60 results about "LDL receptor" patented technology

Specific monomer domains and multimers comprising the monomer domains are provided. Methods, compositions, libraries and cells that express one or more library member, along with kits and integrated systems, are also included in the present invention.

Disclosed are methods for the use of therapeutic polypeptide-encoding polynucleotides in the creation of transformed host cells and transgenic animals. In particular, the use of recombinant adeno-associated viral (rAAV) vector compositions that specifically target mammalian cells, such as pancreatic islets cells, that express low-density lipoprotein receptors on their cell surface. The disclosed vectors comprise one or more polynucleotide sequences that express one or more mammalian polypeptides having therapeutic efficacy in the amelioration, treatment and / or prevention of AAT- or cytokine polypeptide deficiencies, such as for example in diabetes and related diseases, as well as a variety of autoimmune disorders including, for example, lupus and rheumatoid arthritis.

A method is disclosed for determining whether a compound binds to a lipoprotein such as LDL or VLDL in a manner which will lower plasma cholesterol. The method provided includes assessing the ability of the compound to form a complex with the lipoprotein, and then determining whether the newly formed complex causes a change in the structure of apoB-100 that results in increased binding affinity to an LDL receptor.

The invention provides a compound of the following formula (1): wherein m, n, and p are independently an integer of 0-4, provided 3≦m+n≦8; X is nitrogen atom or a group of the formula: C—R15; Y is a substituted or unsubstituted aromatic group, etc.; R15, R1, R2, R3, R4, R5, R6 and R7 are hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and Z is hydrogen atom, cyano group, etc., or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which exhibits an action for enhancing LDL receptor expression, and is useful as a medicament for treating hyperlipidemia, atherosclerosis, etc.

The present invention provides a synthetic LDL nanoparticle comprising a lipid moiety and a synthetic chimeric peptide so s to be capable of binding the LDL receptor. The synthetic LDL nanoparticle of the present invention is capable of c incorporating and targeting therapeutics for diseases associated with the expression of the LDL receptor. The invention further provides methods of using such synthetic LDL nanoparticles.

Aromatic-ring azacyclo derivatives and an application thereof are provided. The invention relates to compounds represented by the formula (V), and a preparation method and an application thereof in medicines. In particular, the invention relates to derivatives of the compounds represented by the general formula (V), and a preparation method and the application thereof as therapeutic agents in prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, type-II diabetes, hyperglycemia, obesity or insulin resistance syndromes and metabolic syndromes. The compounds disclosed by the invention also can reduce total cholesterol, LDL-cholesterol and triglycerides, increase the expression of hepatic LDL receptors and inhibit the expression of PCSK9.

The present invention relates to a compound as shown in a formula (VII), a preparation method and applications thereof in medicines. In particular, the present invention relates to a derivative of the compound as shown in the formula (VII), a preparation method, and the applications of the derivative used as a therapeutic agent in prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, II-type diabetes, hyperglycemia, obesity or insulin resistance syndrome and metabolic syndrome. The compound disclosed by the present invention can also reduce total cholesterol, LDL-cholesterol and triglyceride, and increases expression of a liver LDL receptor and decreases expression of PCSK9.

Provided are a tetrahydroisoquinoline derivative and an application thereof. The invention relates to a compound represented by the formula (V) and a preparation method and an application thereof in medicines. In particular, the invention relates to the derivative of the compound represented by the general formula (V) and a preparation method and the application thereof as a therapeutic agent in prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, type-II diabetes, hyperglycemia, obesity or insulin resistance syndromes and metabolic syndromes. The compound disclosed by the invention also can reduce total cholesterol, LDL-cholesterol and triglycerides, and increases the expression of hepatic LDL receptors and inhibits the expression of PCSK9.

Controlled studies demonstrate that methods using soy related peptides inhibit H3 acetylation, reduce expression of HMG CoA reductase and increase LDL receptor and Sp1 expression in mammals. The present disclosure is generally directed to using lunasin peptides and / or lunasin peptide derivatives to 1) inhibit H3 acetylation, 2) reduce expression of HMG CoA reductase, 3) increase LDL receptor expression or 4) increase Sp1 expression in a mammal. In at least one exemplary embodiment of the present disclosure, an effective amount of lunasin peptides or lunasin peptide derivatives and one or more enzyme inhibitors is provided to a mammal to 1) inhibit H3 acetylation, 2) reduce expression of HMG CoA reductase, 3) increase LDL receptor expression or 4) increase Sp1 expression in a mammal.

