151 results about "Receptor expression" patented technology

This invention relates to compounds, compositions, and methods useful for modulating tumor necrosis factor and / or tumor necrosis factor receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of tumor necrosis factor and / or tumor necrosis factor receptor gene expression and / or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of tumor necrosis factor and / or tumor necrosis factor receptor genes, (TNF and / or TNF receptor).

The present invention relates to non-human animals and in vivo methods for testing the efficacy of antibodies directed to antigens expressed by tumors in such animals. In particular, the invention relates to an animal deficient in the expression of one or more Fc receptors. Additionally, such an animal is also immunodeficient, and thus permits the growth of a xenogeneic tumor implant. Such immunodeficient animals may also express human receptors. The present invention also relates to methods of evaluating the enhanced ability of an existing antibody or Fc-modified antibody to act as an immunotherapeutic to eradicate tumor cells or infectious agents.

The present invention is drawn to a method of controlling gene expression in plants. Specifically, the method comprises obtaining a transgenic plant comprising at least two receptor expression cassettes and at least one target expression cassette. The first receptor expression cassette comprises a nucleotide sequence for a 5′ regulatory region operably linked to a nucleotide sequence which encodes a first receptor polypeptide, and a 3′ termination region. The second receptor expression cassette comprises a nucleotide sequence for a 5′ regulatory region operably linked to a nucleotide sequence which encodes a second receptor polypeptide, and a 3′ termination region. The target expression cassette comprises a nucleotide sequence for a 5′ regulatory region operably linked to a nucleotide sequence which encodes a target polypeptide, and a 3′ termination region, wherein the 5′ regulatory region of the target expression cassette is activated by the first and second receptor polypeptides in the presence of one or more chemical ligands which are complementary to the ligand binding domain of the receptor polypeptides, whereby expression of the target polypeptide is accomplished. The method is useful for controlling various traits of agronomic importance, such as plant fertility.

The present invention relates to methods of modulating epithelial stem cell lineage by regulating the expression of Lef1 or a BMP inhibitor and / or the stability of β-catenin or the expression of a Wnt; regulating the expression or activity of GATA-3; or regulating BMPR1A activity either at the level of receptor expression or at the level of pathway activation. Methods of regulating E-cadherin, GATA-3, BMPR1A and HK1-hair keratin and methods of identifying agents which modulate the epithelial stem cell lineage are further provided. Such agents are useful for inhibiting or stimulating inner root sheath development or hair follicle formation.

Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

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 relates to novel antagonists to a B1-bradykinin (B1-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the B1 receptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B1-BK receptors in these two models. B1-BK antagonists abolished the vasocontraction induced by B1-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B1-antagonists are useful for treating any condition wherein B1-receptor is expressed, particularly during inflammation, and more particularly wherein B1-receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B1-receptor.

The invention discloses a method for editing a large white pig CD163 gene by using CRISPR / Cas9. The large white pig CD163 gene is edited by using the CRISPR / Cas9, the extracellular domain SRCR5 of a CD163 receptor is destroyed, the 7th exon DNA fragment of the CD163 gene is knocked out, and the nucleotide sequence of the 7th exon of the CD163 gene is represented by SEQ ID NO.1. The edited gene obtained by adopting the method can completely resist infection of PRRSV including a highly pathogenic strain HP-PRRSV, allows the cell surface CD163 receptor expression to be normal, and has normal other biological functions.

This invention relates to mutant G protein-coupled receptors with improved G-protein coupling and receptor response, yeast cells expressing such receptors, vectors useful for making such cells, and methods of making and using same.

This invention relates to compounds, compositions, and methods useful for modulating Vitamin D Receptor (VDR) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of Vitamin D Receptor gene expression and / or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of Vitamin D Receptor.

Provided is a composition and method for modulating serotonergic receptor expression, reducing anxiety-like behavior and stress-induced inflammatory response in a pediatric subject, the method including administering to the pediatric subject a nutritional composition including lactoferrin from a non-human source and a prebiotic composition including polydextrose and / or galactooligosaccharides. Further provided is a method for reducing constipation in a pediatric subject by providing a nutritional composition including lactoferrin from a non-human source and a prebiotic composition including polydextrose and / or galactooligosaccharides.

The invention provides a preparation method of bispecific chimeric antigen receptor gene modified natural killer cells, comprising the features: constructing a bispecific chimeric antigen receptor gene containing specific-binding signaling lymphocyte activation molecule family member 7 and fibronectin mutants, recombining the bispecific chimeric antigen receptor gene to a viral vector, transfecting with human natural killer cells, and highly expressing the bispecific chimeric antigen receptor gene, thus specifically binding tumor cells that express the signaling lymphocyte activation molecule family member 7 and fibronectin mutants, inhibiting expression of natural killer cell inhibitory receptors, and preventing immune escape of tumor cells; meanwhile, activating a first signal and a co-stimulatory signal to trigger toxic activity of the tumor cells, and great anti-tumor killing toxicity is shown in in-vivo and in-vitro experiments; the invention also provides a kit for the preparation of autologous natural killer cells through the above method, and with the kit, it is possible to highly express the bispecific chimeric antigen receptor gene and trigger great anti-tumor effect.

