84 results about "Kinase protein" patented technology

The application relates to the field of agricultural disease control technology, and particularly relates to the use of indole compounds and pharmaceutically acceptable salts, solvates, crystal forms, prodrugs, stereoisomers and tautomers thereof for preparing a medicine for inhibiting pathogenic key protein kinase CgSlt2 of pathogenic fungi. The application first proposes a new type of CgSlt2-targeted inhibitor, specifically, indole compounds ((S)-N-(1-(1H-indol-3-yl)-4-(methylamino)-4-oxobutan-2-yl)-8-bromo-1,6-naphthyridine-2-carboxamide) and ((S)-N-(2-((1H-indol-3-yl)-1-(methylamino)-1-oxopropyl)-8-bromo-1,6-naphthyridine-2-carboxamide) are used as CgSlt2 inhibitors, have the characteristics of high target specificity and high activity, and exhibit excellent pathogenicity inhibition of a strain of the complex group of Colletotrichum gloeosporioides.

This invention discloses compounds of Formula I, or pharmaceutically acceptable salts, isomers, racemates, precursors, or solvates thereof. Compounds of Formula I exhibit excellent inhibitory activity against RSK protein kinase, thus showing promise for development into drugs targeting RSK.

The application discloses a protein kinase gene positively regulating drought resistance of oats AVESA.00022b.r1.6C0001455 and application thereof, and belongs to the technical field of plant genetic engineering. AVESA.00022b.r1.6C0001455 The CDS sequence of the gene is shown as SEQ ID NO. 1, and the amino acid sequence is shown as SEQ ID NO. 2. Expression mode analysis shows that the gene is significantly induced and up-regulated under drought stress; virus-induced gene silencing verification shows that silencing the gene can significantly reduce the drought resistance of the oats; overexpression verification shows that overexpression of the gene can significantly enhance the drought resistance of the oats, and the performance is that wilting is delayed, the water loss rate is reduced, and the survival rate is improved. The application first proves that the gene is a key positive regulation factor of drought resistance in the oats, and can be used for cultivating drought-resistant transgenic plants and as a drought-resistant molecular marker for assisted breeding, and has important application value in genetic improvement of crop drought resistance.

The application belongs to the field of plant genetic engineering, and discloses a key gene for positively regulating salt stress and oxidation stress tolerance of rice OsHPCA1 . The gene (accession number: Os05g40770) encodes a receptor protein specifically sensing hydrogen peroxide, which is classified into the leucine repeat receptor-like kinase (LRR-RLKs) family, which is the largest subfamily in the receptor-like kinase (RLKs) family. OsHPCA1 In response to salt and oxidation stress signals, the rice salt and oxidation stress tolerance is positively regulated. OsHPCA1 The overexpression rice strain shows strong salt tolerance; and OsHPCA1 the knockout strain oshpca1 is more sensitive to salt stress. OsHPCA1 The leucine repeat receptor protein kinase OsHPCA1 encoded by the gene can positively regulate the activity of catalase C (CatC) in the rice body, enhance the H2O2 clearance efficiency under salt stress, and thus improve the salt tolerance of the rice. When OsHPCA1 overexpressed, the activity of CatC in the overexpression strain OsHPCA1 is significantly increased, the H2O2 clearance capacity is enhanced, and the salt tolerance and oxidation stress tolerance of the rice are improved.

Disclosed in the invention are a type of compounds having activity of activating 5′-adenosine monophosphate-activated protein kinase (AMPK), a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for reducing fatty acid synthesis, for inhibiting triglyceride and cholesterol synthesis, for preventing and / or treating obesity and type II diabetes, for preventing and / or treating tumor, for preventing and / or treating Parkinson's disease, for preventing and / or treating Alzheimer's disease or for prolonging the lifespan of mammals:

The present invention pertains to the treatment of diseases associated with a dysregulated immune response such as auto immune disorders, inflammatory diseases or pathological immune responses as adverse effects of medical treatments. In particular the invention provides a combined use of inhibitors of Receptor-interacting serine / threonine-protein kinase (RIPK1) and inhibitors of Inhibitor of κB (IκB) Kinase (IKK) in subjects suffering from such disorders. The invention provides such inhibitory compounds and their combinations for use in medical applications, as well as pharmaceutical compositions comprising the compounds of the invention.

