53 results about "Transferase inhibitor" patented technology

The application discloses a specific palmitoyl transferase inhibitor and application thereof, and an active ingredient of the palmitoyl transferase inhibitor is 4-(3-(2-(trifluoromethyl)-9H-thioxanthene-9-ylidene)propyl)-1-piperazine ethanol or a salt thereof. Current palmitoylation inhibitors, 2-bromohexadecanoic acid (2-BP), cerulenin and tunicamycin can all inhibit protein palmitoylation in cells, but all are not selective. And the existing palmitoylation inhibitors are similar to endogenous fatty acids, and inevitably affect lipid metabolism in the body, which limits the clinical application. The application discloses, for the first time, the application of 4-(3-(2-(trifluoromethyl)-9H-thioxanthene-9-ylidene)propyl)-1-piperazine ethanol as a specific palmitoyl transferase inhibitor, and the palmitoyl transferase inhibitor is better in specificity and reversible in inhibition.

The present invention relates to the use of carnitine palmitoyltransferase 1 inhibitors in the treatment of heart failure with preserved ejection fraction. The use in particular is the use of the carnitine palmitoyltransferase (CPT1) inhibitor Etomoxir for the prevention and / or treatment of heart failure with preserved ejection fraction by oral administration.

The invention relates to a class of compounds useful as Hedgehog Acyltransferase inhibitors, as well as the treatment or prevention of diseases associated with the Hedgehog signalling pathway using the compounds of the present invention. In one aspect, the present invention provides a compound of formula (I) below.

The invention relates to the technical field of oral medicine, in particular to a DNMTi and ZIF-8 nano-complex and application thereof.The DNMTi and ZIF-8 nano-complex is technically characterized in that in-situ synthesized zeolite imidaze-8 (ZIF-8) is adopted for delivering a DNA methyltransferase inhibitor (DNMTi), dental pulp stem cell (DPSC) cell spheres are combined, the DNMTi and ZIF-8 nano-complex can be used for bionic therapy, the activity of medicine is prolonged, and the effect of treating dental pulp stem cells is achieved. And zinc ions are continuously released to activate a PI3K-AKT signal channel, so that the dentin differentiation of stem cells and the generation of blood vessels are promoted. Through accurate simulation of a tooth development microenvironment, the biomimetic therapy can realize regeneration of a dental pulp-dentin complex. The therapy for simulating the tooth development process not only solves the key problems in the dental tissue engineering, but also opens up a new direction for treating the dental pulp and periapical diseases, and highlights the wide application prospect in regenerative medicine.

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).

This invention relates to the application of methyltransferase inhibitors as adjuvants for respiratory syncytial virus (RSV) vaccines and allergy vaccines. Methyltransferase inhibitors, as adjuvants for RSV vaccines or allergy vaccines, can target and regulate the antigen presentation function of vaccine-induced memory dendritic cells (DCs), thereby regulating the balance of T cell responses and balancing the dominant Th2 and / or Th17 cellular immune responses induced by RSV vaccines or allergy vaccines. This allows the vaccine recipient to develop a balanced immune memory, providing protection while preventing the occurrence of vaccine-enhanced inflammatory diseases when RSV infection or allergen stimulation occurs, thus being both safe and effective.

Methods and compositions for treating cancer e.g., liver cancer in a subject in need thereof are provided. Compositions including an effective amount of an 1-Acylglycerol-3-Phosphate O-Acyltransferase 4 (AGPAT4) inhibitor alone, or in combination with a kinase inhibitor and methods of use thereof for treating cancer are disclosed. The composition includes one or more small molecule inhibitors, inhibitory nucleic acids, or inhibitor proteins in a pharmaceutically acceptable carrier. Administration of the AGPAT4 inhibitor, alone or in combination with a kinase inhibitor is effective to reduce cancer cell proliferation or viability in a subject with cancer. Methods of selecting and treating subjects with cancers, particularly liver cancer are also provided.

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.

Disclosed are compounds and pharmaceutically acceptable salts thereof, which are useful as inhibitors nicotinamide N-methyltransferase (NNIMT). Also disclosed are pharmaceutical compositions comprising a compound disclosed herein. Related methods of treating cancer in a subject and methods of inhibiting tumor growth in subject are also disclosed.

Disclosed are compounds and pharmaceutically acceptable salts thereof, which are useful as inhibitors nicotinamide N-methyltransferase (NNMT). Also disclosed are pharmaceutical compositions comprising a compound disclosed herein. Related methods of treating cancer in a subject and methods of inhibiting tumor growth in subject are also disclosed.

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 a compound, the compound is a compound represented by a formula (I), or an isomer, an isotope derivative, a polymorphic substance, a prodrug, a pharmaceutically acceptable salt or a solvate (I) thereof, and the definitions of A, B and C are the same as the definitions in the specification. Also provided are pharmaceutical compositions and compounds of formula (I) for use in methods of treating related diseases by inhibition of MAT2A, including some cancers in which a gene encoding a methylthioadenosine phosphorylase (MTAP) is deleted and / or not fully functioning.

