23 results about "Transferase inhibitor" patented technology

This invention discloses a high-throughput screening method for monkeypox virus (MPXV) N7-methyltransferase (N7-MTase) inhibitors based on fluorescence polarization technology and its application. This method uses MPXV E1... CTD Using the / E12 protein complex as a target, and leveraging the specific binding characteristic of the fluorescent probe FL-NAH to the target catalytic center, small molecule inhibitors that competitively bind to the SAM binding site are screened by monitoring changes in fluorescence polarization signals. This invention yielded a series of candidate compounds with significant inhibitory activity. Experiments demonstrated that these inhibitors exhibit strong inhibitory effects on MPXV N7-MTase, with a biochemical IC50 level of [missing information]. 50 Preferably, the concentration can reach 4.65 μM; at the cellular level, the compound exhibits a clear attenuation effect against poxviruses, with an EC50 value of [missing value]. 50 The range is up to 46.75 μM, and it has low cytotoxicity (CC). 50 >200 μM).

To provide a new antitumor agent.SOLUTION: The present invention provides an antitumor agent containing a glutathione concentration lowering agent or a glutathione S-transferase inhibitor as an active ingredient to be administered simultaneously with an aldehyde dehydrogenase inhibitor, or an antitumor agent containing an aldehyde dehydrogenase inhibitor as an active ingredient to be administered simultaneously with an effective amount of a glutathione concentration lowering agent or a glutathione S-transferase inhibitor, or a combination drug containing an aldehyde dehydrogenase inhibitor and a glutathione concentration lowering agent or a glutathione S-transferase inhibitor as active ingredients. The aldehyde dehydrogenase inhibitor is a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof.SELECTED DRAWING: None

Disclosed herein are serine palmitoyltransferase inhibitors of formula (I); or a pharmaceutically acceptable salt form thereof. The variables in formula (I) are described herein. Also disclosed is a method of treating a subject with a disease characterized by elevated ceramide levels or a disease or condition that is mediated by serine palmitoyltransferase, comprising administering an effective amount of the disclosed serine palmitoyltransferase inhibitors disclosed herein.

The present invention relates to series of peptidomimetic compounds as an inhibitor targeting protein N-terminal methyltransferase pharmacological pathway. Pharmaceutical compositions of those compounds and methods of using them in the treatment of diseases caused by abnormal protein methyltransferase pathway, including cancer, inflammation, neurodegenerative and cardiovascular diseases, are within the scope of this disclosure.

The present invention relates to series of peptidomimetic compounds as an inhibitor targeting protein N-terminal methyltransferase pharmacological pathway. Pharmaceutical compositions of those compounds and methods of using them in the treatment of diseases caused by abnormal protein methyltransferase pathway, including cancer, inflammation, neurodegenerative and cardiovascular diseases, are within the scope of this disclosure.

The present invention belongs to the technical field of cellular anti-aging, and specifically relates to a small-molecule compound composition capable of reversing the senescence of an adult stem cell and restoring the regeneration activity thereof, and a method for reversing cellular senescence by means of using a chemical small-molecule composition and the use thereof. The composition capable of reversing cellular senescence comprises a WNT / β-catenin agonist, a TGF-β receptor inhibitor, an RAR agonist, a Smoothened receptor agonist, a multi-target inhibitor of the VEGFR and PDGFR families, a histone methyltransferase inhibitor, and a JAK1 / 2 inhibitor. The composition effectively solves the problem of the weak proliferation and regeneration potential of senescent adult stem cells, effectively reverses the senescence of the adult stem cells and maintains the intrinsic biological characteristics of the cells, and can thus improve and enhance the efficacy of clinical autologous cell transplantation therapy and cell derivative therapy.

The present disclosure refers to therapeutic combinations and pharmaceutical compositions comprising glycolysis inhibitors / modulators and prenyltransferase inhibitors for treating brain tumors. In particular, the disclosure describes therapeutic combinations and pharmaceutical compositions of dichloroacetate (DCA) and perillyl alcohol (POH) useful for treating brain cancers such as glioblastoma multiforme (GBM). Additionally, the disclosure provides methods for treating GBM and other forms of brain cancer using the same.