Provided are methods for inserting a large gene / polynucleotide between about 4.5Kb and about 8Kb and lacking a selection marker into a target genomic position in a cell by delivering the gene / polynucleotide by two AAV vectors in the presence of a p53-binding protein 1 (53BP1) inhibitor and a DNA-dependent protein kinase catalytic subunit (DNA- PKcs) inhibitor. The disclosed methods improve large gene insertion by at least 10-fold and obviate the need for a selection marker in the vector design, thereby providing more room in the AAV vector for gene delivery.

The present disclosure is directed to compositions comprising POLQ inhibitor Compounds of Formula (I), methods of preparing the forgoing, combinations of the forgoing with DNA PK inhibitors as well as methods of use for said compositions.

The present disclosure is directed to DNA-PK inhibitors having the Formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate, prodrug, or tautomer thereof, methods of preparing the forgoing, and compositions thereof, as well as methods of use for the compounds of Formula (I), in combination with a DNA cutting agent.

Disclosed are compounds and pharmaceutically acceptable salts thereof that may be used in the treatment of subjects in need thereof. The compounds disclosed herein may be inhibitors of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR). Also disclosed are pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and methods of their preparation and use.

The present invention relates to a compound of formula (I) as inhibitors of calcium calmodulin dependent protein kinase 2 (CAMK2) for the treatment of for the treatment of heart failure, fibrosis, cardiomyopathies, atrial fibrillation, catecholaminergic polymeric ventricular tachycardia, heart block, cardiac arrhythmias, contraception, anxiety, post-traumatic stress disorder, hypertension, tachycardia, diabetes, allergy, and asthma.

The application discloses genetically engineered bacteria for producing alpha-ketoglutaric acid and application. The genetically engineered bacteria are obtained by weakening the expression of alpha-ketoglutaric acid dehydrogenase gene odhA, weakening the expression of glutamate transporter protein gene cg1434, weakening the expression of glutamate synthase key subunit gene gltB, weakening the expression of lactic acid dehydrogenase gene ldh, weakening the expression of glutamate dehydrogenase gene gdh, weakening the expression of serine / threonine protein kinase gene pknG, enhancing the expression of pyruvate carboxylase gene pyc, introducing and expressing glutamate oxidase gene lgox at the site of lactic acid dehydrogenase ldh gene, and enhancing the expression of strong catalase gene katA on the basis of a Corynebacterium glutamicum starting strain. The genetically engineered bacteria can efficiently produce alpha-ketoglutaric acid under the condition of limited ammonia culture, and have a good application prospect.

The present disclosure is directed to DNA-PK inhibitors having the Formula (I), (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, prodrug, or tautomer thereof, methods of preparing the foregoing, and compositions thereof, as well as methods of use for the compounds of Formula (I), in combination with a DNA cutting agent.

The present invention relates to polymorphs of a protein kinase Mek inhibitor benzothiazole compound, processes for their preparation, and their medical use.

This invention relates to the field of plant genetic engineering, and in particular to a method for increasing the total starch content and / or the proportion of amylose in plant tubers. This invention is the first to clone a 5'-AMP-activated protein kinase gene, named StPTST1, from the potato cultivar "Atlantic." Its full-length cDNA sequence is 840 bp, encoding a protein composed of 279 amino acids. Overexpression of StPTST1 in potatoes and tobacco increases the total starch content in the tubers, and also significantly increases the proportion of amylose. Using this invention, new plant varieties with specific starch qualities can be rapidly cultivated to meet diverse industrial processing and consumer demands.

