC50 value of the polypeptide FPEVF is 328.86 mu M, and it is proved that the polypeptide has a better inhibition effect compared with similar polypeptides.

The invention relates to the technical field of activity detection, and particularly discloses a colloidal gold method for rapidly detecting ACE inhibitory activity and a test paper preparation method. The test paper comprises a sample pad, a gold-labeled pad, a nitrocellulose membrane and a water absorption pad, angiotensin converting enzyme labeled by colloidal gold is loaded on the gold-labeled pad, and a detection line coated with an angiotensin II antibody and a quality control line coated with an anti-ACE antibody are arranged on the nitrocellulose membrane. During detection, an ACE inhibitor in a sample can inhibit enzyme activity and influence aggregation of colloidal gold on the detection line, so that rapid judgment is realized through color comparison of the detection line and the quality control line. The invention also provides a preparation method and a detection method of the test paper, and the test paper has the advantages of simplicity and rapidness in operation, no need of large instruments, low cost, suitability for field detection and the like, and can be widely applied to drug screening, food detection and clinical sample preliminary screening.

The application discloses a kind of S3B polypeptide with SHP2 as action target point and its application in treating tumor and inflammation.The amino acid sequence of the polypeptide is RLLREEEYVAPPRGPLPTLQVVPL, the amino acid sequence of transmembrane peptide included in the polypeptide is TAT:YGRKKRRQRRR, the polypeptide can enter cell after being wrapped by liposome, inhibits QPCTL enzyme activity, promotes the degradation of SHP2 protein, thereby playing the role of inhibiting tumor cell proliferation, migration and growth, etc., to achieve the purpose of treating tumor and other diseases.The application provides a certain reference for treating SHP2 related tumor or immune inflammatory disease and developing new SHP2 degradation drug.

The invention provides an application of a UGCG enzyme inhibitor in preparation of a medicine for treating sepsis, and particularly relates to an application of a UGCG enzyme activity inhibitor Eliglulukast as a medicine for treating sepsis. The UGCG enzyme is remarkably increased in sepsis patients, and organ injury and systemic inflammatory response related to sepsis are effectively relieved by inhibiting the expression quantity or activity of the UGCG enzyme, influencing MIF release and inhibiting PI3K / AKT / mTOR signal channel activation, so that the survival rate of the sepsis patients is remarkably increased.

The application discloses application of a preparation for inhibiting IL4I1 expression in preparation of a medicine for treating renal fibrosis, and belongs to the technical field of biological medicine.The application finds through in-vivo and in-vitro experiments that IL4I1 is closely related to kidney injury and renal fibrosis, and is a potential target for treating kidney injury and renal fibrosis.IL4I1 inhibitors are substances capable of inhibiting IL4I1 enzyme activity, and the in-vivo and in-vitro experimental results show that, for example, extract of plantago, salted plantago extract, verbascoside, isoverbascoside and akebone phenylethanoid glycoside B are all beneficial to relieving renal fibrosis.The application provides theoretical support for developing a medicine for treating renal function impairment and treating and / or relieving renal fibrosis disease by inhibiting IL4I1.

The invention discloses a sophora moorcroftiana protein source antihypertensive peptide and application of the sophora moorcroftiana protein source antihypertensive peptide. The sophora moorcroftiana protein source antihypertensive peptide comprises at least one of active peptides with the sequence structure of MGLPWYR, WHRPLR, INPLGFR, LPNSLFLFR and LFLWPIYR. A polypeptide sequence library is constructed through proteolysis of sophora moorcroftiana, bioinformatics analysis is combined, multiple polypeptides with ACE inhibitory activity are found, after high-purity polypeptides are obtained through a chemical method, a liquid chromatograph-mass spectrometer is used for characterization, the effect of the polypeptides is verified through ACE inhibition experiments, all the polypeptides can inhibit ACE, and the inhibitory activity of the polypeptides MGLPWYR and WHRPLR is about 90%.

The invention provides application of pyrrolimidazole in development of a CrtN enzyme inhibitor, and a CrtN enzyme activity test, a growth curve, pigment yield determination, a hydrogen peroxide killing test, a whole blood killing test and a mouse skin scald infection test prove that pyrrolimidazole can inhibit the activity of the CrtN enzyme, reduce the anti-oxidation removal capability of staphylococcus aureus and inhibit the growth of the CrtN enzyme. The protection effect of a staphylococcus aureus skin infection model is improved. Therefore, as a potential staphylococcus aureus pigment synthesis inhibitor, the depyrrolimidazole can reduce the oxidative stress resistance of staphylococcus aureus by inhibiting the activity of the CrtN enzyme, and has important significance for clinically developing safe and effective antioxidant adjuvants.