The present invention relates to an amide derivative compound, which exhibits the activity of a diacylglycerol acyltransferase (DGAT) 2 inhibitor and is represented by chemical formula (1), a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

This invention discloses an NK cell-like inducer and its application. The NK cell-like inducer comprises a DNA methyltransferase inhibitor, a histone deacetase inhibitor, a histone methyltransferase inhibitor, and vitamin C or a derivative thereof; the final concentration of the DNA methyltransferase inhibitor is 0.05~0.45 μM; the final concentration of the histone deacetase inhibitor is 0.05~1 μM; and the final concentration of vitamin C or a derivative thereof is 1~1000 μM. The inducer combination of this invention can activate the synthesis of intracellular cryoprotective substances such as glutathione, effectively reducing cell damage during cryopreservation, and increasing the survival rate of NK cell-like cells after 7 days of liquid nitrogen cryopreservation to over 90%, thus achieving long-term storage of NK cell-like cells.

The present invention relates to an amino aryl derivative compound, represented by chemical formula (1) and exhibiting the activity of a diacylglycerol acyltransferase 2 (DGAT2) inhibitor, a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

The invention discloses a method for efficiently inducing hybrid liriodendron somatic embryogenesis, and belongs to the technical field of plant embryogenesis. The method mainly comprises the following steps: performing callus multiplication culture on embryogenic calluses of hybrid liriodendron in a callus multiplication culture medium containing a DNA methyltransferase inhibitor 5-Aza-dC or Zebularine, then transferring the embryogenic calluses into a somatic embryo induction culture medium for somatic embryo induction, and obtaining mature hybrid liriodendron somatic embryos after somatic embryo induction is completed. The method is easy to operate, and the effects of inhibiting mass proliferation of embryonic tissues, promoting generation and development of somatic embryos and improving the somatic embryo generation efficiency can be achieved only by adding a proper amount of DNA methylated transferase inhibitor in the callus proliferation stage. The method can enhance the somatic embryo induction efficiency of the hybrid liriodendron, provides a new technical scheme for optimizing the somatic embryo generation of the hybrid liriodendron by using an epigenetic regulation means, and has important application value in the field of rapid propagation of the hybrid liriodendron.

The present disclosure refers to therapeutic combinations and pharmaceutical compositions comprising glycolysis inhibitors / modulators and prenyltransferase inhibitors for treating brain tumors. In particular, the disclosure describes therapeutic combinations and pharmaceutical compositions of dichloroacetate (DCA) and perillyl alcohol (POH) useful for treating brain cancers such as glioblastoma multiforme (GBM). Additionally, the disclosure provides methods for treating GBM and other forms of brain cancer using the same.

The present application relates to the technical field of pharmaceutical analysis, and particularly relates to a method for analyzing mutagenic impurities in new drug raw materials. The new drug raw material belongs to a small molecule fungal inositol acyltransferase 1 inhibitor, and is a new drug for treating fungal infections. Impurity A and impurity B are potential mutagenic impurities. The potential mutagenic impurities in the new drug raw material are detected and analyzed by using gas chromatography-mass spectrometry. By limiting the gas chromatography conditions and the mass spectrometry conditions, trace detection of impurity A and impurity B can be realized. The analysis method provided by the present application has strong specificity, and the blank solvent does not interfere with the detection of various impurities. The analysis method has high sensitivity and good accuracy, the average recovery rate of each impurity is within the range of 70% to 130%, and significant detection performance advantages are shown.

A metal complex comprising: (a) a pharmaceutically acceptable central metal; (b) a DNA methyltransferase (DNMT) inhibitor; and (c) 2,5-dihydroxyterephthalic acid (DTA) and / or syringic acid (SA).

The invention relates to the technical field of medicine for resisting keloid. The invention discloses a pharmaceutical composition for resisting keloid, application and a preparation method. The pharmaceutical composition comprises a therapeutically effective amount of nicotinamide N-methyltransferase (NNMT) inhibitor and a pharmaceutically acceptable carrier. According to the invention, an NNMT inhibitor is taken as a core, and keloids are treated through metabolism-epigenetic regulation. NAD / SAM balance can be recovered, fibroblast activation, collagen deposition and chronic inflammation are inhibited from the source, and the anti-fibrosis and anti-inflammatory dual effects are achieved. The scheme adopts a local delivery system such as a microneedle and gel, has the advantages of strong targeting property, low toxicity, relapse prevention, clear mechanism and the like, and provides a root intervention strategy for skin fibrosis.

