11 results about "Inhibition enzyme" patented technology

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 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 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.

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 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.

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 present invention relates to cyano-containing 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.