30 results about "Synthetase kinase" patented technology

The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

The invention discloses a high-efficiency non-integrated human iPSC induction platform which comprises a composition, wherein the composition is used for inducing a human cell into iPSC, and the composition comprises a previous inducer and a later inducer; the previous inducer comprises the following active components: a transforming growth factor beta inhibitor, a glycogen synthetase kinase 3 inhibitor, a cAMP agonist, an S-adenosyl homocysteine hydrolase inhibitor and a p21 activated kinase inhibitor; and the later inducer comprises the following active components: the glycogen synthetase kinase 3 inhibitor, a selective ATP noncompetitive MEK inhibitor and the S-adenosyl homocysteine hydrolase inhibitor. The high-efficiency non-integrated human iPSC induction platform disclosed by the invention achieves the previous induction efficiency of the iPSC of 6.4% under the action of a previous inducer composition, can achieve the induction of a full culture of 20.8% through later induction culture or be used for totally further inducing a previous inductor clone into a human iPSC clone approaching to ESC and is far higher than the prior art in induction efficiency; in addition, the obtained iPSC is high in maturity, free of being inserted with an exogenous gene, is more approaching to the ESC in cell morphology and property and has the advantages of good stability and great high application value.

The invention relates to 3,4-dihydrobenzo[f][1,4]thiazepine compound of the general formula I or salts of the same and medicinal use of the same, belonging to the field of pharmaceutical chemistry. The 3,4-dihydrobenzo[f][1,4]thiazepine compound can inhibit glycogen synthase kinase-3beta (GSK-3beta) and be used as the non-ATP competitive micromolecular inhibitor of the GSK-3beta to prepare medicaments used for preventing or treating diseases related to the GSK-3beta. The invention further discloses the application of a medical combination formed by the compound and pharmaceutically acceptablesalts of the same to preparation of medicaments for preventing or treating the diseases related to the GSK-3beta, such as diabetes, Alzheimer's diseases and tumors.

The invention discloses a culture method of vascular endothelial progenitor cells, which comprises the following steps: 1) inducing differentiation of multipotent stem cells in a culture medium A to form mesendoderm precursor cells; and 2) inducing differentiation of the mesendoderm precursor cells in a culture medium B to form the vascular endothelial progenitor cells. The culture medium A contains a DMEM (dulbecco's modified eagle medium) culture medium, an F12 culture medium, sodium selenate, sodium bicarbonate, vitamin C, insulin, activin A, a bone formation protein 4 and a glycogen synthetase kinase-3 inhibitor. The culture medium B contains a DMEM culture medium, an F12 culture medium, vitamin C, insulin, a vascular endothelial growth factor and a transforming growth factor beta signal pathway inhibitor. The culture media used in the culture method do not contain any animal-derived component, and can provide sufficient nutrient substances and stable living environments for the cultured cells, thereby efficiently inducing the differentiation of the human multipotent stem cells to form the vascular-grid vascular endothelial progenitor cells which are highly similar to the human cord vessel endothelial cells.

The present invention relates to a wheat glycogen synthetase kinase gene obtained by utilizing cDNA-AFLP technique to clone the salt-stressed specific expression fragment of wheat salt-tolerant mutant, adopting sequence determinatio Blast identification and RACE method. The total length of said gene is 1573bp, in which its open reading frame (ORF) contains 1143 bp, coding 381 amino acids, its coded protein extensively participates in plant response reaction to drought, ABA induction and light induction, specially participates in salt-stressed signal conduction process. After said gene is cloned into prokaryotic expression vector, it can express out a prokaryotic expression product whose molecular weight is 43.6 KD in the colibacillus, i.e. glycogen synthetase kinase protein. Said invention also provides its application field.

The present invention relates to a new compound of formula I as a free base or a pharmaceutically acceptable salt thereof, a process for the preparation, pharmaceutical formulations containing said therapeutically active compound and to the use of said compound in therapy.

