6results about How to "Has inhibitory activity" patented technology

The invention discloses an application of Lycobetaine in the preparation of an SHMT2 protein targeted inhibitor. According to the invention, 11 candidate compounds are obtained by adopting a molecular docking technology, and a CCK-8 cell viability experiment shows that the anti-proliferative activity of Lycobetaine on non-small cell lung cancer A549 and H1299 cells is superior to that of a standard SHMT2 inhibitor SHIN1. A Western blot result shows that the expression of the SHMT2 is down-regulated by the Lycobetaine in a dose-dependent manner, and the SHMT1 is not influenced. A gene knockout experiment shows that the anti-proliferative activity of the Lycobetaine depends on the expression of the SHMT2. In-vitro experiments and organoid models show that Lycobetaine significantly inhibits tumor growth and induces structural collapse and volume reduction of tumor organoids. The Lycobetaine can be used as an SHMT2 protein targeted inhibitor, and is applied to tumor treatment.

This invention provides compounds useful as active ingredients in pharmaceutical compositions for the treatment of pancreatic cancer. The inventors studied compounds useful as active ingredients in pharmaceutical compositions for the treatment of pancreatic cancer and discovered that 4-aminoquinazoline compounds possess excellent G12D mutant KRAS inhibitory activity, making them suitable for use as therapeutic agents for pancreatic cancer, thus completing this invention. The 4-aminoquinazoline compound or its salt of this invention can be used as a therapeutic agent for pancreatic cancer.

This invention discloses an antimicrobial peptide, HlHepcidin, derived from *Hemibarbus labeo*, and its application in regulating fish gut microbiota and preventing *Aeromonas hydrophila* infection. The antimicrobial peptide comprises the amino acid sequence QSHLSLCRYCCNCCRNKGCGYCCKF shown in SEQ ID NO:1, or a functional variant retaining antimicrobial activity and / or fish gut microbiota regulation activity. This invention further provides a nucleic acid molecule encoding the peptide, a recombinant expression vector, engineered bacteria or host cells, a preparation method, a composition containing the antimicrobial peptide, and its applications. The antimicrobial peptide exhibits inhibitory activity against various aquaculture-related bacteria and can be used to restore the diversity and community composition of fish gut microbiota after *Aeromonas hydrophila* infection. The antimicrobial peptide or composition can be prepared as a feed additive, bath agent, water treatment agent, spray, injection, or other aquaculture product, thereby providing a green technology solution for the prevention and control of bacterial diseases in fish and reducing antibiotic use.

The application discloses a donkey skin oligopeptide, and an application thereof. The amino acid sequence of the donkey skin oligopeptide is selected from Glu-Thr-Trp-Arg or Ala-Tyr-Phe-Pro-Lys. The donkey skin oligopeptide disclosed by the application has alpha-glucosidase and alpha-amylase inhibitory activity, can assist in reducing blood sugar, has very important significance for developing medicines with blood sugar reducing function, and can be used for preparing alpha-glucosidase, alpha-amylase inhibitors and anti-type 2 diabetes drugs.

This invention provides a benzothiadiazine 1,1-dioxide compound, its preparation method, and its applications. The general structural formula of the benzothiadiazine 1,1-dioxide compound is shown in Formula (I), or its isomers, or pharmaceutically acceptable salts, esters, or prodrugs thereof. The benzothiadiazine 1,1-dioxide compound of this invention has a novel structure, can selectively inhibit HDAC6 enzyme, has a strong protective effect on nerve cells, low toxicity, and low potential cardiotoxicity, and is expected to be used as a neuroprotective agent for the treatment of neurodegenerative diseases.