701 results about "Kinase protein" patented technology

Methods and systems for inducing apoptosis of adipose cells are disclosed herein. In some embodiments, the method comprises identifying a target area comprising the adipose cells and injecting a therapeutic agent at the target area. Injecting the therapeutic agent can inhibit a protein kinase B (Akt) pathway of the adipose cell, induce a proinflammatory response of adipose cells at the target area, and / or initiate lipolysis / cell death of the adipose cells at the target area. In doing so, a volume of the adipose cells at the target area can be reduced.

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 disclosure relates to compounds that elicit degradation of proteins directed against the protooncogene tyrosine protein kinase receptor (RET), which may be a wild-type RET or a mutant form of RET, including compounds of formula (I), for use in the treatment of diseases and conditions mediated by said proteins. # imgabs0 #

Methods and systems for inducing apoptosis of adipose cells are disclosed herein. In some embodiments, the method comprises identifying a target area comprising the adipose cells and injecting a therapeutic agent at the target area. Injecting the therapeutic agent can inhibit a protein kinase B (Akt) pathway of the adipose cell, induce a proinflammatory response of adipose cells at the target area, and / or initiate lipolysis / cell death of the adipose cells at the target area. In doing so, a volume of the adipose cells at the target area can be reduced.

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.

The invention provides a synthetic anti-cancer lipopeptide and application thereof, and particularly provides a non-natural polypeptide comprising domains X1, X2 and X3, in which X1 is selected from C6-C20 fatty acid residues, X2 is selected from C6-C20 fatty acid residues, X3 is selected from C6-C20 fatty acid residues, and X3 is selected from C6-C20 fatty acid residues; x2 is selected from a fragment of a cell penetrating peptide (CPPs); x3 is selected from fragments of peptides that specifically bind to protein kinase 2 (CK2). Compared with the prior art, the polypeptide can more effectively inhibit CK2, has higher targeting property on RPS6 protein, has better tumor inhibition activity and anti-metastasis effect and higher safety, and can realize large-scale production.

The invention discloses a receptor-like protein kinase gene containing a Malectin-like structural domain and associated with the heat resistance character of cotton, and belongs to the field of biotechnology application. The invention provides a cDNA (complementary deoxyribonucleic acid) sequence (SEQ ID NO.1) and a genomic sequence (SEQ ID NO.2) of the gene in allotetraploid upland cotton, 456 upland cotton varieties can be divided into two haplotype promoters according to a heat-resistant character GWAS associated site A11: 20036111, the sequence of a CC heat-labile haplotype promoter is shown as SEQ ID NO.3, and the sequence of a TT heat-resistant haplotype promoter is shown as SEQ ID NO.4. The invention also provides a method for preparing the promoter. The gene provided by the invention is obtained by cotton variety re-sequencing and whole genome association analysis, and is significantly associated with the heat-resistant character of cotton, and two promoter haplotypes of the gene are utilized to distinguish heat-resistant and non-heat-resistant haplotypes. The gene has important research value and application prospect in improvement of the heat-resistant character of cotton and cultivation of new heat-resistant varieties of cotton.

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.

Methods and compositions for modulating repeat non-ATG protein (RAN protein) translation are provided. In some aspects, the disclosure provides methods of inhibiting RAN protein translation by contacting a cell with an effective amount of an inhibitor of eIF2 phosphorylation or an inhibitor of protein kinase R (PKR). In some embodiments, methods described by the disclosure are useful for treating diseases associated with RAN protein translation, such as certain neurodegenerative diseases.

The invention belongs to the technical field of plant heredity and genetic engineering, and particularly relates to a wheat saline-alkaline tolerant protein kinase gene TaCRCK and application thereof. Specifically, the invention discloses a wheat saline-alkaline tolerant protein kinase gene TaCRCK, and the nucleotide sequence of cDNA of the gene is as shown in SEQ ID NO. 1. The invention also discloses a plant expression vector containing the gene TaCRCK and application of the gene and the plant expression vector in cultivation of saline-alkali resistant plants. Tests prove that silent expression of the gene promotes the resistance of wheat to saline-alkaline stress, and the saline-alkaline tolerance of transgenic plants is obviously improved. The gene has a negative regulation effect on the salt and alkali tolerance of plants, provides a new tool and method for improving the salt tolerance of crops by using a genetic engineering means, and has important scientific significance and application prospects.

The invention relates to application of mitogen-activated protein kinase PiPmk1 in screening molecules for inhibiting formation of a phytophthora infestans infection structure. The invention finds that the molecular marker plays a key role in the development of a phytophthora infestans cyst bud tube and / or the formation of an infection structure, which indicates that the molecular marker has the potential of serving as a target for inhibiting phytophthora infestans infection, and a corresponding molecular screening method and a generative prediction model are further developed and utilized; rapid and accurate prediction and screening of phytophthora infestans infection inhibitory molecules are realized, the research and development period and cost are greatly shortened, and a new thought and a new method are provided for development of accurate targeted green pesticides.