The invention discloses a preparation method and application of cordyceps militaris sporocarp heteropolysaccharide. The preparation method mainly comprises the following steps that cordyceps militaris sporocarp is subjected to drying, pulverization, ethanol degreasing and hot water ultrasonic extraction, and an extracting solution is subjected to concentration, alcohol precipitation, deproteinization, column chromatography, dialysis and freeze-drying, so that the cordyceps militaris sporocarp heteropolysaccharide TY258 is obtained. The cordyceps militaris polysaccharide has the efficacy of lowering lipid and resisting to atherosclerosis and can remarkably lower the cholesterol level, the triglyceride level and the low density lipoprotein level of high-fat induced atherosclerosis model mice (mice with apolipoprotein and low density lipoprotein receptors knocked out) and lipid accumulation of the livers and arcus aortae at the concentration of 25 mg / kg, lift the high density lipoprotein cholesterol level of the mice and improve activity of superoxide dismutase and lipoprotein esterolysis enzyme. The cordyceps militaris sporocarp polysaccharide can also remarkably lower the contents of plasma triglyceride, cholesterol, malonaldehyde and oxidized low-density lipoprotein of high-fat induced guinea pigs and rats.

The present invention relates to a monoclonal antibody raised against the human LDL (Low Density Lipoprotein) receptor, binding to the peptide corresponding to amino acids 195-222 (SEQ ID NO: 1) in the peptide sequence for the human LDL receptor; to the use thereof as a drug; to a pharmaceutical composition containing this antibody; and to the use thereof in immunohistochemical analyses of cancerous, healthy, or cirrhotic tissues, in Western-Blot or ELISA analyses, or in in vivo quantification tests.

Controlled studies demonstrate that methods using soy related peptides inhibit H3 acetylation, reduce expression of HMG-CoA reductase and increase LDL receptor and Sp1 expression in mammals. The present disclosure is generally directed to using lunasin peptides and / or lunasin peptide derivatives to 1) inhibit H3 acetylation, 2) reduce expression of HMG-CoA reductase, 3) increase LDL receptor expression or 4) increase Sp1 expression in a mammal. In at least one exemplary embodiment of the present disclosure, an effective amount of lunasin peptides or lunasin peptide derivatives and one or more enzyme inhibitors is provided to a mammal to 1) inhibit H3 acetylation, 2) reduce expression of HMG-CoA reductase, 3) increase LDL receptor expression or 4) increase Sp1 expression in a mammal. Additionally, lunasin will protect against, prevent, or reduce: 1) the expression of Matrix metalloproteinase (MMP-1), 2) collagen breakdown, 3) photoaging and 4) the formation of skin wrinkles.

The invention provides a self-heal health-care oral solution capable of reducing blood fat, which comprises the following raw medicines in parts by weight: 10-50 parts of self-heal, 10-20 parts of cape jasmine, 10-20 parts of pollen typhae, 10-20 parts of purslane, 10-20 parts of rehmannia root, 10-20 parts of baikal skullcap root, 10-20 parts of kudzu root, 10-20 parts of gynostemma pentaphylla, 10-20 parts of sophora fruit, 10-20 parts of dried orange peel, 10-20 parts of corn silk, 10-20 parts of oriental wormwood, 10-20 parts of hawthorn, 10-20 parts of trichosanthes root, 10-20 parts of burdock fruit, 10-20 parts of lysimachia, 10-20 parts of tribulus terrestris, 10-20 parts of oldenlandia and 10-20 parts of centella. The oral solution provided by the invention is capable of preventing absorption of cholic acid or cholesterol from the intestinal tract, promoting cholic acid or cholesterol to be discharged with feces, inhibiting in vivo synthesis of cholesterol, or promoting conversion of cholesterol, promoting LDL receptor expression on a cell membrane, and accelerating lipoprotein decomposition.

A truncated dominant negative mammalian LDL receptor related protein (LRP) cytoplasmic tail mutant (LRP-CT) molecule and DNA sequences for its construction is described in this disclosure as is a method for disrupting generation of amyloid beta-protein (Abeta). Methods for preventing or treating diseases wherein amyloid beta-protein (Abeta) is a major constituent of amyloid plaques or amyloidosis by interfering with production of Abeta are described, as is a high throughput assay for screening compounds that inhibit Abeta production. Also described is a method for inhibiting LRP or APP:Fe65 interaction in vivo, and kit suitable for providing the required reactants for screening assays.

