19 results about "Fatty acid synthase" patented technology

The application belongs to the technical field of biological medicine, and specifically discloses a compound for targeted degradation of fatty acid synthase and application thereof, which has a structure shown in general formula I or a pharmaceutically acceptable salt thereof. The compound provided by the application is designed through a target ligand-connection bridge-E3 ligand structure, realizes efficient degradation, can significantly reduce the level of FASN in high-expression cells, and thus specifically targets cells related to abnormal lipid metabolism. The mechanism of action depends on the ubiquitin-proteasome pathway and is time-dependent. The compound provided by the application has good biological activity of degrading FASN, can be applied to the development of anti-liver cancer drugs, and has a wide application prospect.

The invention belongs to the technical field of biological medicines, and particularly relates to a daphniphyllum calycinum extract compound, an extraction method thereof and application of the daphniphyllum calycinum extract compound in preparation of a medicine for preventing or treating non-alcoholic fatty liver diseases. A natural compound with a novel structure is obtained from daphniphyllum calycinum for the first time, a preparation method of the compound is provided, activity research is carried out on the compound, and experimental data shows that the compound is low in cytotoxicity and has no obvious cytotoxicity to normal cells, and the compound can be used for preparing the compound by inhibiting expression of fatty acid synthetases ACC, ACLY and FAS. The compound inhibits the de novo synthesis of fatty acid in cells, thereby inhibiting the accumulation of lipid droplets in the cells and reducing the lipid level in the cells, and has wide application prospects in the field of preparation of drugs for preventing or treating non-alcoholic fatty liver diseases.

The invention relates to the field of biological medicines, in particular to application of fatty acid synthase (FASN) as a target spot in screening or preparing medicines for treating breast cancer, and particularly relates to targeted therapy for breast cancer stem cells (BCSCs). The invention discloses application of an FASN target spot in screening or preparing a medicine for treating breast cancer. Research finds that FASN is highly expressed in BCSCs, and stem cell characteristics of the BCSCs are maintained by activating a Wnt / beta-catenin pathway. By inhibiting the activity of FASN (such as using lansoprazole), the proliferation, self-renewal and tumor formation ability of BCSCs can be significantly reduced. The invention provides an FASN-based drug screening method and a drug composition, and provides a new strategy for breast cancer treatment.

The application discloses a method for constructing a multi-enzyme complex engineering strain, and has the characteristics that the method comprises the following steps: S1, constructing a light decarboxylase FAP and an oil-producing yeast fatty acid synthase fusion expression vector; S2, electrically shocking and transforming the constructed target vector into an agrobacterium competent AGL1, and introducing the target vector into a starting strain through an agrobacterium-mediated transformation method to obtain an engineering strain that is back-supplemented with a fatty acid defect; the engineering strain that is back-supplemented with the fatty acid defect is obtained, the FAP-FAS2 fusion expression is realized at the same time as the self-assembly of the intracellular FAS1, and a FAP-FAS synthase complex is obtained. The complex not only back-supplements the fatty acid defect function, so that the strain grows normally, but also can synthesize alkanes in the process of blue light irradiation fermentation culture, and realizes the intracellular assembly of protein macromolecules.

Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

The invention relates to the field of gene engineering, and discloses a CRISPRi (clustered regularly interspaced short palindromic repeats i) system, a recombinant strain containing the CRISPRi system, a construction method and application of the recombinant strain, and a method for producing gibberellin. The CRISPRi system comprises a coding gene of a dCas9 mutant protein without cleavage activity, sgRNA and an induction regulation component, wherein the induction regulation component is used for regulating the expression of the dCas9 mutant protein coding gene; the sgRNA guides the dCas9 mutant protein to be combined to a target gene, so that the expression of the target gene is inhibited; the dCas9 mutant protein is obtained by mutation on the basis of a Cas9 protein, and mutation sites are D10A and H840A of the dCas9 protein; the target genes comprise squalene synthase encoding genes, fatty acid synthase encoding genes and the like, the CRISPRi system can accurately and efficiently regulate and control gibberellin gene expression, the gibberellin yield is remarkably increased, the influence on strain growth is small, regulation and control are reversible, specificity is high, and the CRISPRi system is matched with gibberellin and has good industrial prospects.