The present invention relates to compositions and methods for treating or preventing infections, in particular infections by intracellular parasites such as Cryptosporidium spp. The present invention also relates to compositions and methods for treating or preventing viral or bacterial infections, in particular intestinal infections such as those caused by rotavirus and Salmonella spp. Infections. The methods comprise administration of, and the compositions comprise, a farnesyl-diphosphate farnesyltransferase 1 (FDFT1) inhibitor, such as lapaquistat.

Provided herein are O-GlcNAc transferase (OGT) inhibitor compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and / or preventing diseases (e.g., diabetes and complications thereof, neurodegenerative diseases, proliferative diseases such as cancers, autoimmune diseases, and inflammatory diseases) in a subject. Provided are methods of inhibiting OGT in a subject or biological sample.

The present disclosure is generally directed to treating a subject having osteoarthritis or confronting risk of developing osteoarthritis by administering to the subject a procollagen galactosyltransferase 2 (COLGALT2) inhibitor.

The invention belongs to the technical field of cell aging resistance, and particularly relates to a small molecule compound composition capable of reversing aging of adult stem cells and recovering regeneration activity of the adult stem cells, a method for reversing cell aging by using the chemical small molecule composition and application of the chemical small molecule composition. The composition capable of reversing cell senescence comprises a WNT / beta-catenin agonist, a TGF-beta receptor inhibitor, an RAR agonist, a Smooth receptor agonist, a VEGFR and PDGFR family multi-target inhibitor, a histone methyltransferase inhibitor and a JAK1 / 2 inhibitor, and effectively solves the problem of weak proliferation and regeneration potential of senescent adult stem cells. The aging of adult stem cells is effectively reversed, the original biological characteristics of the cells are maintained, and the clinical cell autotransplantation treatment and cell derivative treatment effects can be improved.

The invention discloses a coronavirus 2 '-O-methyltransferase inhibitor and an application of the coronavirus 2'-O-methyltransferase inhibitor. The inhibitor provided by the invention takes the coronavirus 2 '-O-methyltransferase as a target spot, can effectively inhibit the enzymatic activity of the coronavirus 2'-O-methyltransferase, shows a good antiviral effect on human and animal coronaviruses (including new coronaviruses and mutant strains thereof) on a cellular level, and shows good pharmacokinetic level, tissue distribution and safety in a mouse body. The inhibitor can effectively inhibit the enzymatic activity of coronavirus 2 '-O-methyltransferase, so that an efficient antiviral effect is achieved; the safety is high, and the clinical application potential is high; the method is wide in applicability and can be used for various types of coronaviruses; moreover, the oral administration utilization rate is high, the antiviral effect is good, and the application scene is greatly enriched. The application scheme also provides another thought for developing more safe, effective and broad-spectrum anti-coronavirus small molecule drugs, and has extremely high scientific research significance and practical value.

The present invention relates to pyrazolopyrimidine methotransferase 2a inhibitors and methods for their preparation. In particular, the compounds of the invention have the structure of Formula I, wherein the various groups and substituents are as described in the specification. Methods for the preparation of the compounds and their use in the treatment of cell proliferative diseases, particularly cancer, are also disclosed.

The present invention relates to a method of treating RAS-dependent cancer in a subject by use of a farnesyltransferase inhibitor. Also described are compositions comprising a farnesyltransferase inhibitor; and an agent that increases the amount of geranylgeranyl pyrophosphate (GGPP). Lastly, the use of farnesyltransferase inhibitor for transdifferentiating a cell into a fibroblast-like stage is described herein.

The application belongs to the technical field of medicines, and particularly relates to a compound with inhibitory activity on DNA methyltransferase 1 (DNMT1) and a preparation method and application thereof. In the application, a DNMT1 small-molecule inhibitor with a 2-isoindole-3-carbazolyl propionic acid skeleton is found and prepared, and is expected to be applied to the treatment of diseases related to DNA hypermethylation, especially tumor treatment.