The invention provides a medical application of daphnetin in preparation of a PPK1 inhibitor. A growth curve test, a PPK1 enzyme activity inhibition test, a bacterial polyphosphate content determination test, a bacterial biofilm inhibition test and a hydrogen peroxide stimulation and thermal stimulation test show that the daphnetin can reduce the resistance mechanism of the acinetobacter baumannii to external stress factors by inhibiting the PPK1 enzyme activity. The invention provides a new way and a potential lead compound for preventing and controlling acinetobacter baumannii infection.

The present invention relates to the field of monoclonal antibodies. Specifically, the present invention relates to a monoclonal antibody against von Willebrand factor-cleaving protease (ADAMTS13), a preparation method thereof, and an application thereof. The ADAMTS13 monoclonal antibody provided by the present invention has high sensitivity and strong affinity, and can effectively inhibit the enzyme activity of ADAMTS13. In addition, the present invention also develops an in vitro diagnostic detection kit using this antibody. The kit has the advantages of a wide detection range, few interfering substances, a short detection time, good stability and repeatability, providing new ideas for the treatment and research of diseases.

This invention belongs to the field of liver disease research and biomedicine, specifically relating to the application of reagents targeting and inhibiting OXCT1 in combination with BHB or pharmaceutically acceptable salts thereof in the preparation of anti-HCC drugs. The reagents inhibiting OXCT1 include: siRNA, shRNA, antisense nucleic acid, and gene editing reagents that reduce OXCT1 expression; and small molecule inhibitors, peptides, antibodies, or fusion proteins that inhibit OXCT1 enzyme activity. This invention proposes a novel therapeutic strategy of targeting and inhibiting OXCT1 in combination with BHB. Studies have shown that targeting and inhibiting OXCT1 can block the pro-cancer metabolic pathway of BHB, reducing the effective concentration of BHB for its anti-cancer effect, enabling it to achieve significant anti-cancer effects at clinically tolerable concentrations and exert a synergistic anti-tumor effect. This invention solves the problem of limited clinical application of high-concentration BHB and provides a new combination therapy regimen with clinical translational potential for hepatocellular carcinoma.

The application discloses small-molecule compounds for targeted inhibition of proline hydroxylase activity, including Aristolone, Isosakuranin, Butein and Brevilin A. The small-molecule compounds screened by the application can be combined with the active site of PHD, and molecular biology experiments prove that the small-molecule compounds can inhibit the enzyme activity of PHD, activate the HIF-1 signal pathway, and cause the expression of a target gene Glut-1 to increase. The small-molecule compounds lay a foundation for future research and development of related drugs by inhibiting the enzyme activity of PHD.

The application discloses an anti-HpFucT protein monoclonal antibody and products and applications thereof, and belongs to the biomedical technical field.The HCDR1, HCDR2 and HCDR3 of the antibody heavy chain variable region are respectively shown as SEQ ID No.1-3 or a homologous sequence thereof, the LCDR1, LCDR2 and LCDR3 of the light chain variable region are respectively shown as SEQ ID No.6-8 or a homologous sequence thereof, or are respectively shown as SEQ ID No.9, 7, 10 or a homologous sequence thereof, or are respectively shown as SEQ ID No.6, 7, 11 or a homologous sequence thereof.The antibody can specifically recognize a target antigen HpFucT protein, has high affinity, and can effectively inhibit the enzyme activity of the HpFucT protein.The antibody can be used for preparing a composition for detecting or diagnosing a disease related to the HpFucT protein, a product for purifying the HpFucT protein, a product for detecting the HpFucT protein level, a cell labeling product, a product for inhibiting the HpFucT enzyme activity, and a product for treating a disease related to the HpFucT protein.

The invention relates to application of cacumen biotae alcohol for reversing drug resistance of polymyxin. The application is realized through the function of the platycladol for inhibiting the MCR-1 enzyme, specifically, the combination of the platycladol and the polymyxin B can recover the bactericidal effect of the polymyxin B on the MCR-1 positive enterobacter, and the bactericidal effect is a synergistic effect. According to the combined medication scheme, host cells can be protected in a cell infection model, the death rate can be remarkably reduced in a mouse peritonitis infection model, and no obvious toxicity is observed in the treatment dosage of platycladi alcohol. The invention provides a therapeutic scheme for solving the problem of drug resistance of clinical polymyxin B mediated by MCR-1.

