11 results about "Hsp Inhibitor" patented technology

The application discloses an albumin nano-drug based on HSP90 inhibitor and a preparation method and application thereof, and belongs to the technical field of medicines.The short peptide A6 is modified to human blood albumin through a connecting chain, and the human blood albumin modified by the A6 is self-assembled with geldanamycin derivative G2111 in the presence of an organic solvent, so that the G2111 is combined to the hydrophobic region of the human blood albumin through a non-covalent bond, effective loading of the G2111 is realized, the solubility of the geldanamycin derivative is improved, the drug is targetedly released into cancer cells with high expression of CD44, the targeted accumulation of the drug in tumor tissues is enhanced, damage to other normal tissues and cells caused by off-target effects of the drug is avoided, the albumin nano-drug can be simultaneously used for chemotherapy of leukemia and solid tumors, and has important practical significance.

The present disclosure is directed to Hsp90 inhibitors having the Formula (I), subformulae thereof, pharmaceutically acceptable salts, stereoisomer, or tautomer thereof, and methods of use thereof.

The present invention relates to a composition comprising an inhibitor of herpesvirus entry mediator (HVEM) or its ligand and a heat shock protein (HSP) inhibitor for treating or preventing cancer. The use of an inhibitor of HVEM or its ligand and an HSP inhibitor in combination exhibits a synergistic effect on anticancer activity, compared to the use thereof singly, and shows an effect within as fast as 72 hours after administration. Therefore, the use of an inhibitor of HVEM or its ligand and an HSP inhibitor in combination can be advantageously utilized for preventing or treating cancer.

The invention discloses a photo-thermal immunoregulation nanofiber scaffold and a preparation method and application thereof.The photo-thermal immunoregulation nanofiber comprises nanofiber with polylactic acid as a base material, and black phosphorus nanosheets and an HSP90 inhibitor 17-DMAG are jointly loaded in the nanofiber through a high-voltage electrostatic spinning technology; the photo-thermal immunoregulation nanofiber scaffold is applied to liver cancer postoperative immunotherapy through a photo-thermal therapy method. According to the photo-thermal immune regulation and control nanofiber scaffold, a PTT effect is locally generated under near-infrared irradiation, and a strong ISR-ICD cascade reaction is driven. Meanwhile, the exposed DAMPs enhance tumor immunogenicity, recruit cytotoxic T lymphocytes and reprogram an immunosuppressive cell population, so that an immunosilence microenvironment is remodeled into a responsive tumor microenvironment and cooperates with anti-PD-L1, lasting immune memory is established, and finally recurrence and metastasis of postoperative liver cancer are effectively inhibited.

The invention discloses a light-controlled heat shock protein 90 degradation agent as well as a preparation method and application thereof, and belongs to the technical field of medicines. The degradation agent is synthesized by coupling a BIIB021 derivative of targeted Hsp90 and a dihydroporphyrin photosensitizer. The compound can degrade Hsp90 protein in tumor cells, client protein HIF-1alpha of the Hsp90 and Hsp70 protein capable of forming a compound with the Hsp90 in a light-controlled manner. The compound is expected to solve the problems of tumor drug resistance and the like of the traditional Hsp90 inhibitor and Hsp90 PROTACs, and the hypoxic microenvironment in tumors is improved.

The present application belongs to the field of biological medicine, and particularly relates to a pharmaceutical composition containing HSP90 inhibitor and application thereof, wherein the composition contains an effective amount of HSP90 inhibitor and a pharmaceutically acceptable carrier. The pharmaceutical composition containing HSP90 inhibitor has a significant therapeutic effect on esophageal cancer, lung cancer, gastric cancer and liver cancer cells, and has less toxicity to normal cells. The HSP90 inhibitor composition has a significant inhibitory effect on the proliferation and migration of esophageal cancer cells, can significantly increase the expression of Cleaved-PARP, and promotes the apoptosis effect. The pharmaceutical composition containing HSP90 inhibitor can improve the bioavailability of the drug, and can produce a synergistic effect on the drug efficacy. The therapeutic effect on tumor drug resistance is obviously better than that of single drug use.

The invention discloses an anti-tumor multifunctional membrane bionic HSP90 nano inhibitor as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention aims to solve the technical problems that the existing HSP90 inhibitor is poor in selectivity, high in systemic toxicity and limited in single-mode treatment effect, and the cancer cell antioxidant mechanism in the existing CDT / PDT combined therapy weakens the ROS anti-tumor effect. According to the key point of the technical scheme, the invention provides the multifunctional membrane bionic HSP90 nano inhibitor consisting of a chlorophyllin-iron complex (having HSP90 inhibition, photosensitivity and Fenton catalysis functions), a calcium carbonate nano core and a tumor cell membrane coating layer.

The application provides a kind of targeted nano-drug based on pH response protein self-assembly and a preparation method thereof, and belongs to the technical field of nanomaterials.The application first activates photosensitizer Ce6 and peptide segment cNGQGEQc respectively, then couples with CAT respectively, to prepare photosensitizer-protein conjugate and photosensitizer-peptide segment conjugate, and then obtains the nano-probe through the self-assembly behavior of photosensitizer-protein conjugate, photosensitizer-peptide segment conjugate, hydrophilic silver sulfide quantum dots and HSP90 inhibitor.The nano-probe not only realizes the drug release and NIR-II imaging guidance of tumor microenvironment response, but also relieves hypoxia and inhibits heat resistance synchronously, truly realizes the synergistic amplification effect of PDT / PTT, and provides a promising strategy for precise and efficient treatment of NSCLC.

The present invention provides inhibitors of proteins that activate the erythroblast transformation-specific proto-oncogene (2)(ETS2), and their use in the treatment or prevention of inflammatory and / or autoimmune diseases. Inhibitors are generally MEK inhibitors, HSP90 inhibitors, RAF inhibitors, SRC inhibitors, and / or ERK inhibitors. The present invention also encompasses diagnostic methods and methods for screening for agents that reduce macrophage activation.

The invention discloses an evodiamine conjugate or a pharmaceutical salt thereof. The structural general formula of the evodiamine conjugate or the pharmaceutical salt thereof is selected from one of the following structures, according to the invention, a compound 1a or a compound 1b with an extremely strong in-vitro inhibition effect on tumor cell growth is used as a pharmacophore to be fused with an Hsp90 inhibitor, and the Hsp90 inhibitor, namely the evodiamine conjugate, is designed and synthesized. According to the evodiamine conjugate disclosed by the invention, an Hsp90 inhibitor in the structure is partially combined with eHsp90 secreted into a microenvironment by tumor cells in a targeting manner, and the tumor targeting property of the evodiamine conjugate is remarkably improved compared with that of a compound 1a and a compound 1b under the cell endocytosis mediated by the eHsp90, so that a new strategy is expected to be provided for improving the tumor treatment effect of a natural product and a derivative thereof.

This invention concerns various methods of using labeled HSP90 inhibitors to improve treatment of cancer patients with HSP90 inhibitors, including ex vivo and in vivo methods for determining whether a tumor will likely respond to therapy with an HSP90 inhibitor.