The invention discloses injectable piezoelectric conductive hydrogel as well as a preparation method and application thereof, and the injectable piezoelectric conductive hydrogel is prepared by forming space coordination between piezoelectric nano-particles and conductive hydrogel through metal and a framework and uniformly fixing the piezoelectric nano-particles in the space structure of the conductive hydrogel. When the injectable piezoelectric conductive hydrogel is injected to the wound surface of a mouse wound, the hydrogel can be completely attached to the wound according to the irregular wound to form gel, and the gel is tightly attached to the wound. When a mouse moves, the piezoelectric nanoparticles are extruded to generate voltage and current, and the current is transmitted to the surface and wound of the hydrogel through the conductive hydrogel skeleton. Under the stimulation of micro-current, phosphorylation of phosphatidylinositol 3-kinase of fibroblasts is activated, then phosphorylation of protein kinase B is activated, migration and proliferation of the fibroblasts are induced, and wound healing is promoted.

The invention belongs to the technical field of biological medicines, and particularly discloses application of (E)-BCI hydrochloride in preparation of a medicine for treating sepsis. According to the application of the (E)-BCI hydrochloride in preparation of the medicine for treating sepsis, by inhibiting the activity of bispecific phosphatase 6, a mitogen activated protein kinase signal channel is regulated and controlled, and the expression level of inflammatory factors IL-1beta and TNF-alpha is reduced. The invention discloses application of (E)-BCI hydrochloride in preparation of drugs for treating sepsis, BCI enters from a new target for regulating inflammation and immune balance through a targeted DUSP6 / MAPK signal channel, a non-antibiotic-dependent drug is provided for treatment of sepsis, and the (E)-BCI hydrochloride is especially suitable for systemic inflammatory response syndromes caused by infection, operations, wounds and other inducements, and has a wide application prospect. Wide clinical application prospects are realized.

The invention belongs to the field of plant genetic engineering, and discloses a key gene OsHPCA1 for positively regulating salt stress and oxidative stress tolerance of rice. The gene (with the login number of Os05g40770) encodes a receptor protein capable of specifically sensing hydrogen peroxide, and belongs to a leucine repeat receptor-like protein kinase (LRR-RLKs) family, wherein the family is the largest subfamily in the receptor-like protein kinase (RLKs). The OsHPCA1 responds to salt and oxidative stress signals, and the salt tolerance and oxidative stress resistance of the rice are positively regulated and responded. The OsHPCA1 overexpression rice strain shows very strong salt tolerance; and the OsHPCA1 knockout strain oshpca1 is more sensitive to salt stress. The OsHPCA1 protein encoded by the OsHPCA1 gene and rich in leucine repeat receptor-like protein kinase can positively regulate and control the activity of catalase C (CatC) in rice and enhance the removal efficiency of H2O2 under salt stress, so that the salt tolerance of rice is improved. When the OsHPCA1 is overexpressed, the activity of CatC in the overexpressed strain OsHPCA1 is obviously increased, the H2O2 removal capability is enhanced, and the salt tolerance and oxidative stress tolerance of the rice are improved.

The present invention relates to compounds of formula (I) below, or any one of its pharmaceutically acceptable salts: [Formula 1] JPEG2023523788000127.jpg41170 where R 1 is (C1-C6) alkyl group, spiro (C5-C 11 ) bicyclic rings, fused phenyl groups, substituted phenyl groups, R'-L- groups, where L is either a single bond or a (C1-C3) alkanediyl group, and R' is a (C3-C8) cycloalkyl group, a bridged (C6-C 10 ) cycloalkyl group, (C3-C8) heterocycloalkyl group, or (C3-C8) heteroaryl group, or R'-L- group, where L is a (C1-C3) alkanediyl group and R' is an optionally substituted phenyl group, and R 2 represents a hydrogen atom or a (C1-C3) alkyl group. The present invention further relates to compositions comprising the compound of formula (I), as well as methods for preparing the compound and synthetic intermediates thereof. The present invention also relates to the compound for use as a pharmaceutical, in particular for treating and / or preventing cognitive impairment associated with Down's syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 deficiency disorders; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; folate and methionine metabolism disorders; osteoarthritis; Duchenne muscular dystrophy; some cancers; neuroinflammation, anemia, and viral and unicellular infections, and for regulating body temperature.

Disclosed are a series of isoquinolone derivatives as ROCK protein kinase inhibitors and uses thereof in preparing medicaments for ROCK protein kinase inhibitor-related glaucoma or ocular hypertension diseases. Specially, disclosed are a compound of formula (I), an isomer thereof or a pharmaceutically acceptable salt thereof.

The invention relates to RIP1 inhibiting compounds and methods of making and using the same. In particular, disclosed herein are kinase inhibitory compounds, such as receptor interacting protein-1 (RIP1) kinase inhibitor compounds, and pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions and / or combinations may be used to treat or prevent kinase-related diseases or disorders, particularly RIP1-related diseases or disorders.

