307 results about "Enzyme inhibitor" patented technology

The invention discloses a preparation method of deer spleen aminopeptide powder in the field of bioactive substance extraction and functional material compositing, and the performance of the deer spleen aminopeptide powder is improved by compositing a multi-stage functional modified material and deer spleen aminopeptide. The preparation method comprises the following steps: cleaning, homogenizing and crushing fresh deer spleen, extracting with a phosphate buffer solution, adjusting the pH value, carrying out enzymolysis, inactivating enzyme, and treating with an ultrafiltration membrane and a nanofiltration membrane in a specific molecular weight range to obtain a concentrated solution; and mixing the concentrated solution with a multi-stage functional modified material under proper conditions, sterilizing, pre-freezing, and freeze-drying to obtain the deer spleen aminopeptide powder. Wherein the modified material is constructed through quaternization modification, nanopore loading, enzyme inhibitor coupling and targeting ligand modification, and has the functions of charge repulsion, steric hindrance, enzyme inhibition and targeting recognition. The deer spleen aminopeptide powder prepared by the invention has high stability and good bioavailability, and is suitable for functional food or health care products.

The present invention belongs to the technical field of genetic engineering. Provided are a single-base editor, a deaminase used therein, and the use thereof. The technical problems to be solved are to identify a naturally occurring cytosine deaminase without sequence preference, construct a base editor, and improve the efficiency and scope of base editing. In order to solve the technical problems above, a cytosine base editor is provided. The cytosine base editor is a fusion protein, wherein the fusion protein is a protein containing a cytidine deaminase, a Cas protein and a uracil-DNA glycosylase inhibitor, and the cytidine deaminase is a protein having an amino acid sequence of positions 28-164 of SEQ ID NO. 2. Further provided is the use of the fusion protein above and a biomaterial related thereto in plant single-base editing. The single-base editor can improve the efficiency of cytosine base editing and accurately mediate the base mutation of a target, and is widely applicable in the cells of maize and even other plants.

The invention provides a method for detecting an anti-C1 esterase inhibitor neutralizing antibody in a biological sample, and the method mainly utilizes the characteristic that protein A resin is combined with an Fc segment of the antibody to capture the antibody (containing the anti-C1 esterase inhibitor neutralizing antibody), so that the C1 esterase inhibitor and complement component 1s (C1s) in the biological sample after thermal inactivation are removed; furthermore, an antibody (containing a neutralizing antibody) or an anti-C1 esterase inhibitor compound on the protein A resin is subjected to acid dissociation through an acidolysis solution, so that not only can the anti-C1 esterase inhibitor neutralizing antibody existing in a free form in a biological sample be detected, but also the anti-C1 esterase inhibitor neutralizing antibody existing in a combined form in the biological sample can be detected.

The invention provides a compound serving as a glutamine cyclase inhibitor and application of the compound, and belongs to the field of medical chemistry. The structure of the compound is shown as a formula I. The compounds have good inhibitory activity on sQC and gQC enzymes and mutants thereof, and the half inhibitory concentration of most compounds reaches the sodium mole level, so that the compounds can be used for preparing glutamine cyclase inhibitors. In addition, the compounds can also be used for preparing medicines for preventing and treating diseases related to glutamine cyclase. The invention lays a material basis for research and development of glutamine cyclase inhibitor drugs, and has a good application prospect. Formula I.

This invention relates to a 1,3,4-thiadiazole peptide deformylase inhibitor and its preparation and application. The structural formula is shown in formula (1): wherein, R 1 It is n-butyl or cyclopentylmethyl; R 2 The compounds are hydrogen-containing, straight-chain alkanes, cyclic alkanes, aromatic rings, substituted biphenyls, or heterocyclic rings. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention can effectively inhibit bacterial protein synthesis, thereby achieving sterilization. These compounds exhibit excellent inhibitory activity against Gram-positive drug-resistant bacteria, especially the clinically challenging methicillin-resistant Staphylococcus aureus (MRSA). In particular, some preferred compounds show inhibitory activity 4-8 times that of the control standards vancomycin and linezolid. The 1,3,4-thiadiazole peptide deformylase inhibitors provided by this invention also exhibit inhibitory activity against Gram-negative drug-resistant bacteria, especially against drug-resistant Acinetobacter baumannii, known as "superbugs," with an inhibitory activity reaching 0.5 μg / mL, far superior to vancomycin and linezolid.

