1027 results about "Enzyme inhibitor" patented technology

In a small molecule drug discovery method, a transition state for a specific enzyme is modelled using quantum mechanics and molecular dynamics based simulation of the enzyme and substrate reaction; data defining the transition state (a ‘quantum pharmacophore’) is fed to a machine learning engine configured to generate transition state analogues, such as enzyme inhibitors.

The invention provides an application of N-trans-p-coumaroyl tyramine or a derivative thereof in preparation of a skin whitening product, and relates to the technical field of biology, and the application of the N-trans-p-coumaroyl tyramine or the derivative thereof in preparation of cosmetics for skin whitening or drugs for skin whitening is as follows: (I) the N-trans-p-coumaroyl tyramine or the derivative thereof is applied to preparation of cosmetics for skin whitening or drugs for skin whitening; (2) inhibiting melanogenesis in a non-diagnostic and therapeutic manner; (3) preparing a melanin inhibitor; (IV) inhibiting the tyrosinase activity of the subject in a non-diagnostic and therapeutic manner; or (V) preparing the tyrosinase inhibitor. According to the invention, a natural compound N-trans-p-coumaroyl tyramine which is derived from a traditional Chinese medicine and has a whitening effect is found, and a new functional component with a whitening effect is provided for the skin beautifying industry.

An α-amylase inhibitory peptide. The peptide comprises amino acid sequences of eight adjacent amino acids X1, X2, X3, X4, X5, X6, X7, and X8, wherein each amino acid of the peptide is independently selected from a D-amino acid or an L-amino acid, and at least one of X2, X4, and X6 is W. The peptide has α-amylase inhibitory activity, has the effects of losing weight and lowering blood sugar, and can be used for preparing α-amylase inhibitors, weight-losing drugs, hypoglycemic drugs, or foods, health-care products or drugs for preventing or treating obesity-related diseases.

The invention discloses an N-phenylbenzenesulfonamide compound as well as a preparation method and application thereof. The compound disclosed by the invention is shown as a formula (I). The compound is an LDHA enzyme inhibitor, is a sulfonamide compound with anti-tumor activity, shows good anti-tumor activity at the cellular level, has good safety and can be used for preparing anti-tumor drugs. # imgabs0 #

Provided herein are certain fused ring compounds, such as a compound of Formula (A), as Werner Syndrome RecQ DNA helicase (WRN) inhibitors, pharmaceutical compositions comprising the compounds, and method of use of the compounds or pharmaceutical compositions in the treatment of diseases or disorders.

Provided is the use of OXCT1 protein as succinyltransferase. It has been found that the OXCT1 protein serving as succinyltransferase can promote the growth of cancer cells by modulating succinylation modification of protein. Therefore, the design of related enzyme inhibitors can inhibit the activity of succinyltransferase, thereby inhibiting the occurrence and progression of cancer, thereby providing a new concept for targeted therapy.

The invention discloses a tyrosinase inhibitory peptide from kelp as well as a preparation method and application of the tyrosinase inhibitory peptide. The preparation method comprises the following steps: pretreating kelp, fermenting the kelp by using lactobacillus plantarum, carrying out centrifugation, ultrafiltration and component identification on the obtained fermentation liquor to obtain the composition of kelp polypeptide, screening the tyrosinase inhibitory peptide through molecular docking, and finally carrying out solid-phase synthesis to obtain the tyrosinase inhibitory peptide prepared by the invention. The lactobacillus plantarum fermentation technology is simple and feasible, the production cost is low, equipment is easy to obtain, active ingredients in kelp can be released to the maximum extent, and the prepared polypeptide has the effect of inhibiting the activity of tyrosinase and can be used for developing a tyrosinase inhibitor.

The disclosure provides compounds, in part, compounds of Formula (I) or Formula (II) and their use in treating medical diseases or disorders, such as neurodegenerative diseases, e.g., Parkinson's disease. Pharmaceutical compositions and methods of making compounds of the disclosure are provided. The compounds are contemplated to be modulators, e.g., inhibitors, of cyclic ADP ribose hydrolase (CD38).

