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68results about How to "Reduce phosphorylation" patented technology

Pyridylpyrimidyl amine compounds or pyridylpyridyl amine compounds and application thereof

The invention discloses pyridylpyrimidyl amine compounds or pyridylpyridyl amine compounds disclosed as Formula I and application thereof in preparing antineoplastic drugs, belonging to the technical field of drugs. The compounds can selectively inhibit CDK4 and CDK6, enable G1-period tumor cells to stop growth and G1-period tumor cells to reduce, can effectively lower the phosphorylation of the tumor inhibiting protein Rb in the Ser780 site, and thus, can be used for various diseases caused by cell cycle control maladjustment participated by CDK4 and CDK6. The compounds are especially suitable for treating malignant tumors, and have the characteristics of high selectivity, high activity and high tumor cell proliferation resistance.
Owner:GUANGZHOU BEBETTER MEDICINE TECH CO LTD

Beta-carboboline GSK3beta/DYRK1A dual inhibitor and preparation method thereof and application of beta-carboboline GSK3beta/DYRK1A dual inhibitor in resisting Alzheimer's disease

The invention discloses a beta-carboline GSK3beta / DYRK1A dual inhibitor as shown in a general formula I, a preparation method of the beta-carboline GSK3beta / DYRK1A dual inhibitor and application of the beta-carboline GSK3beta / DYRK1A dual inhibitor in resistant the Alzheimer's disease. A novel beta-carboline derivative has GSK3beta / DYRK1A dual inhibition activity, and a preparation method of the beta-carboline derivative serving as the GSK3beta / DYRK1A dual inhibitor is provided. Meanwhile, the invention also discloses application of the beta-carboline derivative in preparation of a medicine for treating the Alzheimer's disease. The beta-carboline derivative can provide a theoretical basis for discovery of a novel AD treatment drug.
Owner:GENERAL HOSPITAL OF THE NORTHERN WAR ZONE OF THE CHINESE PEOPLES LIBERATION ARMY

GSK-3beta/ChE double inhibitor as well as preparation method and application thereof

The invention discloses a GSK-3beta / ChE double inhibitor with the structural formula shown as formula (I), or pharmaceutically acceptable salts and solvates of formula (I). The chemical small molecules involved in the invention can effectively inhibit the enzyme activity of GSK-3 beta, AChE and BChE, have the effects of improving cognition, reducing tau protein phosphorylation and reducing neuroinflammation, and have important application value in the preparation of drugs for preventing or treating Alzheimer's disease.
Owner:CHINA PHARM UNIV

Research method for pharmacologic action of mangiferin on mouse diabetes

InactiveCN111317830AIncreased antioxidant enzymesImprove renal dysfunctionCompounds screening/testingOrganic active ingredientsStainingAntioxidative enzyme
The invention discloses a research method for the pharmacologic action of mangiferin on mouse diabetes. The research method comprises material selection and an experimental method, biochemical parameter evaluation, histological analysis, measurement of reactive oxygen species (ROS), determination of malondialdehyde (MDA) and antioxidase, analysis of renal tissue inflammatory factors, immunofluorescent staining, Western blotting and statistic analysis. According to the research method, a trichrome staining method is utilized to observe renal morphology; a kit is utilized to determine a blood biochemical index; levels of inflammatory cytokines, the antioxidase, the MDA and the ROS are determined; expression of fibronectin, collagen I and alpha-SMA is detected by an immunohistochemical method, and regulation of paths of TGF-beta 1 and phosphatase and tensin homolog/phosphatidylinositol 3-hydroxy kinase/protein kinase B (PTEN/PI3K/Akt) is detected by Western blotting; researches show thatthe mangiferin can significantly improve the renal dysfunction of diabetic mice; renal interstitial fibrosis can be prevented by reducing positive expression of fibronectin (FN), collagen type I (ColI) and alpha-smooth muscle actin (SMA) during therapy with the mangiferin; and meanwhile, mangiferin increases the antioxidase, reduces phosphorylation of the PI3K and Akt, inhibits the renal interstitial fibrosis, and provides more theoretical foundations for clinical application of traditional Chinese medicine in treating diabetes.
Owner:JILIN UNIV

CaMKII, IP3R, CALCINEURIN, P38 AND MK2/3 INHIBITORS TO TREAT METABOLIC DISTURBANCES OF OBESITY

ActiveUS20140314789A1Reduce activityReduces activationOrganic active ingredientsFermentationHepatic glucoseIsrapafant
The present invention relates to methods of treating or preventing a metabolic disorder in a subject, methods of treating or preventing coronary artery disease in a subject with a metabolic disorder, as well as methods of reducing hepatic glucose production in a subject. Such methods include, but are not limited to, the administration to the subject of inhibitors or activators of CaMKII, IP3Rs, calcineurin, p38, MK2 / 3, HDAC4, Dach1, Dach2, or any combination thereof. The invention also provides methods of identifying a compound that inhibits the activity of CaMKII, IP3Rs, calcineurin, p38, MK2 / 3, HDAC4, Dach1 or Dach2, or reduces the activity and / or activation of CaMKII, IP3Rs, calcineurin, p38, MK2 / 3, HDAC4, Dach1 or Dach, or activates CaMKII, IP3Rs, calcineurin, p38, MK2 / 3, HDAC4, Dach1 or Dach2.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK

Methods for treating neurodegenerative diseases and for identifying agents useful for treating neurodegenerative diseases

InactiveUS20140220036A1Improve neurotransmissionIncrease neurotransmissionOrganic active ingredientsCompound screeningMolecular biologyDegenerative disease
The present invention provides methods of inhibiting a tau protein such as h-tau42 or a biologically active fragment, derivative or analog thereof, methods of treating a disease caused by a tau protein such as h-tau42, and methods to identify agents that may inhibit a tau protein such as h-tau42. The methods for identifying an agent effective to inhibit a tau protein may feature administering an agent; and observing either i) a reduction in biological activity of the tau protein or a biologically active fragment, derivative or analog thereof or ii) a reduction in phosphorylation of the tau protein or a biologically active fragment, derivative or analog thereof.
Owner:NEW YORK UNIVERSITY

Irak-1 as regulator of diseases and disorders

The present invention provides methods and compositions for treatment of diseases and disorders. More specifically, the invention for the first time shows a link between IRAK-1 and phosphorylation of proteins involved in cardiovascular disease, diabetes, neurodegeneration, and associated diseases and disorders and complications. Typically, the diseases and disorders involve an inflammatory component. Assays for bioactive substances affecting IRAK-1 regulated progression of inflammation and diseases and disorders involving inflammation are also disclosed.
Owner:VIRGINIA TECH INTPROP INC
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