The invention relates to a method for producing particles comprising urea and at least one urease inhibitor and / or at least one nitrification inhibitor, and to a suitable apparatus for carrying out the method.

The present application relates to "application of a compound in soybean cyst nematode chitinase inhibitor", belong to the technical field of leguminous plant symbiotic protection, the application of the compound and its pharmaceutically acceptable salt in soybean cyst nematode chitinase inhibitor, the present application is evaluated and researched through the inhibitory activity of compound by screening work, the inhibitor is screened finally, the inhibitor is likely to have good application prospect in controlling soybean cyst nematode disease aspect.The present application also provides a kind of chitinase inhibitor with the function of inhibiting the establishment of symbiosis of soybean cyst nematode to destroy, the number of nodule obtained by processing is flat with the number when only inoculating rhizobium, the inhibitory effect of Hg-CHI-1 on rhizobium nodule is completely restored, and it has good application prospect in the aspect of leguminous plant symbiotic protection.

Disclosed herein is a method of modifying a T cell during T cell activation comprising contacting the T cell with an inhibitor of prolyl hydroxylase. Also disclosed is a method of producing a chimeric antigen receptor (CAR) or T cell receptor (TCR) T cell comprising (i) modifying the T cell during activation of the T cell by contacting the T cell with an inhibitor of prolyl hydroxylase, (i) introducing a CAR or TCR transgene into the modified T cell, and (iii) harvesting the CAR or TCR T cell. In particular, the inhibitor of prolyl hydroxylase is a small molecule prolyl hydroxylase inhibitor, such as 1, 4-DPCA. The harvested CAR or TCR T cells can be used for adoptive T cell immunotherapy of cancer.

The invention discloses a semeglutide capsule and a preparation method thereof.The semeglutide capsule comprises a pill core, a coating layer and a capsule shell, the pill core is coated with the coating layer, the capsule shell is filled with the pill core coated with the coating layer, and the total mass percentage of the pill core and the coating layer is 100%. The pellet core is prepared from the following components in percentage by weight: 0.43 to 0.85 percent of semeglutide, 19.94 to 37.04 percent of an absorption enhancer, 4.84 to 8.26 percent of an enzyme inhibitor, 14.25 to 22.79 percent of an adhesive, 19.66 to 44.01 percent of a shaping agent and 2.85 to 4.56 percent of an adhesive; and the coating layer comprises the following components in percentage by weight: 7.41 to 10.83 percent of a film forming agent, 0.28 to 0.57 percent of a plasticizer and 0.56 to 1.14 percent of an emulsifying agent. The capsule disclosed by the invention can target colon, and does not need fasting before and after taking medicine, so that the bioavailability of the semeglutide is greatly improved, and the production cost of the preparation is reduced.

The present invention relates to a novel crystalline form of a helicase-primase inhibitor compound, and to pharmaceutical compositions comprising the novel crystalline form, to methods of production of the novel crystalline form, to the crystalline form in medicine and for use in the treatment of herpes viral infections.

The invention discloses a tea yellow liquid as well as a preparation method and application thereof, and belongs to the field of agricultural additives. The preparation process of the tea yellow liquid comprises the following steps: drying and crushing raw materials, adding water for dissolving out, centrifuging to obtain a mixed fine suspension, finally adding an enzyme inhibitor, and carrying out secondary sanding and dilution to obtain the tea yellow liquid. The tea yellow liquid is prepared from, by mass, 7-99.5% of tea saponin liquid, 0.5-93% of coptis chinensis liquid and the balance water, tea saponin active ingredients contained in the tea saponin liquid can remarkably reduce the surface tension of pesticide liquid, the tea saponin active ingredients cooperate with macromolecular substances such as polysaccharide in the coptis chinensis liquid to form a biomass affinity film, the spreadability and adsorbability of the pesticide liquid are greatly improved, and the pesticide effect is improved. Therefore, the content of the pesticide liquid in unit area is increased, the application amount of the pesticide is greatly reduced, and pesticide residues caused by excessive application are reduced.

