13 results about "Phosphorylation Inhibition" patented technology

The present invention relates to nuclear mitotic apparatus (NuMA) protein serine 395 (S395) phosphorylation inhibitor for use in preventing and / or treating cancer in a subject. The invention also relates to a pharmaceutical composition comprising a NuMA S395 phosphorylation inhibitor. Furthermore, the invention provides a method of screening for a candidate compound for preventing and / or treating cancer, and a method of detecting a dormant cancer cell in a subject. Corresponding methods of treating and / or preventing cancer are also provided.

The invention belongs to the technical field of biological medicine, and relates to pharmaceutical application of an oxidative phosphorylation inhibitor, in particular to application of the oxidative phosphorylation inhibitor in preparation of an immunomodulatory drug, and the immunomodulatory drug has the advantages that the function damage of newborn myeloid-derived suppressor cells caused by antagonism BCG (bacillus calmette guerin) vaccination is inhibited, and the immunomodulatory effect is improved. The compound is used for preventing or treating neonatal immune-related diseases caused by bacillus calmette guerin vaccine inoculation. The invention finds that the BCG can cause damage to the immunosuppression function of the MDSC of the suckling mouse through up-regulation oxidative phosphorylation, and the negative effect caused by inoculation of the BCG can be reversed by using the OXPHOS inhibitor, so that the immunosuppression function of the MDSC of the suckling mouse is successfully recovered in an in-vivo and in-vitro model, and the immune-related adverse reaction caused by inoculation of the BCG is expected to be improved.

This invention discloses the application and method of a STAT1-targeting inhibitor in the treatment of immune thrombocytopenic purpura (ITP). It employs ivermectin, a STAT1 nuclear translocation inhibitor, and fludarabine, a STAT1 activation inhibitor. By injecting either the activation inhibitor or the nuclear translocation inhibitor, the platelet count in a mouse model of ITP is increased. Fludarabine, a fluorinated nucleotide analog of vidarabine, is non-radioactive and a small-molecule phosphorylation inhibitor. Ivermectin is a small-molecule inhibitor of nuclear translocation mediated by α / β1 introgression protein. Both have high bioavailability and are widely used to treat various hematological diseases with good safety profiles. Their application in treating ITP is safe, effective, and shows high compliance.

The present invention provides a method for screening for a telomerase reverse transcriptase (TERT) phosphorylation inhibitor using TERT or a fragment thereof, and a TERT kinase.

The invention discloses an application of a polyphyllin monomer drug in cancer treatment. The polyphyllin monomer drug comprises at least one of polyphyllin I, polyphyllin II, polyphyllin VI and polyphyllin VII. The polyphyllin monomer drug inhibits proliferation, migration and angiogenesis of cancer cells and inhibits up-regulation of EGFR (epidermal growth factor receptor) by regulating phosphorylation of FGFR2 and a downstream signal channel thereof, and a new application scheme is provided for cancer treatment.

The present invention relates to nuclear mitotic apparatus (NuMA) protein serine 395 (S395) phosphorylation inhibitor for use in preventing and / or treating cancer in a subject. The invention also relates to a pharmaceutical composition comprising a NuMA S395 phosphorylation inhibitor. Furthermore, the invention provides a method of screening for a candidate compound for preventing and / or treating cancer, and a method of detecting a dormant cancer cell in a subject. Corresponding methods of treating and / or preventing cancer are also provided.

The invention provides a method for improving the sensitivity of an esophageal squamous carcinoma (ESCC) patient to neoadjuvant chemoradiotherapy. Specifically, by reducing the levels of CEBPB, AREG and / or EREG proteins, mitochondrial oxidative phosphorylation (OXPHOS) is inhibited, TCA circulation is inhibited, and / or ERBB signal pathways are inhibited, so that the sensitivity of ESCC patients to neoadjuvant radiotherapy and chemotherapy is improved. In addition, the invention also provides a method for predicting the sensitivity of an ESCC patient to neoadjuvant chemoradiotherapy, and a biomarker for predicting the sensitivity of the ESCC patient.

The invention discloses liver-soothing and depression-relieving type medicinal and edible weight-reducing tea based on AMPK / SREBP-1c pathway regulation and control and a preparation method of the weight-reducing tea. A targeted extraction technology is introduced and comprises the steps of step-by-step extraction, embedding purification, liquid phase preparation and the like, key components, such as hawthorn flavone, nuciferine and the like, acting on an SREBP-1c pathway are accurately extracted, the key components and medicinal and edible components such as ginseng, poria cocos and the like in a formula have a synergistic effect, AMPK phosphorylation is effectively activated, SREBP-1c nuclear translocation is inhibited, and the SREBP-1c protein is prepared. Deeper lipid metabolism regulation and control and liver-intestinal axis balance are realized. Cell and animal experiments show that the tea can significantly reduce accumulation of triglyceride and has no side effects of drugs.

