4results about How to "Inhibit enzyme activity" patented technology

The application belongs to the technical field of biological medicine, and particularly relates to a polypeptide degradation agent for targeted degradation of CD26 and a preparation method and application thereof. The polypeptide degradation agent is obtained after coupling of a tetrapeptide and lenalidomide. The amino acid sequence of the tetrapeptide is any one of SEQ ID NO. 1 and SEQ ID NO. 2. The polypeptide degradation agent can specifically target and degrade DPP4, i.e. CD26, but cannot degrade DPP4 isozymes such as DPP7, DPP8 and DPP9, and thus has high selectivity. In addition, the polypeptide degradation agent has small molecular weight, one end is a natural short peptide, has good tissue compatibility, can quickly degrade target proteins in 6 hours, and thus has good tissue permeability.

The application discloses a quinazoline-4(3H)-ketone compound and a preparation method, a pharmaceutical composition and application thereof, the structure of the compound is as shown in the formula (I), and the compound comprises isomers, pharmaceutically acceptable salts or mixtures thereof. The compound and the pharmaceutical composition thereof have a high inhibitory effect on PARP7, the inhibitory activity reaches a nanomolar concentration level, can significantly promote the release of immune factors, are used for immunotherapy of tumors, and can exert good drug efficacy at a molecular level and a cell level. In addition, the preparation method of the compound is simple and easy to implement.

The application discloses a use of hydrogen peroxide (H2O2) in constructing an oxidative stress model of female and male chicken primordial germ cells (PGCs); in the application, the H2O2 can achieve the effect of oxidative stress of the female and male chicken PGCs by increasing the ROS content in the female and male chicken PGCs, inhibiting the T-SOD and CAT enzyme activities and increasing the MDA content; the application verifies the effect of the oxidative stress model established by the H2O2 on the female and male chicken PGCs by screening different concentrations of the H2O2 added into the female and male chicken PGCs and then detecting the apoptosis, reproductive markers, mitochondrial functions and autophagy genes of the cells; in the application, the effect of the oxidative stress model constructed by the H2O2 on the female and male chicken PGCs provides new experimental basis for clarifying the molecular mechanism of oxidative stress causing poultry reproductive damage, and provides new ideas and targets for protecting the PGC functions of poultry and improving the reproductive efficiency by regulating the oxidative stress, autophagy or apoptosis pathways in the future, and provides important research and development basis for the selection of compounds resisting oxidative stress.

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.