The invention discloses a PCSK9-combined fusion protein which is represented by the following general formula: X-connecting peptide-Y-connecting peptide-Z-connecting peptide-IgG Fc segment, wherein X, Y and Z are EGF(A) region polypeptide mutants in LDL-R (low-density lipoprotein receptor), and the connecting peptide is (GGGGS)n. The fusion protein disclosed by the invention can be combined with the PCSK9 at high affinity to inhibit the PCSK9 from degrading the hepatocyte LDL-R and increase the intake of the hepatocytes for LDL-C, and thus, has obvious advantages and favorable prospects in the aspect of treating hypercholesteremia, familial hypercholesteremia and other diseases.

The invention relates to a compound as shown in formula (V), a preparation method of the compound and application of the compound to medicine, in particular to the derivatives of the compound as shown in formula (V), a preparation method of the derivatives, and application of the derivatives which serve as the therapeutic agent to antitumor medicine and medicine for preventing and treating hyperlipemia, hypercholesteremia, hypertriglyceridemia, fatty degeneration of liver, type II diabetes, hyperglycemia, obesity, insulin resistance syndrome and metabolic syndrome.The compound can also lower total cholesterol, LDL-cholesterol and triglyceride, increase liver LDL receptor expression and inhibit PCSK9 expression.

There are provided monoclonal antibodies to the LDL receptor which are useful for the identification and purification of LDL and in treatment of e.g. hepatitis C infection.

The present invention pertains to a silkworm-type biotinylated CTLD14 or sRAGE and a method for manufacturing the same. One embodiment of the present invention provides a method for manufacturing biotinylated proteins, wherein the method includes A) a step for inserting a nucleic acid molecule for coding biotin ligase and protein in a coexpressable manner into a silkworm or a living organism that imparts sugar chains that are the same as the sugar chains of the silkworm, B) a step for causing the biotin ligase and protein to be expressed by disposing the silkworm or the living organism that imparts sugar chains that are the same as the sugar chains of the silkworm to conditions with which the nucleic acid molecule will carry out expression, and C) a step for administering biotin to the living organism and obtaining the biotinylated protein.

The invention relates to a tetrahydroberberine derivative and application thereof and relates to a compound represented by a formula (V) shown in the description, a preparation method therefor and application of the compound in medicine. Particularly, the invention relates to a derivative of the compound represented by the general formula (V), a preparation method for the derivative of the compound and use of the derivative of the compound in the prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, fatty degeneration of liver, type II diabetes, hyperglycemia, obesity or insulin resistance syndrome and metabolic syndrome. The compound disclosed by the invention can also be used for lowering total cholesterol, LDL (Low-Density Lipoprotein)-cholesterol and triglyceride, improving liver LDL receptor expression and inhibiting PCSK9 expression.

A method is disclosed for determining whether a compound binds to a lipoprotein such as LDL or VLDL in a manner which will lower plasma cholesterol is provided that includes assessing the ability of the compound to form a complex with the lipoprotein, e.g., LDL or VLDL, and then determining whether the newly formed complex causes a change in the structure of apoB-100 that results in increased binding affinity to the LDL receptor. Also disclosed is a method for lowering cholesterol in a host in need thereof, including a human, is provided that includes the administration fo an effective amount of a compound which binds to cholesterol-carrying lipoprotein (e.g. LDL or VLDL) in a manner that alters the three dimensional configuration of the lipoprotein and increases the binding affinity of the apoB-100 protein to the LDL receptor, including those on the surface of a hepatic cell.

A nitrogen-containing heterocyclic derivative and application thereof. The present invention relates to the compound of formula (V) and its preparation method and its application in medicine. Specifically, the present invention relates to derivatives and preparation methods of the compound of general formula (V) and its use as a therapeutic agent in the prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis , Type II diabetes, hyperglycemia, obesity or insulin resistance, metabolic syndrome and use in antineoplastic drugs. The compounds disclosed herein can also reduce total cholesterol, LDL-cholesterol and triglyceride, increase the expression of hepatic LDL receptors, and inhibit the expression of PCSK9.

