129results about How to "Inhibit phosphorylation" patented technology

The present invention relates to antibodies that differentially recognize multi-dimensional conformations of Aβ-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLS, and tau phosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid β1-42.

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.

A use of probiotic strain GM-263 (ADR-1) in treating renal fibrosis in diabetes is disclosed. The probiotic strain such as Lactobacillus renteri strain GM-263 (ADR-1) (accession No. CCTCC M 209263) is utilized to produce a composition for treating renal fibrosis in diabetes in an effective dose, thereby reducing the concentration of glycated hemoglobin and blood sugar and keeping body weight and kidney weight within normal range, as well as specifically inhibiting phosphorylation of JAK2/STAT1 signal transduction pathway and renal fibrosis-related protein expression.

A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.

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 provides application of a sesquiterpene compound 6-OAP in preparation of STAT3 inhibitors and in treatment of diseases unusually relevant to STAT3, and a pharmaceutical composition for treatment of diseases unusually relevant to STAT3. The pharmaceutical composition contains 6-OAP. 6-OAP can quickly combine with STAT3, can significantly inhibit phosphorylation of STAT3 in a cell and animal tumor-bearing model and significantly inhibit the activity of STAT3 induced by inflammatory factors, and has no significant toxic and side effect on other normal tissues. With the advantages of proper dose, significant curative effect, definite action target, and low toxic and side effects, etc., the 6-OAP has wide anticancer and anti-inflammatory application prospects clinically.

The invention discloses a formula of a traditional Chinese medicine for treating diabetic nephropathy. The formula is characterized by involving the following raw materials by weight: 6 parts of astragalus roots, 3 parts of Pseudostellaria heterophylla, 2 parts of angelica, 2 parts of radix rehmanniae, 2 parts of cornus officinalis, 2 parts of Salvia miltiorrhiza, 3 parts of raw coix seeds, 2 parts of earthworm, 2 parts of Poria, and 2 parts of rhizoma alismatis. Directed at qi-yin deficiency, i.e. the traditional Chinese medicinal core pathogenesis of diabetic nephropathy, the formula has the efficacy of supplementing Qi and nourishing Yin, dispersing blood stasis and promoting dieresis, and is suitable for different-stage diabetic nephropathy with the main manifestations of soreness and weakness of waist and knees, weakness all over the body, edema, foaming urine, nausea, skin pruritus, limb numbness or acroanesthesia (or chilling), dark red tongue, thin or greasy tongue coat, thin pulse or rapid pulse and the like. The formula involves simple medicines and can achieve a special effect. Previous long-term clinical practice and scientific research prove that the formula can significantly reduce the urinary protein excretion rate, delay the renal function progress, effectively improve glucolipid metabolism, effectively control blood pressure, improve the quality of life of patients, and greatly decrease kidney disease end point events, and has the advantages of stable long-term effect and good safety.

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 novel application of desloratadine and a pharmacologically acceptable salt of desloratadine in preparing a drug for treating alzheimer's disease and novel application in preparing a drug for treating and protecting nerve cells and/or increasing Abeta, clearing and/or inhibiting Tau protein phosphorylation related neurodegenerative diseases such as Parkinson's disease. According to a great number of experiments, the desloratadine and the pharmacologically acceptable salt of desloratadine have obvious effects of protecting nerve tool cells SH-SY5Y from STZ injuries, promoting removal of exogenous Abeta by SH-SY5Y cells, and also can obviously inhibit phosphorylation level of Tau proteins in the SH-SY5Y cells. Therefore, desloratadine and the pharmacologically acceptable salt of desloratadine can be used for treating the alzheimer's disease and nerve cell damages and/or Abeta and/or Tau protein related diseases, and is of significant meaning in developing novel clinical applicability of desloratadine.

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 provides application of evodiamine in preparation of an anti-osteoporosis drug and the anti-osteoporosis drug and relates to the technical field of biological medicine. The evodiamine can inhibit activation of protein kinase in an RANKL-induced osteoclast differentiation and maturation RANKL-ERK-NFAT signal channel in effective dose, further bone phagocytosis capability of RANKL-induced osteoclast is inhibited, expression of osteoclast differentiation specific genes such as c-Fos and NFATc1 is obviously reduced, bone absorption is inhibited, bone formation is promoted, and finally the effect of preventing osteoporosis is achieved. The application of the evodiamine in preparation of the anti-osteoporosis drug has the characteristics of definite curative effect and small side effect, and the problem that an existing medicine used for treating bone loss disease has serious adverse reaction in clinical application is relieved.

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.

The present invention discloses an Erk signal pathway inhibitor, and belongs to the field of cell biology. According to the present invention, the Mycobacterium tuberculosis secretory protein Mce3E capable of inhibiting the Erk1/2 signal pathway is firstly determined, and the Mce3E achieves the inhibition on the Erk1/2 signal pathway through spatial regulation on the Erk1/2 protein; the results of the present invention can provide new tools and ideas for the clinical treatment of various diseases, especially provide wide prospects in the fields of development, clinical application and the like of anti-tumor drugs and other drugs, and can further be directly used in the scientific research field or be used for guide the development of Erk1/2 inhibitor; and the result further provides the important theoretical significance for finding of the new drug target and screening of the new drug.