The application belongs to the field of tumor diagnosis and treatment, and relates to a potential inhibitor of fatty acid synthase (FASN) and application of the potential inhibitor in treating various tumors such as colorectal cancer, breast cancer, ovarian cancer and the like. The small-molecule inhibitor is a compound shown in formula I or II, or a stereoisomer of the compound shown in formula I or II, or a pharmaceutically acceptable salt, a solvate, a hydrate, a polymorph, a co-crystal, a tautomer, an isotopically labeled derivative and a prodrug thereof. The compound is mainly used for inhibiting the enzyme activity of FASN and then inhibiting the proliferation of various tumors, for example, the growth and proliferation of colorectal cancer, breast cancer, ovarian cancer and the like, and is expected to become a novel broad-spectrum tumor treatment drug and has a wide application prospect.

The invention discloses application of a Reg4 gene in treatment of metabolism-related fatty liver, and relates to the technical field of biomedicine. The Reg4 gene is applied to the aspect of treating obesity and metabolism-related fatty liver; according to the application, by increasing expression of the Reg4 gene, liver lipid deposition, liver cell ballooning and inflammatory infiltration related to the metabolism-related fatty liver are inhibited; the application is realized by inhibiting the processes of de novo synthesis of fat in the liver, liver lipid uptake and fatty acid beta oxidation. The step of inhibiting the de novo synthesis of fat in the liver comprises the step of inhibiting the expression of genes of acetyl coenzyme A carboxylase 1, fatty acid synthase and / or stearoyl coenzyme A desaturase 1. The invention definitely proves that the Reg4 gene has an obvious effect of improving obesity and metabolism-related fatty liver, and can relieve hepatic fatty degeneration and inflammation.

Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and / or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatopepatitis (NASH).

The invention discloses functional feed for protecting liver and intestines of mandarin fish and a preparation method of the functional feed, and belongs to the technical field of feed. The functional feed for protecting the liver and the intestine of the mandarin fish comprises the following components: an intestine and liver protecting compound, an enteric coating material, an adsorbent, an anti-sticking agent, a protein source, a fat source, carbohydrate, compound vitamins and compound minerals. The preparation method comprises the following steps: firstly, preparing a coating solution, putting an intestine and liver protecting compound into a fluidized bed, spraying the coating solution at the bottom, curing, adding an adsorbent, and mixing to obtain a coated compound; then mixing a protein source, a fat source and carbohydrate to obtain a basic nutrient; and finally, mixing the coated compound, the basic nutrient mixture, the compound vitamins and the compound minerals, extruding and granulating, spraying an anti-sticking agent, and drying to obtain the feed. The functional feed for protecting liver and intestine of mandarin fish provided by the invention can inhibit fatty acid synthase in liver, reduce liver lipid deposition of mandarin fish, restore the liver-body ratio, improve the feed conversion rate and enhance the growth performance of mandarin fish.

The invention relates to a fatty acid synthase inhibitor and application thereof. Particularly, the invention relates to a compound shown in a general formula (I), a stereoisomer or pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and application of the compound shown in the general formula (I) or the pharmaceutical composition thereof in preparation of drugs for preventing and / or treating fatty acid synthase (FASN) mediated diseases, and substituents in the general formula (I) are as defined in the specification.

The invention provides application of tauroursodeoxycholate in prevention or treatment of mitochondrial encephalopathy, and belongs to the technical field of medicine. The core of the invention lies in that the pathological mechanism of the mitochondrial encephalopathy is coped with by utilizing multiple biological effects of the TUDCA. In-vivo and in-vitro experiments find that after a cKO mouse is treated by TUDCA, the expression of an endoplasmic reticulum stress marker Atf4 and fatty acid synthase (Fasn) in the mouse can be remarkably reduced, and abnormal accumulation of lipid is reduced, so that the metabolic state of cells is improved. In animal models, treatment with TUDCA not only alleviates dyskinesia, but also promotes the neurogenesis process and extends the survival time of mice.

