131results about How to "Inhibit phosphorylation" patented technology

This invention provides substituted Phenyl-(2-[1,3,4]thiadiazol-2-yl-phenyl)-amine and (2-[1,3,4]Oxadiazol-2-yl-phenyl)phenyl-amine compounds which act as inhibitors of MAPK/ERK Kinase (“MEK”) enzymes and pharmaceutical compositions and methods for their use in immunomodulation and in the treatment and alleviation of inflammation, and proliferative diseases such as cancer and restenosis.

A thiazolylimidazole derivative represented by the formula

or a pharmaceutically acceptable salt thereof, and an ALK5 inhibitor, an therapeutic agent for alopecia or a hair growth agent having the above as an active ingredient, wherein:

X¹ and X² are different from each other and represent a sulfur atom or a carbon atom; R¹ represents a phenyl group; a substituted phenyl group; a phenyl group condensed with a hetero aromatic ring; a pyridyl group; or a pyridyl group condensed with a hetero aromatic ring; R² represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms substituted with 1 to 5 halogen atoms, an alkoxy group having 1 to 6 carbon atoms, an alkanoyl group having 1 to 5 carbon atoms, or a hydroxyalkyl group having 1 to 6 carbon atoms, A represents a group which is represented by the formula.

The present invention provides an inhibitory substance against ALK5 which is a TGF-β type I receptor and provides a hair growth stimulant or a hair growth agent based on its novel activities.

The present invention relates to methods and compositions for the diagnosis, treatment, management, or prevention of plasma cell disorders, including systemic light-chain amyloidosis (AL) and multiple myeloma (MM). In particular, the invention encompasses the use of anti-CD32B antibodies, analogs, derivatives or fragments thereof, or compounds or agents that bind to CD32B and modulate CD32B activity in the plasma cells of mammals. The invention also encompasses the use of anti-CD32B antibodies, analogs, derivatives or fragments thereof, or CD32B binding compounds or agents in combination with or in addition to other cancer therapies for the treatment, prevention, management, or amelioration of a plasma cell disorder characterized by the expression of CD32B, or one or more symptoms thereof. The invention further relates to the use of anti-CD32B antibodies, analogs, derivatives or fragments thereof for the detection of aberrant or altered expression of CD32B in plasma cells, to diagnosis and/or characterize a plasma cell disorder.

The present invention includes the disclosure of the hPER2 gene and a mutant of the hPER2 gene that participates in the human circadian biological clock. The product of the mutant hPER2 gene found in some familial advanced sleep phase syndrome patients is hypophosphorylated by casein kinase epsilon due to the serine-to-glycine mutation caused by the point mutation of the genomic sequence. Specifically, this serine-to-glycine mutation affects the casein kinase epsilon binding region of the hPER2 protein, thus blocking the phosphorylation cascade ordinarily caused by the binding of casein kinase epsilon to hPER2.

The invention relates to pharmaceutical compositions, as well as health functional food compositions and quasi-drug compositions, for preventing, treating, or improving rheumatoid arthritis, comprising a monoacetyldiacylglycerol compound as an active ingredient. The monoacetyldiacylglycerol of the invention is effective in inhibiting the phosphorylation of STAT-3 known to be a therapeutic target for rheumatoid arthritis. As the monoacetyldiacylglycerol is an effective therapeutic agent without toxicity, the monoacetyldiacylglycerol can overcome the side effects of the medicines currently used in the treatment of rheumatoid arthritis. Thus, the monoacetyldiacylglycerol can be used for preventing, treating or improving rheumatoid arthritis.

The invention relates to the field of diagnosis and treatment of tumors, in particular to a polypeptide in plasma, which has an amino acid sequence as shown in SEQ ID No.1, wherein the polypeptide can be used as a tumor marker used in a method and a kit for diagnosing the generation and the metastasis of the tumors. The invention also relates to a method and a medicament for treating tumors and metastasis of tumors.

The invention discloses a medicinal composition for resisting non-small cell lung cancer. The active components of the medicinal composition comprise an artemisinin derivative and EGFR-TKI (epidermal growth factor receptor-tyrosine kinase inhibitor), wherein the artemisinin derivative is selected from one of dihydroartemisinin, artesunate, artemether and arteether; and the EGFR-TKI is selected from one of gefitinib, erlotinib, afatinib and osimertinib. The invention also discloses application of the medicinal composition to preparation of medicines for treating and resisting the non-small cell lung cancer. When the medicinal composition provided by the invention is used for treating the non-small cell lung cancer, the medicinal effect which is more excellent than that of the singly used EGFR-TKI can be achieved, the sensitizing effect is achieved, the problem of partial medicine resistance of the non-small cell lung cancer EGFR-TKI is solved, and a scientific basis is provided for the development of new medicines.