The present invention relates to novel blood-brain barrier (BBB) ​​permeable substituted bicyclic derivatives capable of selectively inhibiting myosin light chain phosphate phosphorylation mediated by ROCK2 and / or Rho kinase, compositions comprising such derivatives, methods for preparing such derivatives and / or compositions, and methods for using such derivatives and / or compositions.

The invention disclosed herein relates generally to the field of recombinant production of a steviol glycoside, to the field of bioconversion of steviol into a steviol glycoside and to the field of bioconversion of a steviol glycoside into a further steviol glycoside. Particularly, the invention provides a process for recombinant production of a steviol glycoside, a process of bioconversion of steviol into a steviol glycoside, a process for bioconversion of a steviol glycoside into a further steviol glycoside and a composition comprising a steviol glycoside. More particularly, the invention relates to a microorganism that has a deficiency of a serine / threonine protein kinase and comprises a polynucleotide encoding a polypeptide having uridine diphosphate-dependent glucosyltransferase (UGT) activity.

This method and composition involves oral administration of a low dose of D-ribose to enhance adenosine monophosphate-activated protein kinase (AMPK) activity in both exercising and sedentary mammals, improve mitochondrial-related oxidative metabolic parameters, and thereby promote overall metabolic health in mammals.

The compounds and methods of the present disclosure exhibit induce Ucp1 transcription, enhance of mitochondrial respiration, activate protein kinase A, increase lipolysis, and increase p38 MAPK phosphorylation in cells, particularly brown adipocytes and white adipocytes. They also protect primary cardiomyocytes against hypertrophy induced by adrenergic agonists. Such compounds and methods are useful in the treatment and prevention of conditions such as obesity and associated complex metabolic, endocrine, and hemodynamic changes, as well as related conditions as dyslipidemias, cardiovascular disease, and type 2 diabetes.

The present invention relates to a population of small extracellular vesicles (sEVs) for use in the treatment of obesity in a subject in need thereof, wherein the sEVs comprise at least one polynucleotide encoding a D168A dominant negative AMP-activated protein kinase alpha 1 (AMPKa1-DN) mutant protein operably linked and under the control of a steroidogenic factor 1 (SF1) promoter, wherein the sEVs are engineered to transiently express in their outer membrane at least one fusion protein comprising the neurotrophic rabies virus (RVG) peptide fused to lysosome-associated membrane protein 2b. Said population is highly safe and effective, as the sEVs, when administered systematically, are capable of exerting their effect in the SF1 expressing neurons located in the ventromedial nucleus of the hypothalamus.

This invention discloses the application of verbascoside in the preparation of drugs for treating obesity and related metabolic disorders, relating to the field of biopharmaceuticals. The drug upregulates the expression of phosphorylated AMP-activated protein kinase α and carnitine palmitoyltransferase-1α, while downregulating the expression of sterol regulatory element-binding protein-1c, fatty acid synthase, and acetyl-CoA carboxylase. This application is the first systematic study of the comprehensive intervention effect of verbascoside on diet-induced obesity and related metabolic disorders. In an in vivo obese mouse model, it was demonstrated that verbascoside can significantly inhibit excessive weight gain induced by a high-fat diet, reduce fasting blood glucose and fasting insulin levels, improve dyslipidemia indicators including triglycerides, total cholesterol, non-esterified fatty acids, and low-density lipoprotein cholesterol, enhance insulin sensitivity, and alleviate macrovesicular steatosis and hepatocellular damage.

Provided is a composition comprising a polyglycolized glyceride and a compound having the following structure (I):or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the compound of structure (I), or a pharmaceutically acceptable salt thereof. Methods of making the same, and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated diseases, disorders or conditions are also disclosed.