The invention relates to the technical field of biological active peptides, in particular to a method for rapidly and effectively screening light protection active peptides from collagen hydrolysate. The invention relates to an application of a photoprotective polypeptide in preparation of a product. The product has at least one of the following purposes: (1) maintaining or increasing the water content of skin; (2) preventing and / or slowing down skin aging; (3) prevention and / or alleviation of skin UVB injury; and (4) promoting healing of skin wounds or wound surfaces. Two key signal factors (NF-kB, AP-1) and a key matrix metalloproteinase (MMP-9) are screened from a mitogen-activated protein kinase (MAPK) and nuclear factor-kB (NF-kB) pathway to be used as docking targets, and a mimic peptide and the three targets act synergistically to make up for the defect that a single target screening peptide is difficult to comprehensively cope with a light damage multivariate pathway, so that the application of the mimic peptide to the light damage multivariate pathway is realized, and the application of the mimic peptide to the light damage multivariate pathway is realized. And the collagen peptide with excellent light protection activity is obtained through screening.

The invention relates to compounds of formula (I) which are inhibitors of MKK4 (mitogen-activated protein kinase kinase 4) and their use in promoting liver regeneration or reducing or preventing hepatocyte death. The compounds selectively inhibit protein kinase MKK4 over protein kinases JNK1 and MKK7. In formula (I), especially, Rw is —NR10SO2R12; either a) Rx and Ry are F and Rz and Rzz are H; or b) Rx, Ry and Rzz are independently halogen and Rz is H; R5 is substituted phenyl or pyrimidinyl.

The invention relates to polymorphic substances of a benzothiazole compound as a protein kinase Mek inhibitor, and a preparation method and medical application of the polymorphic substances.

The present disclosure relates to inhibitors of Rho-associated protein kinase (ROCK), pharmaceutical compositions comprising said inhibitors and their use for the prevention or treatment of diseases mediated by said ROCK. In particular, the inhibitor of ROCK has selectivity for inhibition of ROCK2.

The present invention relates to compounds having cyclin-dependent kinase (CDK)-inhibitory functions and / or pharmaceutically acceptable salts thereof, the use of these compounds as pharmaceutically active agents, especially for the prophylaxis and / or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing such compounds.

The present invention relates to an N-containing heteroaryl derivative and a pharmaceutical composition comprising same as an active ingredient for the prevention or treatment of cancer. The derivative exhibits high inhibitory activity against various protein kinases, particularly excellent ret proto-oncogene (RET) enzyme inhibitory ability, and has an excellent effect of inhibiting the proliferation of medullary thyroid cancer cells and lung cancer cells, which express RET fusion genes, and thus the derivative can be effectively used in the treatment of cancer, for example, medullary thyroid cancer or lung cancer, and particularly, can be effectively used in the treatment of cancer in which RET fusion genes are expressed.

This invention relates to novel compounds and pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as modulators of Rho-associated protein kinase (ROCK), for example ROCK1 and / or ROCK2 inhibitors. This invention also relates to processes for preparing the compounds, uses of the compounds and methods of treatment employing the compounds. The compounds of the invention may therefore be used in treating ROCK-mediated diseases.

The invention discloses an application of a GhMKK5 gene in improving the disease resistance of cotton verticillium wilt, and belongs to the field of biotechnology application. The GhMKK5 gene disclosed by the invention is used for coding a mitogen activated protein kinase kinase. The invention provides a full-length CDS nucleotide sequence and an amino acid sequence of GhMKK5 in an upland cotton genetic standard line TM-1. The gene is expressed in all tissues of cotton, and is induced by verticillium dahliae to realize obvious up-regulation expression. The verticillium wilt resistance of cotton is reduced by silencing the gene in cotton, and the disease resistance of arabidopsis thaliana is improved by overexpressing the gene in arabidopsis thaliana, which indicates that the gene plays an important role in cotton verticillium wilt resistance.

The disclosure relates to compositions and methods for modulating, e.g., reducing or eliminating, the expression of mutated DMPK via delivery using an adeno-associated viral (AAV) capsid variant. The compositions and methods of the present disclosure are useful in the treatment of subjects diagnosed with, suspected of having, or having myotonic dystrophy type 1 or another DMPK-related disorder or at least one symptom thereof.

This invention provides rho-associated protein kinase (ROCK) inhibiting compounds for therapeutic applications as described further herein.

The invention belongs to the technical field of plant genetic engineering, and particularly discloses application of an important member of a potato mitogen-activated protein kinase (MAPK) family, namely an StMKK9 gene in regulation and control of maturity and cold resistance of potatoes. CDNA of a cultivar Desiree leaf is used as a template, the potato StMKK9 gene is separated and cloned, an over-expression vector is constructed, and the over-expression vector is used for expression of the potato. Genetic transformation of the potatoes is further carried out, it is found that the overexpressed StMKK9 gene can promote prematurity of the potatoes, meanwhile, the cold resistance of potato plants can be improved, and a new genetic material and a theoretical basis are provided for analysis of a potato tuberization molecular mechanism and improved breeding of the potatoes.

A method and composition for enhancing adenosine monophosphate-activated protein kinase (AMPK) activity and improving mitochondrial-related oxidative metabolism parameters in motor and sedentary mammals by oral intake of low doses of D-ribose, thereby promoting overall metabolic health in mammals.