The present invention relates to novel heterocyclic compounds of formula I

wherein the variables are as defined in the claims or the description,

which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3β, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3β activity using the compounds.

The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

The invention discloses a synthesis technology of a glycogen synthase kinase-3 inhibitor for treating plasmodium falciparum causing malaria. The synthesis method has the advantages of simple operationand short production period, and can massively prepare the glycogen synthase kinase-3 inhibitor, namely 3-amino-4-(2-chloromethyl)-6,7-dihydro-5H-cyclopentene[b]thieno[3,2-e]pyridine-2-ylphenyl ketone.

A pharmaceutical composition for preventing or treating ovary granulosa cell tumors containing, as an active ingredient, one selected from the group consisting of a compound represented by chemical formula 1, a pharmaceutically acceptable salt of the compound represented by chemical formula 1, a compound represented by chemical formula 2, and a pharmaceutically acceptable salt of the compound represented by chemical formula 2, or a functional health food composition. The composition inhibits glycogen synthase kinase-3 beta (GSK3beta) and thus has an effect of inhibiting a phosphorylation of a serine, which is the 33rd amino acid of the forkhead box L2 (FOXL2) protein.

The invention relates to the technical field of genetic engineering, and discloses a polypeptide for inhibiting glycogen synthase kinase-3[beta] acetylation, and a coding gene of polypeptide and application of polypeptide and coding gene. The sequence of the polypeptide is shown as SEQ.ID.NO:1. The polypeptide for inhibiting glycogen synthase kinase-3[beta] acetylation can block the combination of tau protein and glycogen synthase kinase-3[beta] in the whole level of cells and animals, and can block the acetylation and activation effects of the tau protein on the glycogen synthase kinase-3[beta]; and the morphology and function of cells are improved, and the learning and memory ability of mice is improved. The polypeptide provided by the invention can play a role in preventing and treating glycogen synthase kinase-3[beta] activation related diseases such as Alzheimer's disease and the like.

The invention relates to the field of medicines, and discloses a group of biomarkers and a kit for predicting MCI risk of type 2 diabetes patients and application thereof. The biomarkers comprise optic nerve protein, glycogen synthase kinase-3beta and Ser9-phosphorylated glycogen synthase kinase-3beta. The rise of the biomarkers can evaluate MCI, and the biomarkers have the characteristics of high accuracy, high detection speed, low cost, small trauma and easy acceptance by patients, and provide a scientific and effective early prediction scheme for MCI of type 2 diabetes patients. The kit can be used for screening MCI in a large range of people, and detection can be completed only by collecting peripheral blood, so that large-range elderly population screening becomes possible.

The invention relates to an Atriplex canescens glycogen synthetase kinase gene clone and its application, and belongs to the technical field of plant gene engineering. A plant resistance related protein AcGSK3 is a protein composed of an amino acid sequence represented by SEQ ID NO:2 in a sequence table; and the coding sequence of the coding gene AcGSK3 of the plant resistance related protein AcGSK3 is one of a coding sequence with the nucleotide sequence represented by 346-684th deoxynucleotides at 5'-terminal of an amino acid sequence represented by SEQ ID NO:1 in the sequence table, and a nucleotide molecule for coding the protein sequence of the SEQ ID NO:2 in the sequence table. The invention also relates to a recombinant expression vector containing the coding gene AcGSK3 of the plant resistance related protein AcGSK3, and a recombinant bacterium containing the coding gene AcGSK3 of the plant resistance related protein AcGSK3. A result of qRT-PCR detection of the original plant Atriplex canescens shows that the gene improves the expression under NaCl and PEG stress. AcGSK3 is introduced into Saccharomyces cerevisiae to obtain transgenic Saccharomyces cerevisiae, and stress treatment is carried out, so the result shows that the AcGSK3 can improve the drought (sorbitol) and salt (NaCl) resistance of yeast.