Antagonistic TNFR superfamily polypeptides, such as antibodies and antigen-binding fragments thereof, and the use of these polypeptides to inhibit the proliferation of regulatory T cells (T-regs). For example, antibodies of the invention include antagonistic TNFR2 antibodies and antigen-binding fragments thereof, and can be used to suppress the T-reg-mediated deactivation of tumor reactive T-lymphocytes, as well as to treat a wide variety of cancers and infectious diseases.

The invention discloses a new use of notoginsenoside R1 in the preparation of medicines for preventing and/or treating the inflammatory diseases of the digestive system or healthcare foods as an active component. Experiment results show that the notoginsenoside R1 has an inhibition effect on the NF-kappa B signal pathway, and has substantial prevention and treatment effects on the NF-kappa B signal pathway mediated ulcerative colonitis, so the notoginsenoside R1 can be developed to medicines for preventing and/or treating the inflammatory diseases of the digestive system or healthcare foods. The new use urges the notoginsenoside R1 to fully perform its medicinal values, and is very important for researching and applying Panax Notoginseng.

The invention relates to the field of tumor diagnosis and treatment, and particularly relates to a polypeptide in blood plasma with an amino acid sequence as shown in SEQ ID No.1. The polypeptide can be used as a tumor marker, and can be used in methods and kits for diagnosing tumorigenesis and tumor metastasis. The invention also relates to a method and a drug for treating tumor and tumor metastasis.

The invention discloses a pyrrolidine[3,4-d]pyrimidine derivative and a preparation method and an application thereof. The pyrrolidine[3,4-d]pyrimidine derivative is an inhibitor of a type I insulin-like growth factor receptor (IGF-1R), and has a good IGF-1R inhibiting function and a good cancer cell proliferation inhibiting function, so that the pyrrolidine[3,4-d]pyrimidine derivative can be taken as a therapeutic agent for treating tumors and relevant diseases.

The invention discloses a polypeptides making up of 25 amino acids, corresponding cDNA coded sequence, its preparation, the use of the peptide, its derivant and corresponding cDNA in treating tumor and other hyperplasia disease. The invention characterized in that it confirms that p55PIK protein with 25 amino acid in its amino end have key function in combining Rb, blocking Rb phosphorylation inside the cell, thus obtain a biological effect of inhibiting cell division. Making use of the peptide and transfecting corresponding cDNA and expressing the peptide inside the cell, can inhibit effectively cell growth and tumor growth. Meanwhile, the invention also discloses a novel method for blocking Rb phosphorylation process, and provides a novel method for manufacturing a tumor treating medicine.

The invention relates to an anti-tumour combined pharmaceutical composition and application thereof, and belongs to the field of biological medicines. In order to further improve the cancer treatmenteffect and reduce the drug cost of applying trabectedin at the same time, the invention provides an anti-tumour combined pharmaceutical composition, which comprises an effective amount of enterolactone or a plant lignan precursor capable of being converted into enterolactone in a body, and further comprises an effective amount of trabectedin. According to the invention, experiments prove that combined application of trabectedin and enterolactone can inhibit proliferation, activity, metastasis, invasion and angiogenesis of ovarian cancer and promote tumour cell apoptosis; and, when the two drugs are combined for use, the inhibition effect on the ovarian cancer is stronger than that of a single drug after the dosage of the two drugs is halved. According to the invention, the administration amount of trabectedin is reduced by using the enterolactone with lower cost; the economic burden of a patient is reduced; and the enterolactone can also reduce the side effect of trabectedin. The combined pharmaceutical composition disclosed by the invention can improve the anti-tumour curative effect and promote clinical popularization of trabectedin.

The present invention discloses a drug for treatment of type II diabetes, and the drug comprises medicinal ingredients of gentiopicroside and / or sweroside, or comprises the medicinal ingredients of a panax notoginseng total extract including the two components. Experiments show that the panax notoginseng total extract, gentiopicroside and sweroside two monomers and a mixture of the gentiopicroside and the sweroside have the role of good resistance to the type II diabetes, and can inhibit phosphorylation of type II diabetes target spot PEPCK and Akt, Erk and the like. The effect of the mixed gentiopicroside and sweroside is better than the effect of other monomer and single use of the gentiopicroside and sweroside two monomers. A new research channel for treatment of type II diabetes is opened, and medicinal value of the panax notoginseng is further developed.