Method and compositions for treating glioblastoma (GBM) and other cancers is disclosed, involving the combination of radiation therapy (RT), fatty acid synthase (FASN) inhibitors, and programmed cell death protein 1 (PD-1) inhibitors or programmed death ligand 1 (PD-L1) inhibitors. The disclosed approach addresses the technical problem of RT-induced immunosuppression and resistance in cancers by targeting RT-induced lipid metabolism, which promotes immune escape. FASN inhibitors block fatty acid synthesis, enhancing immune cell infiltration and restoring anti-tumor immunity. PD-1 / PD-L1 inhibitors further counteract immunosuppressive pathways to improve therapeutic efficacy. This combination therapy prolongs survival, induces immune memory, and is applicable to other cancers, including those exhibiting increased lipid content post-RT or chemotherapy, including melanoma, breast cancer, and lung cancer.

When employed, a recombinant expression vector carrying a daptomycin production gene including a foreign fatty acyl AMP ligase (FAAL) gene, a thioesterase (TE) gene, and a fatty acid synthase (FAS) gene according to the present invention can enhance specificity for decanoic acid, and produce daptomycin without supplementation of lipopeptides, such as decanoic acid, from the outside of the strain. In addition, no by-products are generated during the production process, thereby enabling production of daptomycin with high purity and high yield.

The application provides an enzyme inhibiting supramolecular complex and application in cosmetics, and relates to the field of cosmetic raw materials.The supramolecular complex is a supramolecular structure formed by hydrogen bond connection of coriander glycoside and sodium phosphatide through high-pressure homogenization treatment and gradient freeze-drying treatment, and can inhibit key enzymes of sebaceous gland secretion, including aminoacylase N, 3beta-hydroxysteroid dehydrogenase and fatty acid synthase.The supramolecular complex can be added into different types of cosmetics, especially cosmetics with oil control and pore shrinking functions, so that the supramolecular complex can not only play a role of the composition itself, but also improve the transdermal rate by using the lipophilicity of phospholipid, and maximizes the cosmetic effect.

The invention relates to a fatty acid synthase inhibitor and application thereof. Particularly, the invention relates to a compound shown in a general formula (I), a stereoisomer or pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and application of the compound shown in the general formula (I) or the pharmaceutical composition thereof in preparation of drugs for preventing and / or treating fatty acid synthase (FASN) mediated diseases, and substituents in the general formula (I) are as defined in the specification.

The present invention relates to heterocyclic modulators of lipid synthesis. Compounds are provided as modulators of fatty acid synthesis. The compounds are useful in treating disorders characterized by dysregulation of fatty acid synthase function and / or the fatty acid synthase pathway by modulating fatty acid synthase function and / or the fatty acid synthase pathway. Methods for treating such disorders are provided, including viral infections, such as hepatitis C infection, cancer, and metabolic disorders, such as nonalcoholic steatohepatitis (NASH).

The invention relates to application of acacetin in alcoholic hepatitis, and relates to the technical field of medicines. According to the application of the acacetin in the alcoholic hepatitis, the acacetin can effectively reduce fatty acid synthase expression, relieve stem cell vacuolar degeneration and reduce cell apoptosis, so that the alcoholic hepatitis is relieved and treated, and the acacetin has an excellent application prospect in the aspect of development of drugs for treating the alcoholic hepatitis.

In a first aspect, the present invention relates to new recombinant polypeptides derived from the newly identified gamma subunit of the fatty acid synthase protein complex. In addition, a fatty acid synthase protein complex comprising these new recombinant polypeptides are disclosed as well as nucleic acid molecules encoding these polypeptides. Further, a host cells containing the nucleic acid molecule encoding the polypeptides according to the present invention or expressing the polypeptide according to the present invention are described. In addition, an isolated fatty acid synthase protein complex is disclosed containing the newly identified gamma subunit thereof. Moreover, methods for determining the suitability of candidate compounds capable of inhibiting either the ketoreductase, enoylreductase or malonyl / palmitoyl transferase present in the FAS protein complex and methods for designing inhibitors of said enzymes are disclosed. Finally, the present invention relates to the inhibitors and their use in medicinal applications.