Provided is a compound of formula (I), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition thereof, having membrane associated tyrosine and threonine kinase inhibitory activity, and the use of the compound of formula (I) or the pharmaceutically acceptable salt thereof as a membrane associated tyrosine and threonine kinase inhibitor for the prevention or treatment of diseases mediated by membrane associated tyrosine and threonine kinase, such as tumors. # imgabs0 #

Disclosed is a series of pyrazolopyridine compounds, and application thereof in the preparation of RET kinase inhibitors for treatment. Specifically disclosed is the compound represented by formula (I), or a pharmaceutically acceptable salt thereof.

Compounds of formula (I)wherein A, R, W, Q, n and m have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.

The invention discloses application of a lysosome cathepsin L inhibitor in a medicine for treating or relieving allergic airway inflammation, and relates to the field of allergic airway inflammation. It is found through research that inflammatory response of asthma can be relieved by inhibiting expression of lysosome CTSL in macrophages and animal models; the inflammatory response of asthma can be relieved by inhibiting expression of lysosome CTSL in macrophages by using a small-molecule inhibitor and myeloid specific knockout CTSL, so that the lysosome cathepsin L inhibitor can effectively relieve allergic airway inflammation, and a new direction can be provided for research and development of drugs for treating and relieving allergic airway inflammation in the future.

The invention provides an application of atractylis lactone as a beta-glucuronidase inhibitor. Experiments find that atractylenolide can act on active sites of beta-glucuronidase to generate various bonding effects and play an inhibition role, and atractylenolide shows a dose-dependent relationship on activity inhibition of beta-glucuronidase. Furthermore, the atractylenolide can be used as a beta-glucuronidase inhibitor for preventing and treating related diseases (such as drug-induced diarrhea, diabetes mellitus, calculus and the like), and has very good research and application values.

The invention discloses a casein peptide-containing composition capable of improving sleep as well as a preparation method and application of the casein peptide-containing composition. The casein peptide-containing composition comprises the following components: casein peptide nanoparticles which are prepared by an ultrasonic nanocrystallization technology; the multi-layer micro-capsule coating comprises a double-layer structure formed by natural polysaccharide and a lipid compound, so that the stability of casein peptide in gastrointestinal tracts is improved; an enzyme inhibitor for temporarily inhibiting the activity of pepsin to enhance the bioavailability of casein peptide; according to the casein peptide sleep-aiding composition, through the comprehensive technical design of multi-layer micro-capsule enveloping, nanocrystallization and enzyme inhibitor sheet layers, the stability, the bioavailability and the sleep-aiding effect of the casein peptide sleep-aiding composition are remarkably improved, and the casein peptide sleep-aiding composition shows superiority in the aspects of user experience and production feasibility.

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.

To provide a transcriptional regulator protein degradation-promoting composition that is capable of directly facilitating the induction of transcription regulator protein degradation and also capable of enhancing the degradation-inducing effect through the combined administration of multiple components, wherein the transcriptional regulator protein degradation-promoting composition serves as a highly effective cancer therapeutic agent, as well as to provide a therapeutic agent comprising the same.SOLUTION: The present invention provides a transcriptional regulator protein degradation-promoting composition that facilitates the degradation of the transcription regulator protein, comprising a PARG inhibitor, a PERK inhibitor, an HSP90 inhibitor, or a histone acetylation enzyme inhibitor, as well as a therapeutic agent comprising the same.SELECTED DRAWING: None

The invention discloses an N-benzylimidazopyridine derivative as well as a preparation method and application thereof. According to the derivative, a structural fragment of lauric acid serving as a catalytic substrate of CYP4Z1 is introduced to N-benzylimidazopyridine, and the length, a connecting chain and an ending group of the introduced fragment are changed, so that the compound disclosed by the invention is prepared; as a CYP450 enzyme inhibitor, the N-benzylimidazopyridine derivative can specifically inhibit CYP4Z1 enzyme, further reduces or inhibits the activity of the CYP4Z1 enzyme in breast cancer cells, achieves the purpose of treating and / or preventing the problems of poor prognosis, invasion and metastasis and the like of breast cancer mediated by the CYP4Z1 enzyme, and has great application prospects in the field of tumor treatment drugs.