The present invention provides a casein-derived hypoglycemic peptide and its application. The present invention studied and analyzed protein hydrolysates and discovered two polypeptides with DPP-IV inhibitory activity, whose amino acid sequences were APFPEV and FPEVF, respectively. After obtaining high-purity polypeptides by chemical synthesis, they were characterized by liquid chromatography-mass spectrometry and their effects were verified by DPP-IV inhibition experiments. The experimental results showed that both polypeptides could effectively inhibit the DPP-IV enzyme and had strong inhibitory activity. The IC value of the polypeptide APFPEV was 0.04. 50 The value is 224.67 μM, and the IC 50 The value was 328.86 μM, which proved that it had a better inhibitory effect than similar peptides.

Compounds and compositions for inhibition of the Cbl-b enzyme and methods of use thereof in modulating the immune system, treatment of diseases. Some compounds in this disclosure are covalent Cbl-b inhibitors, which can form a covalent bond with a cysteine in the Cbl-b protein. Also disclosed herein are methods for use of a Cbl-b inhibitor in treating cancer. Formula (I) or tautomer, stereoisomers or a pharmaceutically acceptable salt thereof, wherein: W is (a) or (b), wherein the (c) represents a double or triple bond and the R1b and R1d are absent when the (d) represents a triple bond.

The present invention relates to compounds and compositions capable of acting as inhibitors of small ubiquitin-like modifier (SUMO) family of proteins. The compounds and compositions may be used in the treatment of cancer. There are disclosed, inter alia, methods of inhibiting an E1 enzyme, and compounds useful for inhibiting an E1 enzyme.

The present invention relates to the technical field of biomedical nanomaterials, and particularly relates to a dual-pathway energy inhibition enzyme-based nano-therapeutic agent, a preparation method thereof, and an application thereof. The dual-pathway energy inhibition enzyme-based nano-therapeutic agent comprises a functional protein, an oxidative phosphorylation inhibitor bound in the hydrophobic cavity of the functional protein, and a bacterial outer membrane vesicle encapsulating the functional protein and the oxidative phosphorylation inhibitor. During transportation, due to the hydrophobic interaction between the hydrophobic oxidative phosphorylation inhibitor and the functional protein, the biosafety is improved; at the same time, the bacterial outer membrane vesicle encapsulates the functional protein and the oxidative phosphorylation inhibitor, improving the tumor accumulation of the nano-therapeutic agent. When the nano-therapeutic agent is in an acidic tumor microenvironment, the nano-therapeutic agent dissociates, the activity of the functional protein is restored, and the oxidative phosphorylation inhibitor is released, realizing the selective control of the dual-pathway energy inhibition enzyme-based nano-therapeutic agent.

The application discloses a kind of bioactive polyamino acid nanocomposites, preparation method and purposes, by condensation reaction synthesis hyaluronic acid-block-poly amphiphilic block copolymer, by hydrophobic, electrostatic, metal coordination etc. Interaction covers CD73 small molecule inhibitor APCP and PD1 / PD-L1 inhibitor S7911, preparation HA@APCP / S7911.HA@APCP / S7911 is enriched in tumor area by EPR effect, under the joint action of hyaluronidase and low pH in tumor area, realize the release of APCP and S7911 in tumor tissue.APCP is inhibited CD73 enzyme activity, restores the metabolism and activity of NK cell, starts NK cell immune response;S7911 is inhibited after release in tumor tissue PD-L1 and PD-1 binding, blocks immune checkpoint and starts T cell immunity, combined with radiotherapy to improve antitumor immune response, amplify the range of effective immune response, for promoting the combined effect of radioimmunotherapy provides a new way of thinking.

To provide an enzyme-containing composition that enables suppression of enzyme activity decrease even in blood or serum and permits desorption between an organic ammonium salt and an enzyme.SOLUTION: An enzyme-containing composition of the present invention is an enzyme-containing composition allowing a reaction between an enzyme and a substrate in blood or serum, the composition containing a complex of the enzyme and an organic ammonium salt, the organic ammonium salt being composed of an amine compound and a carboxylic acid.SELECTED DRAWING: None

The invention discloses an application of gallic acid in preparation of a salmonella typhimurium CDSH inhibitor, and belongs to the technical field of biological medicine. CDSH enzyme activity inhibition experiment, H2S detection experiment, antibiotic stimulation experiment and greater wax moth infection model experiment analysis finds that the gallic acid can reduce the stress tolerance of S.Typhimurium by inhibiting the activity of CDSH enzyme, reduce the stress tolerance of S.Typhimurium, reduce the stress tolerance of S.Typhimurium, reduce the stress tolerance of S.Typhimurium, and reduce the stress tolerance of S.Typhimurium by inhibiting the activity of CDSH enzyme. The cysteine thiotransferase has the advantages that the cysteine thiotransferase can be used as a transferase inhibitor, the antibiotic sensitivity and the in-vivo removal effect of the cysteine thiotransferase are enhanced, the gallic acid is used for inhibiting the enzyme activity of CDSH and reducing the salmonella tolerance, and the cysteine thiotransferase inhibitor and the medicine for treating the caused infectious diseases are prepared and are used for preventing or treating salmonella typhimurium infection.