The invention belongs to the field of biochemical engineering, and in particular relates to a chemical synthetic method of a low affinity ligand of an oxidized low density lipoprotein receptor CD36. The method comprises the following steps of: carrying out a chemical reaction on 4-Dimethylaminopyridine, N, N'-Dicyclohexylcarbodiimide, azelaic acid and 7-ketocholesterol; and obtaining oxLig-1 through extraction, sample mixing, packing, purification and collection. Experiments show that the chemically synthesized oxLig-1 has same physiological activity with that of oxLig-1 separated and purified from oxLDL (oxidized low density lipoprotein), and the oxLig-1 activates cell signaling mediated by CD36. According to the chemical synthetic method disclosed by the invention, oxLig-1 is synthesized by the chemical method, and oxLig-1 has a completely consistent chemical structure with that of the low affinity ligand of CD36 and can activate ERK (Extracellular Signal-Regulated Kinase) and JNK (Jun N-Terminal Kinase) and up-regulate expression of a cholesterol outflow gene, namely, a triphosadenine binding cassette transporter A1 (ABCA1).

The invention provides a low-density lipoprotein receptor related gene 2 LmLRP2 of migratory locust and application of dsRNA of the gene in prevention and control of the migratory locust. The specificlow-density lipoprotein receptor related gene 2 can be silenced to kill the migratory locust. After cloning and sequencing of the low-density lipoprotein receptor related gene 2 of the migratory locust, the low-density lipoprotein receptor related gene 2 with the sequence shown as SEQ ID NO:1 is obtained; the dsRNA of the gene is designed and synthesized according to SEQ ID NO:1. After the dsRNAof the gene is injected into the body cavity of the migratory locust, the migratory locus dies before molting, during molting or after molting separately, and the permeability of the epidermis is enhanced. A new specific molecular target is provided for pest prevention and control on the basis of RNA interference, and a new approach is provided for pest prevention and control.

The invention relates to the use of the souluble LDL receptor (sLDLR) in viral hepatitis.

The invention discloses an amaryllidaceous alkaloid targeted sustained-release preparation and a preparation method and a use thereof. The amaryllidaceous alkaloid targeted sustained-release preparation is composed of amaryllidaceae alkaloid, propargyl acylated chitosan and low density lipoprotein having an azide probe, wherein the molar ratio of the three components is 1 to (0.1-1) to (0.1-2). An LDL receptor of blood-brain barrier endothelial cells is selected as a target for transmission of amaryllidaceae alkaloid to treat AD, chitosan having excellent biological compatibility is used as a drug carrier material, the low-toxicity and high-efficiency amaryllidaceous alkaloid nano brain-targeted preparation is developed, and some blanks in researches before clinical application of amaryllidaceae alkaloid as an AD treatment drug at present are filled.

The invention relates to construction of a lipid metabolism disorder animal model and repair using AAV-CRISPR / CAS9. According to the invention, the animal model with typical lipid metabolism disorder disease symptoms is constructed, a construct capable of repairing a low-density lipoprotein receptor in a targeted manner and inhibiting lipid metabolism disorder diseases is further constructed, and a virus obtained by packaging can continuously and effectively repair the low-density lipoprotein receptor, the action time is long, and stability is good.

Controlled studies demonstrate that methods using soy related peptides inhibit H3 acetylation, reduce expression of HMG-CoA reductase and increase LDL receptor and Sp1 expression in mammals. The present disclosure is generally directed to using lunasin peptides and / or lunasin peptide derivatives to 1) inhibit H3 acetylation, 2) reduce expression of HMG-CoA reductase, 3) increase LDL receptor expression or 4) increase Sp1 expression in a mammal. In at least one exemplary embodiment of the present disclosure, an effective amount of lunasin peptides or lunasin peptide derivatives and one or more enzyme inhibitors is provided to a mammal to 1) inhibit H3 acetylation, 2) reduce expression of HMG-CoA reductase, 3) increase LDL receptor expression or 4) increase Sp1 expression in a mammal. Additionally, lunasin will protect against, prevent, or reduce: 1) the expression of Matrix metalloproteinase (MMP-1), 2) collagen breakdown, 3) photoaging and 4) the formation of skin wrinkles.

The invention relates to a functionalized exosome as well as a preparation method and application thereof. The functionalized exosome simultaneously expresses a low-density lipoprotein receptor targeting polypeptide and a cell-penetrating peptide, the low-density lipoprotein receptor targeting polypeptide comprises Angiopep-2, and the cell-penetrating peptide comprises a TAT polypeptide. In the functionalized exosome, the low-density lipoprotein receptor targeting polypeptide and the cell-penetrating peptide synergistically play a role, so that the dual active selectivity of the functionalized exosome to the blood-brain barrier and glioma cells can be enhanced, the cell membrane penetrating efficiency of the functionalized exosome can be improved, and the disease treatment effect is further improved.