This application relates to a method, apparatus, computer device, and storage medium for identifying enzyme substrates. The method for identifying enzyme substrates analyzes the sequence information of substrate peptides before and after enzyme digestion by quantitative detection of control samples and enzyme inhibitor-treated samples, thereby identifying potential enzyme substrates. It effectively identifies enzyme cleavage sites, detects the sequences of substrate peptides before and after enzyme digestion, and promotes enzyme substrate identification and site analysis. This plays an important role in understanding biological processes and identifying biomarkers for diseases.

The present disclosure provides methods, pharmaceutical compositions, and kits for treating cancer in patients in need thereof. The methods comprise administering to a patient in need a small ubiquitin-like modifier (SUMO) activating enzyme (SAE) inhibitor, such as [(1R,2S,4R)-4-{[5-({4-[(1R)-7-chloro-1,2,3,4-tetrahydroisoquinolin-1-yl]-5-methyl-2-thienyl}carbonyl)pyrimidin-4-yl]amino}-2-hydroxy-cyclopentyl]methyl sulfamate (Compound I-263a) or a pharmaceutically acceptable salt, in combination with one or more anti-CD19 antibodies. Also provided are medicaments for use in treating cancer.

In certain aspects, the disclosure relates to mobilized colistin resistance (MCR) enzyme (MCR-1) inhibitors, pharmaceutical compositions thereof, and methods of use thereof for treating, preventing, and / or ameliorating bacterial infections and / or sensitizing bacteria to polymyxin antibiotics.

The invention discloses a kit and a method for preparing cDNA (complementary deoxyribonucleic acid) by reverse recording of a single B cell of a mouse. The kit comprises a B cell lysis solution and a reverse transcription buffer solution system, wherein the B cell lysis solution is prepared from a nonionic detergent, dNTP (deoxyribonucleoside triphosphate), dCTP (deoxycytidine triphosphate), a secondary structure stabilizer, a reducing agent, BioIS-mCH2-RT (reverse transcriptase), BioIS-CK-RT, a mouse RNA (Ribonucleic Acid) enzyme inhibitor and nuclease-free water; the reverse transcription buffer solution system comprises 5X RT Buffer, a secondary structure stabilizer, Mg < 2 + >, a reducing agent, a mouse RNA enzyme inhibitor, a Bio-Adaptor primer, reverse transcriptase and nuclease-free water. The kit can significantly improve the success rate, accuracy and sensitivity of reverse transcription of a single B cell, and simplify the operation process.

Provided are methods of treating spinal muscular atrophy (SMA) using a combination of a 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitor and an agent that increases motor neuron survival (SMN) protein expression. Furthermore, provided herein is a composition, a pharmaceutical formulation, or a kit comprising a 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitor and an agent that increases the expression of a motor neuron survival (SMN) protein.

This invention provides a ternary herbicidal composition containing an ALS enzyme inhibitor and its application. The herbicide composition comprises three active ingredients: active ingredient A is pyrimisulfuron and its salt; active ingredient B is quinclorac acid and its salt; and active ingredient C is selected from one of clopyralid, triclopyralid, clopyralidic acid, fluorochloropyralidic acid and its salts and esters. The weight ratio of each active ingredient is 1:(1-50):(1-50), and the total weight percentage of the active ingredients in the herbicidal composition is 1-80%. This ternary herbicidal composition can be used to control various grass weeds, broadleaf weeds, and sedge weeds in warm-season lawns. It has a significant synergistic effect compared to single-component herbicides, improving control efficacy, especially against pyrimisulfuron-methyl weeds. Furthermore, it also has good control efficacy against older weeds, with a long-lasting effect and high safety.

The invention relates to the technical field of medicinal chemistry, in particular to salt of a dihydroorotate dehydrogenase inhibitor as well as a preparation method and application of the salt. The salt of the dihydroorotate dehydrogenase inhibitor is a salt of a compound as shown in a formula (I), the salt is sulfate or hydrochloride. Compared with the compound shown in the formula (I), the salt of the compound shown in the formula (I) has better solubility and bioavailability, and has excellent stability.

