11 results about "Hsp90" patented technology

The invention relates to the technical field of aquaculture disease prevention and control and molecular biology, in particular to an RNA interference agent for killing ichthyophthirius multifilis, a preparation method, a composition and application. The interference agent is dsRNA / siRNA / shRNA or an expression vector of the dsRNA / siRNA / shRNA of targeted EF1-alpha, HSP90, ICP1 and ICP2; t7 tailed primer amplification, in-vitro transcription and annealing are adopted to prepare dsRNA, the dsRNA can be further prepared into a water body treatment composition with liposomes / chitosan and other carriers, and soaking treatment (20-28 DEG C, 1-48 h) is carried out in a grazing body stage. Under the conditions of 1 mu g / mL, 25 DEG C and 24 hours, the expression of the target gene is obviously reduced (2-delta delta Ct is less than or equal to 0.55), and the corrected death rates of 40.16% (EF1-alpha), 45.51% (HSP90), 21.39% (ICP < 1 >) and 19.39% (ICP < 2 >) are obtained. The scheme is green, has low residue, can be engineered, and is suitable for preposed blocking of the white-spot disease transmission chain in aquaculture.

This invention discloses a monoclonal antibody targeting HSP90 and its application. The monoclonal antibody targeting HSP90 can effectively inhibit the tumorigenicity and invasiveness of breast cancer cells, lung cancer cells, and osteosarcoma cells, and can significantly inhibit tumor growth in vivo. This invention provides a new targeted drug for diseases or symptoms related to high expression of HSP90, with broad prospects for clinical application.

This invention relates to a compound based on CRBN ligand-induced ubiquitination degradation of Hsp90, its preparation method and uses, as shown in X-Y-Z, where X represents the ligand of HSP90 protein, Z represents the ligand of E3 ligase, and Y represents the chain connecting X and Z. This type of compound can be used to treat or prevent tumors.

The invention relates to the technical field of radiopharmaceuticals, and discloses a polypeptide compound targeting HSP90, a radioactive probe labeling precursor, a radioactive probe and a preparation method and application thereof, a T7 bacteriophage display polypeptide library is adopted to screen polypeptide specifically bound with HSP90, and the polypeptide compound targeting HSP90 is obtained; the method comprises the following steps: synthesizing a polypeptide compound targeting HSP90, mixing the polypeptide compound with a connecting arm and a chelating agent, carrying out a coupling reaction to obtain a labeled precursor crude product, and purifying to obtain a radioactive probe labeled precursor targeting HSP90; the nuclide eluent is eluted, then the nuclide eluent is mixed with the radioactive probe labeling precursor of the targeted HSP90, and after incubation, the radioactive probe of the targeted HSP90 is obtained. The radioactive molecular probe prepared by the invention can be specifically combined with HSP90 protein, has higher affinity and functional activity to HSP90, and can evaluate the expression level of HSP90 in vivo in real time.

The present invention relates to a chromene-benzimidazole derivative or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the derivative as an active ingredient, the chromene-benzimidazole derivative of the present invention being activated in cancer cells, being capable of inhibiting tubulin polymerization and inhibiting a C-terminal domain of Hsp90, and being capable of preventing or treating cancer, or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the derivative as an active ingredient. When the compound is administered to a subject, cancer cell cycle arrest can be caused to induce cell apoptosis and hinder the activity of onco-protein, and the compound can be used as a novel double-targeting anti-cancer drug to prevent or treat cancers, preferably to prevent or treat triple negative breast cancer.

The expression of the ATXN2 gene can be modulated to reduce the amount of ataxin-2 protein produced by a cell. This can be accomplished by administering to the cell an effective amount of an ATXN2 modulating agent. Screening was performed with 428,749 compounds for lowering expression of an ATXN2-luciferase reporter in HEK-293 cells, with a multiplexed cell viability assay to ensure target reduction in the absence of cytotoxicity. Secondary qHTS assays included a CMV-luciferase reporter expressed in HEK-293 cells as well as a biochemical assay using recombinant luciferase to detect inhibitors of the reporter enzyme. A diverse set of compounds were found to reduce ATXN2 expression, including compounds targeting HSP90, cardiac glycosides, NaK-ATPases and topoisomerases.

