5 results about "Inhibition enzyme" patented technology

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.

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.