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 invention relates to a biaryl derivative compound, which exhibits the activity of a diacylglycerol acyltransferase 2 (DGAT2) inhibitor and is represented by chemical formula (1), a pharmaceutical composition comprising same as an active ingredient, and a use thereof.

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.

Described herein are crystalline forms of small molecule methionine adenylyltransferase 2a (MAT2A) inhibitors and pharmaceutical compositions thereof, and methods of use thereof in the treatment of diseases or conditions that benefit from treatment with methionine adenylyltransferase 2a (MAT2A) inhibitors.

Methods and compositions for treating cancer, e.g., liver cancer in a subject in need thereof are provided. Compositions including an effective amount of an 1-Acylglycerol-3-Phosphate O-Acyltransferase 4 (AGPAT4) inhibitor alone, or in combination with a kinase inhibitor and methods of use thereof for treating cancer are disclosed. The composition includes one or more small molecule inhibitors, inhibitory nucleic acids, or inhibitory proteins in a pharmaceutically acceptable carrier. Administration of the AGPAT4 inhibitor, alone or in combination with a kinase inhibitor is effective to reduce cancer cell proliferation or viability in a subject with cancer. Methods of selecting and treating subjects with cancers, particularly liver cancer, are also provided.

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 present disclosure provides methods and compositions for treating cancer (e.g., liver cancer) in a subject in need thereof. Compositions comprising an effective amount of an inhibitor of 1-acylglycerol-3-phosphate O-acyltransferase 4 (AGPAT4), alone or in combination with a kinase inhibitor, and methods of use thereof for the treatment of cancer are disclosed. The composition comprises one or more small molecule inhibitors, inhibitory nucleic acids or inhibitory proteins in a pharmaceutically acceptable carrier. Administration of an AGPAT4 inhibitor alone or in combination with a kinase inhibitor is effective in reducing cancer cell proliferation or viability in a subject with cancer. Also provided are methods of selecting and treating subjects having cancer, in particular liver cancer.

Disclosed are inhibitors of mevalonate pathway as an efficient vaccine adjuvant and use thereof. In particular, the inhibitor is an acetoacetyl-CoA transferase inhibitor, a HMG-COA synthase inhibitor, a HMG-CoA reductase inhibitor, a mevalonate kinase inhibitor, a phosphomevalonate kinase inhibitor, a mevalonate-5-pyrophosphate decarboxylase inhibitor, an isopentenyl pyrophosphate isomerase inhibitor, a farnesyl pyrophosphate synthase inhibitor, a geranylgeranyl pyrophosphate synthase inhibitor or a geranylgeranyl transferase (I, II) inhibitor. Also disclosed is an immunogenic composition including inhibitors of mevalonate pathway as an adjutant.

The present disclosure relates to solid forms of Compound 1, or pharmaceutically acceptable forms thereof, pharmaceutically acceptable salts of Compound 1, or pharmaceutically acceptable solvates thereof, pharmaceutical compositions comprising them, methods of making them, and methods of using them in the treatment of farnesylated protein dependent cancers.

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.

Certain embodiments of the invention pertain to a method of treating an infection in a subject caused by an infectious agent other than Escherichia coli, the method comprising administering to the subject arsinothricin or a salt thereof. The infectious agent other than E. coli can be a bacterium, protozoan, helminth, archaebacterium, or a fungus. In preferred embodiments, the infectious agent is Mycobacterium tuberculosis, Mycobacterium bovis, or Enterobacter cloacae. The invention also pertains to a method of treating an infection in a subject caused by an infectious agent, comprising administering to the subject arsinothricin or a salt thereof in combination with an inhibitor of phosphinothricin N-acetyltransferase or arsinothricin N-acetyltransferase. In certain such embodiments, the infectious agent expresses phosphinothricin N-acetyltransferase or arsinothricin N-acetyltransferase. Further embodiments provide compositions comprising arsinothricin or a salt thereof and an inhibitor of phosphinothricin N-acetyltransferase or arsinothricin N-acetyltransferase.

The invention relates to a method for differentiating mesenchymal stem cells into neural stem cells and application, and belongs to the technical field of stem cell engineering.The method comprises the steps that (a) the mesenchymal stem cells are cultured in a culture medium containing an HDAC inhibitor and a DNA methyltransferase inhibitor to induce differentiation of the mesenchymal stem cells, and therefore cells for promoting expression of neural stem cell marker genes are formed; (b) culturing the cells obtained in step (a) in a culture medium containing an HDAC inhibitor, a DNA methyltransferase inhibitor, a retinoic acid receptor agonist and a GSK-3 inhibitor to induce differentiation thereof, thereby forming cells that initiate expression of a neural stem cell marker protein; and (c) culturing the cells obtained in step (b) in a culture medium containing a GSK-3 inhibitor and a retinoic acid receptor agonist to induce differentiation thereof, thereby forming neural stem cells. The differentiation method disclosed by the invention has the characteristics of short preparation period and high differentiation efficiency, and the prepared neural stem cells can be used for treating / or preventing neurodegenerative diseases.