The invention belongs to the technical field of medicines, and particularly relates to pyrrolo [2, 3-d] pyrimidine compounds of aryl fragments and piperidine fragments as well as a preparation method and application of the pyrrolo [2, 3-d] pyrimidine compounds. The pyrrolo [2, 3-d] pyrimidine compound containing the aryl fragment and the piperidine fragment is an HIV-1 reverse transcriptase inhibitor, and the pyrrolo [2, 3-d] pyrimidine compound further comprises pharmaceutical salt, hydrate and solvate of the pyrrolo [2, 3-d] pyrimidine compound, polycrystal or eutectic of the pyrrolo [2, 3-d] pyrimidine compound, and precursors and derivatives with the same biological functions of the pyrrolo [2, 3-d] pyrimidine compound. The invention also relates to a preparation method of the compound and application of a composition containing one or more of the compounds in related medicines for treating AIDS and the like. The result of an in-vitro cellular level anti-HIV-1 activity experiment shows that the micromolecule has relatively strong anti-HIV-1 biological activity, can remarkably inhibit virus replication in MT-4 cells infected by HIV-1 viruses, and has relatively low cytotoxicity.

The invention provides a compound for preparing an MBL and / or SBL enzyme inhibitor, application of the compound and a medicine of the compound, and belongs to the field of medicine. The structure of the compound is shown as a formula I. The compound provided by the invention has good and broad-spectrum inhibitory activity on clinically common metal beta lactamase (MBL) and serine beta lactamase (SBL), can be used as an MBL and / or SBL enzyme inhibitor, and is used for preparing antibacterial drugs, especially drugs for resisting drug-resistant bacteria. In addition, the compound disclosed by the invention is combined with beta-lactam antibiotic meropenem and the like for use, so that the compound has relatively good antibacterial activity on various beta-lactam antibiotic drug-resistant bacteria. The compound disclosed by the invention has great potential in preparation of MBL and SBL dual broad-spectrum inhibitors and medicines for resisting beta-lactam antibiotic-resistant bacteria. The invention provides a new choice for the use of antibacterial drugs, and has a good application prospect.

The disclosure relates to pharmaceutical formulations and method of using chymase inhibitors for the prevention and treatment of mast cell-related disease states in which chymase is involved. More particularly the present disclosure is in the field of treating or preventing or reducing the symptoms of mast cell-related diseases, including atopic dermatitis (AD), chronic urticaria (CU), Eosinophilic Gastrointestinal Disorders (EGIDs), and prurigo nodularis (PN), using a chymase inhibitor, including a chymase inhibitor that prevents cleavage of stem cell factor (SCF) and its interaction with receptor tyrosine kinase (c-kit), thereby reducing mast cell activation and proliferation.

The invention provides a composition, cell culture and application of the composition in differentiation of human pluripotent stem cells to myocardial cells and / or construction of human-derived heart organoid, and belongs to the technical field of cell engineering. The invention provides a composition. The composition comprises a fatty acid receptor antagonist, a fatty acid synthetase inhibitor and a fatty acid oxidation activator. The composition provided by the invention can regulate cell metabolism, breaks through the contradiction that the proliferation capacity and the cell maturity cannot be obtained at the same time in the traditional technology, can maintain the myocardial cells in a proliferation stage, and obtains the myocardial cells with relatively mature structures and functions, and the contractility of 3D heart organs constructed by the myocardial cells is greatly improved. The invention provides a high-quality cell source for myocardial regeneration treatment, high-throughput drug cardiotoxicity screening and heart disease mechanism research, and has remarkable clinical application value and industrialization prospect.

The present application discloses a FabI enzyme inhibitor and use thereof. The FabI enzyme inhibitor is a compound as represented by Formula I, provides a new option for clinical screening and / or preparation of drugs for the treatment of diseases associated with FabI enzyme activity.

The invention belongs to the technical field of biology, and particularly relates to a method for determining the activity of an RNA enzyme inhibitor. According to the method, a DNA-RNA hybrid chain is used as a substrate for determining the activity of the RNA enzyme inhibitor (preferably the enzyme activity of the RNA enzyme inhibitor), and the cost of the method is far lower than that of a substrate cCMP of a traditional activity (enzyme activity) unit detection method (cyclic monophosphate (CMP) detection method).