This application relates to a cyanobacteria extract with photothermal damage repair effects, its preparation method, and its application, belonging to the field of cosmetic raw material technology. The cyanobacteria extract provided in this application can be used to balance the inflammatory and repair signaling pathways of skin cells after photothermal damage, and can be used to prepare skin care products with soothing, anti-inflammatory, and barrier-repair-promoting effects. It can synergistically balance the pro-inflammatory damage signaling pathway TLR4 / NF-κB axis and the survival-promoting repair signaling pathway HSP90 / PI3K-Akt axis simultaneously activated in skin cells after photothermal damage, targeting multiple points. This can more effectively control excessive inflammation, reduce secondary damage, and enhance the cell's self-repair ability. It is suitable for various scenarios such as sunburn, post-laser surgery, and thermal environment damage, and has significant technical advantages compared to existing technologies, with broad application prospects and huge market value.

The invention relates to a novel EZH2-HSP90 double-effect inhibitor for the first time, a preparation method of the EZH2-HSP90 double-effect inhibitor and application of the EZH2-HSP90 double-effect inhibitor to treatment of diseases / symptoms mediated by EZH2, HSP90 or the EZH2 and the HSP90, especially glioblastoma.

The present invention relates to: a chromene-benzimidazole derivative or a pharmaceutically acceptable salt thereof; and a composition for preventing or treating cancer, the composition comprising the derivative as an active ingredient. The chromene-benzimidazole derivative according to the present invention is activated in cancer cells to inhibit tubulin polymerization and suppress the C-terminal domain of Hsp90, thereby blocking the cell cycle of cancer cells, inducing apoptosis, and inhibiting the activity of oncoproteins, and thus can be used as a novel dual-target anticancer drug for preventing or treating cancer, preferably for preventing or treating triple-negative breast cancer.

The present invention relates to an inhibitor of heat shock protein 90. Disclosed are a heat shock protein 90-based bivalent inhibitor, and a preparation method therefor and the use thereof. The bivalent inhibitor is a compound having a structural formula as shown in formula I: A-L-B Formula I, or a pharmaceutically acceptable salt, solvate, or optical isomer thereof, wherein A and B are ATP inhibitors of heat shock protein 90, and the motif structure of L is a flexible linker group of PEG or alkanes, or a rigid linker group comprising aryl, heteroalkyl, or heteroaryl. The bivalent inhibitor can effectively inhibit the activity of molecular chaperone HSP90, hinder the folding and modification of a substrate protein, degrade the substrate protein via a ubiquitin-proteasome degradation pathway, induce non-native dimerization of HSP90, and interfere with protein-protein interactions associated with HSP90. In addition, the bivalent inhibitor reduces the heat shock response induced by HSP90 inhibition, and exhibits potent activity in degrading the substrate protein.

The present application relates to the technical field of radiopharmaceuticals, and discloses a polypeptide compound targeting HSP90, a radioactive probe labeling precursor, a radioactive probe and a preparation method and application thereof, wherein a polypeptide compound targeting HSP90 is obtained by screening a polypeptide specifically combined with HSP90 from a T7 phage display polypeptide library; the polypeptide compound targeting HSP90 is synthesized, and is subjected to a coupling reaction by being mixed with a linking arm and a chelating agent to obtain a crude product of a labeling precursor, and after purification, a radioactive probe labeling precursor targeting HSP90 is obtained; a nuclide eluent is eluted, and then is mixed with the radioactive probe labeling precursor targeting HSP90, and after incubation, a radioactive probe targeting HSP90 is obtained. The radioactive molecular probe prepared by the present application can be specifically combined with HSP90 protein, has high affinity and functional activity for HSP90, and can evaluate the expression level of HSP90 in real time in vivo.