In one embodiment, a problem to be solved by the present invention is to provide a new agent the agent being for at least one selected from the group consisting of promoting breast milk secretion, enhancing breast milk secretion function, improving inhibition of breast milk secretion function, and inhibiting mammary gland involution, said agent comprising, as an active ingredient, a substance that has not heretofore been known to have a breast milk secretion promoting effect. The present invention provides an agent for at least one selected from the group consisting of promoting breast milk secretion, enhancing breast milk secretion function, improving inhibition of breast milk secretion function, and inhibiting mammary gland involution, said agent containing a starting material derived from at least one selected from the group consisting of oranges, aloe, carrots, American ginseng, figs, almonds, hyuganatsu, laurel, apples, soybeans, chrysanthemums, wheatgrass, pepper, ginger, ebi-imo, Japanese yams, kuugaimo, Nikko maple, poppies, and radishes.

The application belongs to the technical field of biological medicine, and particularly relates to the use of SH2 domain-containing protein tyrosine phosphatase 1 (SHP1) in the preparation of a drug for treating chronic pain, in particular to the use of SHP1 in the preparation of a drug for treating chronic pain by regulating the morphology of spinal cord astrocytes, the integrity of the blood-spinal cord barrier and the STAT1-CXCL10-CXCR3 neuroimmune signal axis, and a chronic pain treatment strategy based on the signal axis. The application first discloses that SHP1 in spinal cord astrocytes directly dephosphorylates STAT1, inhibits the transcription of CXCL10 and the subsequent infiltration of T lymphocytes into the spinal cord, and discloses the core analgesic mechanism, thereby establishing SHP1 as a new target for treating chronic pain, and opening up a new way for the precise treatment of clinical chronic pain, especially neuropathic pain.

The invention discloses application of a CCNB1 phosphorylation inhibition tool in preparation of a medicine for preventing and / or treating triple negative breast cancer, and particularly relates to application of a CCNB1 protein S128 site phosphorylation inhibitor in preparation of a medicine for preventing and / or treating triple negative breast cancer. The phosphorylation inhibitor refers to a tool or means used in the process of blocking or weakening protein phosphorylation, particularly a gene editing system, and the 128 serine Ser coded by a CCNB1 gene is mutated into alanine Ala which is recorded as S128A in a target cell. Compared with a traditional small molecule drug, the gene editing tool accurately intervenes phosphorylation modification at the gene level, has the advantages of being clear in mechanism, high in targeting performance, high in safety and the like, is suitable for basic research and potential clinical transformation of TNBC targeted therapy, and has a good application prospect.

The present application relates to the technical field of medicine, and particularly relates to application of ganoderma triterpene in preparation of medicine for treating cervical cancer. Ganoderma triterpene (Ganodecalone A, referred to as GDA) can inhibit migration, proliferation and clonogenic capacity of cervical cancer cells; GDA can arrest the cell cycle of cervical cancer cells in G0 / G1 phase, and with the increase of the concentration of GDA, the proportion of cells in G0 / G1 phase is significantly increased; GDA can promote apoptosis of cervical cancer cells, and with the increase of the concentration of GDA, the proportion of late apoptotic cells is significantly increased; GDA can promote apoptosis of cervical cancer cells by reducing the phosphorylation level of Akt in the cervical cancer cells. GDA and Akt phosphorylation agonist SC79 are mutually antagonistic, and when GDA is combined with Akt phosphorylation inhibitor MK-2206, the apoptosis of two strains of cervical cancer cells is promoted. GDA can induce apoptosis of cells by inhibiting phosphorylation of Akt, up-regulating pro-apoptotic protein Bad and down-regulating anti-apoptotic protein Bcl-2, and thus the anti-tumor effect is exerted.

The invention relates to the field of natural products, in particular to application of a p65 phosphorylation inhibitor in preparation of a medicine for treating or preventing inflammation. The p65 phosphorylation inhibitor is any one of sesquiterpene compounds I, II and III or a medicinal derivative thereof, and the structural formulas of the sesquiterpene compounds I, II and II are respectively shown as the formulas I, II and III. The invention has the following technical effects: the three sesquiterpenoids provided by the invention can be used as p65 phosphorylation inhibitors for inhibiting phosphorylation of P65 protein. The compound has a remarkable inhibition effect on synthesis and release of inflammatory factors TNF-alpha, IL-1alpha, IL-1beta and IL-6 in immune cells, and can be used as an anti-inflammatory drug for treating inflammatory diseases.