Provided herein are compositions and methods for reducing levels of at least one biomarker in a subject. The at least one biomarker may include p75ECD, PGE-MUM, or both. In some cases, the compositions and methods provided herein involve administering to a subject an amount of a 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitor effective to reduce levels of the at least one biomarker in the subject.

The invention discloses a gymnadenia conopsea octasaccharide-decaose mixture as well as a preparation method and application thereof, and belongs to the technical field of medicines. The monosaccharide of the octasaccharide-decataccharide mixture of the gymnadenia conopsea comprises N-acetamino galactose, fucose, glucuronic acid or sugar alcohol thereof, galactose, N-acetylglucosamine, dehydrated talose and a sulfate group. The octasaccharide to decataccharide mixture of the gymnadenia conopsea disclosed by the invention can be used for remarkably prolonging the time of activating partial thromboplastin and prothrombin and effectively inhibiting endogenous and common coagulation pathways. The octasaccharide-decaose mixture of the gymnadenia conopsea can be used as a potential endogenous factor X enzyme inhibitor for preparing medicines for treating thrombotic cardiovascular diseases.

Compounds that inhibit p38α MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.

The invention relates to the technical field of plant tissue extraction, in particular to an efficient extraction method and application of ginseng callus-derived exosomes, the extraction method comprises the following steps: S1, mixing ginseng callus with a PBS buffer solution, homogenizing and filtering to obtain a filtrate; s2, adding a protease inhibitor and a deep eutectic solvent into the filtrate, uniformly mixing, and standing to obtain a mixed solution; s3, centrifuging and filtering the mixed solution, and reserving supernate; s4, carrying out ultracentrifugation on the supernatant, collecting the precipitate, and resuspending with PBS to obtain a resuspension; and S5, further filtering the resuspension to obtain a filtrate, and storing at low temperature. The ginseng callus exosome extracted by the extraction method disclosed by the invention can be applied to preparation of drugs or cosmetics with anti-oxidation, anti-inflammatory and anti-aging effects, and the technical problems of low extraction efficiency, insufficient purity, complex extraction operation and poor stability of the extracted exosome in the existing exosome extraction technology can be effectively solved.

The invention discloses a rice ACCase mutant protein and a preparation method thereof. The amino acid sequence of the ACCase mutant gene encoding protein has the following mutations: the 2052nd site corresponding to the amino acid sequence of wild rice ACCase is mutated, isoleucine (I) is changed into asparagine (N), or isoleucine (I) is changed into glutamine (Q), or isoleucine (I) is changed into cysteine (C), or isoleucine (I) is changed into cysteine (C), or isoleucine (I) is changed into cysteine (C), or isoleucine (I) is changed into cysteine (C), or isoleucine (I) is changed into cysteine (C). And the plant can have extremely strong resistance (tolerance) to acetyl-coenzyme A carboxylase inhibitor herbicides. After the rice containing the rice ACCase mutant protein disclosed by the invention is applied with an acetyl-coenzyme A carboxylase inhibitor herbicide with 8 times of recommended use concentration, plants still grow normally, and the tolerance of the herbicide is greatly enhanced, so that the rice ACCase mutant protein can be widely applied to breeding of herbicide-resistant plants.

The invention discloses a CRISPR (clustered regularly interspaced short palindromic repeats)-Cas system-combined high-sensitivity DNA (deoxyribonucleic acid) methyltransferase activity determination system and a CRISPR-Cas system-combined high-sensitivity DNA methyltransferase activity determination method. DNA tetrahedrons capable of forming dumbbell rings at four corners are designed, when Dam MTase exists, Dam methyltransferase modifies an adenine residue in a GATC sequence, the adenine residue is subjected to Dpn I recognition and shearing and then is combined with a CRISPR / Cas 12a system, and only when a recognition site is methylated, the Dam methyltransferase can be used for detecting the activity of the GATC sequence. Only when the DpnI identifies the site and cuts the site, the exposed single chain can be combined with a CRISPR / Cas system to generate an enzyme digestion effect, the fluorescent single chain is cut and cut to generate fluorescence, and the concentration of Dam MTase can be known according to the size of the fluorescence. Certain clinical significance is realized when the kit is applied to early diagnosis of diseases such as cancers.