The application discloses a corn mitogen-activated protein kinase kinase gene ZmMKK1 and application thereof, relates to the technical field of plant genetic engineering, and the nucleotide sequence of the gene ZmMKK1 is shown as SEQ ID NO. 1. The ZmMKK1 gene is transferred into Arabidopsis thaliana by a method of agrobacterium mediation, and the result shows that the heat resistance of the transgenic Arabidopsis thaliana is obviously improved by overexpressing the ZmMKK1 gene. The ZmMKK1 knockout corn mutant is subjected to heat treatment, and it is found that the heat resistance of the ZmMKK1 knockout corn mutant is obviously reduced, which indicates that the ZmMKK1 positively regulates the heat resistance of plants. The application will be helpful to improving the high-temperature stress resistance of plants, has important theoretical guiding significance for cultivating new crop varieties resistant to high temperature, and has great application value for agricultural production in China.

The present application relates to the technical field of plant genetic engineering, and specifically provides the role of protein kinase gene GmCIPK6 in regulating soybean salt tolerance. The GmCIPK6 gene is cloned from soybean, and the GmCIPK6 overexpression and CRISPR / Cas9 knockout transgenic soybean plants are obtained by Agrobacterium-mediated genetic transformation technology. The results show that under salt stress, the leaf damage degree of the overexpression plants is significantly lower than that of the wild type, while the damage degree of the knockout plants is significantly aggravated; at the same time, the activities of antioxidant enzymes CAT, POD and APX in the overexpression plants are significantly increased, while those in the knockout plants are significantly decreased. Transcriptome analysis shows that the differentially expressed genes are significantly enriched in the hydrogen peroxide catalytic pathway and the oxidative stress related pathway. The present application confirms that the GmCIPK6 gene positively regulates the salt tolerance of soybean by regulating the antioxidant enzyme system, and provides an effective gene resource for breeding new salt-tolerant soybean varieties.

The application belongs to the technical field of medicine, and particularly relates to application of acacetin or 6-hydroxyflavone in preparation of anti-angina pectoris drugs, and aims to solve the problems of adverse reactions such as blood pressure drop, reflex tachycardia and the like caused by non-selective vasodilation of existing anti-angina pectoris drugs, wherein the drug improves myocardial blood supply by selectively dilating coronary vessels of the heart, wherein acacetin dilates coronary vessels of the heart by inhibiting cardiac coronary vessel myosin light chain kinase and activating myosin light chain phosphatase, and 6-hydroxyflavone dilates coronary vessels of the heart by inhibiting protein kinase C and enhancing myosin light chain phosphatase activity; and the acacetin or 6-hydroxyflavone significantly reduces the symptoms of myocardial ischemia of rats caused by isopropyl adrenaline, improves characteristic ECG abnormal changes of angina pectoris, does not affect heart rate and systemic blood pressure, and is safer, thereby providing a potential drug selection for anti-angina pectoris treatment.

This invention belongs to the field of biotechnology, specifically relating to a complex peptide for enhancing animal immunity and its preparation method. The complex peptide is composed of InflamBlock-9 peptide and ImmunoEnhance-7 peptide in a mass ratio of 3:1. InflamBlock-9 peptide reduces the excessive secretion of pro-inflammatory factors IL-1β, IL-6, and TNF-α by targeting and inhibiting the key protein IκB kinase (IKK) in the NF-κB signaling pathway. ImmunoEnhance-7 peptide promotes the synthesis of immunoglobulins IgG, IgA, and apolipoprotein A1 (Apo-A1) by activating the JAK-STAT signaling pathway. The combined use of these two peptides significantly reduces the levels of IL-1β, IL-6, and SAA in cat serum under stress (P<0.05) and increases the levels of IL-10, IgG, and Apo-A1 (P<0.05 or P<0.10), effectively alleviating excessive inflammatory response and improving immunosuppression. The preparation method of this invention achieves efficient peptide preparation through a dual prokaryotic and eukaryotic expression system. The process is controllable and low-cost, making it suitable for the development of functional pet foods or health products.