This invention belongs to the field of biomedical technology and relates to a polypeptide targeting cGAS and its applications. The polypeptide comprises an active peptide and a membrane-penetrating peptide, the membrane-penetrating peptide being fused to the N-terminus of the active peptide. The amino acid sequence of the active peptide is identical to amino acid regions 45-63 of human IκB kinase-binding protein (IKIP) or 43-60 of mouse IKIP. The polypeptide provided by this invention can enter cells, specifically bind to cGAS, inhibit cGAS aggregation and phase separation, thereby inhibiting cGAS enzyme activity, reducing type I interferon expression, maintaining antiviral immune homeostasis, and providing a new candidate strategy for the clinical treatment of viral infections and autoimmune diseases.

This invention provides the application of norzelamin in the preparation of NDM-1 enzyme inhibitors. Through cefotaxime hydrolysis assays, checkerboard minimum inhibitory concentration (MIC) tests, growth curves, bactericidal curves, hemolysis tests, and *Gnaphalium affine* infection experiments, it was demonstrated that norzelamin can inhibit NDM-1 enzyme activity and exhibits good synergistic antibacterial activity with the carbapenem antibiotic meropenem, enhancing the protective effect of meropenem against *Gnaphalium affine* larval infection models. Therefore, norzelamin, as a potential adjuvant for β-lactam antibiotics, can enhance the antibacterial effect of β-lactam antibiotics by inhibiting NDM-1 enzyme activity, which is of great significance for the clinical development of safe and effective β-lactam antibiotic adjuvants.

The invention belongs to the field of nucleic acid detection, and discloses a method for detecting oligonucleotide drugs based on an MSD (Meso Scale Discovery) platform and application of the method. According to the method, high-sensitivity quantitative detection is realized by designing a specific probe system: a capture probe and a detection probe are synergistically hybridized with target oligonucleotide to form a compound, the compound is fixed on a streptavidin-coated MSD plate, an anti-digoxin-SULFO-TAG antibody is combined, and a signal is detected by an electrochemical luminescence method. The innovation points are as follows: LNA modification enhances the stability and specificity of the probe, and the use amount of the probe is reduced by 50%; the process of a non-enzyme reaction system is simplified to 4 hours; sample treatment is optimized (RNALater is added to inhibit RNA enzyme degradation), and the method is suitable for complex matrixes such as serum and tissue homogenate. The sensitivity reaches 0.4 pM, the linear range spans five orders of magnitude, high specificity and high flux are achieved, and efficient and reliable technical support is provided for research and development of oligonucleotide drugs, pharmacokinetic research and clinical tests.

To provide anti- CD73 antibodies that achieve effective inhibition of CD73 enzymatic activity, which may be useful in the treatment of CD73 mediated diseases and disorders.SOLUTION: Anti- CD73 antigen binding proteins are provided. Biparatopic anti- CD73 antigen binding proteins are provided. Also provided are methods of inhibiting CD73 activity and methods of treating CD73 mediated diseases and disorders.SELECTED DRAWING: None

The invention discloses a specific glucanase protein crystal of oomycete core pathogenic factor xylan as well as a preparation method and application of the specific glucanase protein crystal. The high-purity PsXEG1 protein is successfully expressed and purified in pichia pastoris through a genetic engineering method, meanwhile, the crystallization condition that the protein can form a perfect crystal form is screened out, finally, crystal data are collected through X-ray crystal diffraction, and then the crystal structure of the protein is analyzed. The PsXEG1 small-molecule inhibitor is obtained through virtual screening, molecular dynamics simulation and other technologies by means of information provided by the structure, and the inhibitor effectively inhibits PsXEG1 enzyme activity and has a good prevention and control effect on various pathogenic bacteria. In conclusion, the PsXEG1 structural information obtained by combining a pichia pastoris cell expression system can be used for designing an antibacterial agent, and has a wide application prospect in the field of preventing and treating plant oomycetes diseases.