The invention relates to a crystal form of a JAK kinase inhibitor, in particular to a polymorphic form of 2-{3-[3-amino-4-(7H-pyrrolo [2, 3-d] pyrimidine-4-yl)-1H-pyrazol-1-yl]-1-(isopropylsulfonyl) azetidin-3-yl} acetonitrile and a preparation method of the polymorphic form of the 2-{3-[3-amino-4-(7H-pyrrolo [2, 3-d] pyrimidine-4-yl)-1H-pyrazol-1-yl]-1-(isopropylsulfonyl) azetidin-3-yl} acetonitrile. The present application also relates to pharmaceutical compositions containing at least one polymorph and therapeutic or prophylactic uses of the polymorph and compositions.

The invention provides inter alia methods of treating cancer comprising administering to a subject a cytidine triphosphate synthase 1 (CTPS1) inhibitor and a B-cell lymphoma 2 (BCL2) inhibitor.

The invention provides an angiotensin converting enzyme inhibitory peptide and application thereof. The amino acid sequence of the angiotensin converting enzyme inhibitory peptide is PVKP. The ACE inhibitory activity of the inhibitory peptide PVKP provided by the invention is obviously improved compared with that of the original inhibitory peptide LYPVK, and the IC50 value is reduced from 10.6 mu g / mL to 9.6 mu g / mL; the digestive enzyme stability of the inhibitory peptide PVKP provided by the invention and the digestive enzyme stability of the original inhibitory peptide LYPVK under the same concentration are improved. Molecular simulation docking verifies that the interaction force between the ACE inhibitory peptide PVKP and ACE is enhanced compared with that of an original inhibitory peptide LYPVK, and the interaction force between alkyl groups and the interaction between the alkyl groups and Zn < 2 + > of an ACE active center are increased. The intracellular antihypertensive activity of the ACE inhibitory peptide PVKP is further verified through cell experiments, and compared with the original inhibitory peptide LYPVK, the intracellular NO release content is increased, and the ET-1 content is reduced. The ACE inhibitory peptide PVKP is small in molecular weight and good in water solubility, and application of the ACE inhibitory peptide PVKP in development of products with the blood pressure lowering effect is facilitated.

The present invention relates to an inhibitory polypeptide for use in treating and / or preventing a transmembrane serine protease (TMPRSS) and / or neutrophil elastase mediated disease in a subject, wherein said inhibitory polypeptide comprises an amino acid sequence of SEQ ID NO:1 or an amino acid sequence at least 70% identical thereto. The present invention further relates to polynucleotides, host cells, devices, kits, and uses related thereto.

A fused ring compound, and a preparation method therefor and a use thereof. The fused ring compound is a Myt1 kinase inhibitor, can be used for treating tumors, and has good selectivity.

The invention relates to the field of cell biology, and particularly discloses a neural stem cell induced differentiation culture medium and application thereof in preparation of neural stem cells. The neural stem cell induced differentiation culture medium is composed of a basic culture medium and additives, wherein the additives are composed of an N-2 additive, a B-27 additive, glutamine, a human leukemia inhibiting factor, a GSK-3 inhibitor, an ALK inhibitor, a gamma-secretase inhibitor and a CDK8 inhibitor. The neural stem cell induced differentiation culture medium is clear and simple in component, does not need to use antibiotics, and does not contain animal-derived components. When the culture medium is used for carrying out differentiation induction on the human pluripotent stem cells, the human pluripotent stem cells can be induced and differentiated into the neural stem cells within a short time (6-7 days) without depending on pluripotent stem cell cloning and a single cell state, the nonuniformity of pluripotent stem cell cloning formation can be overcome, and the purity of the neural stem cells is improved.