The present invention relates to methods and compositions for the treatment of autoimmune diseases and of excessive hair shedding or hair loss in a subject or for promoting hair growth in a subject wherein the subject has an autoimmune hair loss disorder, such as alopecia areata. The methods and compositions comprise the administration of a janus kinase inhibitor, such as tofacitinib, wherein the inhibitor is predominantly absorbed through the oral mucosal routes such as the sublingual mucosa.

Provided herein are compounds that inhibit glucosylceramide synthase (GCS). Also provided are pharmaceutical compositions comprising the compounds, and methods of treating diseases and disorders associated with GCS activity, such as lysosomal storage disorders.

The present invention relates to isoquinolines as HPK1 inhibitors. Isoquinoline compounds and their use as HPK1 (hematopoietic kinase 1) inhibitors are described. The compounds are useful in treating HPK1 dependent disorders and in enhancing immune responses. Methods of inhibiting HPK1, methods of treating HPK1 dependent disorders, methods for enhancing immune responses, and methods for making the isoquinoline compounds are also described.

The invention discloses a method for extracting cell nucleuses from animal tissues, and relates to the technical field of biology. The background technology indicates that cell nucleus extraction is crucial to multidisciplinary research, but a traditional method has the problems of complex operation, time consumption, low purity, easiness in damaging cell nucleuses and the like, and the prior art is still limited although the prior art is improved. The method comprises the following steps: preparing a sample, and taking fresh or cryopreserved animal tissues; homogenizing the tissues, namely putting the tissues into a homogenizer, and homogenizing at a low speed by adding a cracking buffer solution; carrying out cell lysis, and incubating homogenate on ice; centrifugally separating, centrifuging at low temperature and medium speed, taking precipitate, and discarding supernatant; core washing, re-suspending the precipitate in a washing buffer solution, uniformly mixing and filtering; performing core extraction, re-suspending the precipitate in a suspension buffer solution, and lightly and uniformly mixing; purifying and washing, carrying out density gradient centrifugation on the suspension, dyeing with trypan blue, taking a core layer, and washing for subsequent experiments. The nuclear extraction lysis buffer solution has two proportions of LB1 and LB2, different tissues are suitable for different proportions, and an enzyme inhibitor can be added as required. The method can be used for rapidly extracting various animal tissue cell nucleuses, is complete in shape, large in quantity and few in impurities, is suitable for different tissues, and can be applied to downstream experiments such as single cell nucleus sequencing.

The invention belongs to the technical field of breeding of aquatic animals, and particularly relates to a breeding method for breeding XX pseudo male fishes by using Chrysophila multistriata. The invention relates to a breeding method for breeding XX pseudo-male fishes by using Christia polyrrhiza, which comprises the following steps of: feeding a feed containing an aromatase inhibitor to Christia polyrrhiza fry with proper day age for induction to obtain pseudo-male fishes with physiological male property and genetic female property; the method comprises the following steps: performing PIT living body electronic marking, then collecting a tail fin tissue sample, performing PCR detection by utilizing a genetic sex specific molecular marker of the Chrysophila polyrrhiza, and screening out pseudo male individuals with female genetic sex and male physiological sex; the obtained pseudo male fish individuals serve as male parents, normal genetic female fishes serve as female parents, intensive cultivation and artificial spawning induction are conducted, and fertilized eggs are obtained; the obtained fertilized eggs are collected and hatched, and pseudo male fishes with all genotypes being XX are obtained. According to the method, the genetic all-female rate of the breeding offspring reaches 100%, and the production purity of the offspring seeds is greatly improved.

The application discloses a small molecule peptide AGGINLAR, and an amino acid sequence of the small molecule peptide is shown as SEQ ID NO. 3. The small molecule peptide is applied to preparation of a xanthine oxidase inhibitor and preparation of a drug for treating or preventing hyperuricemia. Through experimental research, six small molecule peptides with xanthine oxidase inhibiting activity are screened from enzymatic hydrolysate of Penaeus vannamei, and the small molecule peptides have the potential of serving as xanthine oxidase inhibitors, wherein AGGINLAR shows higher xanthine oxidase inhibiting activity, and has greater potential value in preventing hyperuricemia.