Relating to the fields of biotechnologies and gene therapy, the invention provides application of a gene modified mesenchymal stem cell in pulmonary fibrosis treatment. The gene modified mesenchymal stem cells are obtained through: in-vitro isolated culture and amplification of a mesenchymal stem cell (MSC) deriving from bone marrow and an umbilical cord, and recombinant adenovirus Ad-HGF mediated in-vitro modification of the MSC by a hepatocyte growth factor (HGF). By transplanting the gene modified MSC to a C57 mouse to intervene in radiation induced lung injury and fibrosis, exudation of a plurality proteins including albumin, IgM and the like from an alveolar space can be reduced, local inflammatory responses of the lung can be alleviated, and expression of TNF-alpha, soluble ICAM-1 and multiple factors is inhibited, expression of the profibrotic factor TGF-beta, the collagen gene col1 alpha 1 and col 3 alpha 1 can be inhibited, and pulmonary tissue collagen fiber deposition is reduced. The expression results of endogenous HGF and its receptor cmet show that endogenous HGF expression can be induced and endogenous MSC can home to injured parts. Therefore, the employment of HGF modified MSC in treatment of lung injury and fibrosis brought by various pathogenic causes is of great significance.

Novel imaging agents targeted to a lymph vascular cell receptor and a hyaluranon cell receptor are disclosed. The disclosed imaging agents incorporate biological molecules such as hyaluronic acid which bind to the receptors. Lymph vascular cell receptor expression may be related to the beginnings of tumor formation. As such, embodiments of the imaging agents may be used to stain lymph structures for detailed imaging of lymph architecture as well as serving as potential markers for tumor angiogenesis, tumor metastases, etc.

Herbal compositions having anti-adipocyte fatty acid-binding protein (aP2), anti-5-lipoxygenase-activating protein (FLAP) and anti-Cysteinyl Leukotriene (CysLT)-1 receptor expression activity contain an extract of Boswellia serrata. More particularly, these herbal compositions comprise an effective amount of an enriched Boswellia extract containing from 10% to 99% by weight of 3-0-acetyl-11-keto-β-boswellic acid; and an effective amount of a second extract selected from the group consisting of an extract of Aegle marmelos, an extract of Zingiber officinale, an extract of Garcinia mangostana, and mixtures thereof. These may be used in dietary supplements or pharmaceutical formulations for controlling diseases associated with or related to inflammation. These diseases in particular include respiratory disorders such as asthma, allergic rhinitis, hay fever, type-1 hypersensitivity and mild allergies. The compositions can also be useful for skin care.

The invention relates to an artificial transcription factor comprising a polydactyl zinc finger protein targeting specifically a receptor gene promoter fused to an inhibitory or activatory protein domain, a nuclear localization sequence, and a protein transduction domain. In particular examples these receptor gene promoters regulate the expression of the endothelin receptor A, the endothelin receptor B, the Toll-like receptor 4 or the high-affinity IgE receptor. Artificial transcription factors directed to the endothelin A or B receptors are useful in the treatment of diseases modulated by endothelin, such as cardiovascular diseases, and, in particular, eye diseases, e.g. retinal vein occlusion, retinal artery occlusion, macular edema, optic neuropathy, central serous chorioretinopathy, retinitis pigmentosa, Leber's hereditary optic neuropathy, and the like. Artificial transcription factors directed to the Toll-like receptor 4 or the IgE receptor are useful for the treatment of autoimmune disorders, and the like, and allergic disorders, respectively.

The present invention relates to methods for modulating the activity of one or more Vps10p-domain receptors selected from the group consisting of Sortilin, SorLA, SorCS1, SorCS2 and SorCS3, in an animal and methods for preparation of a medicament for the treatment of abnormal plasma lipid concentrations and associated diseases and / or disorders. The modulation is carried out by inhibiting or promoting the binding of ligands to the Vps10p-domain receptor. In vitro and in vivo methods for screening for agents capable of modulation of said Vps10p-domain receptor activity are also provided. The invention furthermore relates to methods of altering expression of said receptors in vivo.

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.

siRNA and antisense reagents capable of blocking expression of the IGF-1 receptor.

Provided is a composition and method for modulating serotonergic receptor expression, reducing anxiety-like behavior and stress-induced inflammatory response in a pediatric subject, the method including administering to the pediatric subject a nutritional composition including lactoferrin from a non-human source and a prebiotic composition including polydextrose and / or galactooligosaccharides. Further provided is a method for reducing constipation in a pediatric subject by providing a nutritional composition including lactoferrin from a non-human source and a prebiotic composition including polydextrose and / or galactooligosaccharides.

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 relates to a chimeric antigen receptor and an expression gene thereof, a double-antigen regulated type T cell modified by the chimeric antigen receptor, and application thereof. The expression gene of the chimeric antigen receptor comprises a first fusion protein expression gene and a second fusion protein expression gene, wherein the first fusion protein expression gene comprises a mucoprotein-1 antibody expression gene, a notch receptor expression gene and a Gal4-VP64 transcription activating protein expression gene which are sequentially connected; the second fusion protein expression gene comprises a Gal4-UAS promoter expression gene and an anti-mesothelin expression gene which are sequentially connected. By adopting the innovative design, the chimeric antigen receptor has the advantages that the chimeric antigen receptor can be successfully imported into the T cell to form the T cell modified by the chimeric antigen receptor; the immune reaction cannot be produced until the mucoprotein-1 and the anti-mesothelin signals simultaneously exist, so as to reach the controllable immune reaction of the chimeric antigen receptor, fewer side effects in treatment, and high specificity.

The invention provides pyrrolidine compounds, salts thereof, applications of the compounds or the salts thereof in nuclear magnetic probes and medicines, a reagent, and a medicine. The benzamide methylpyrrolidine compounds have a chemical structure represented by general formula (I); and in the formula (I), R<1> is selected from a methyl group, an ethyl group, a methoxy group, an ethoxy group and halogen, R<2> is selected from a methyl group, an ethyl group, a methoxy group, an ethoxy group and halogen, R<3> is selected from C1-5 alkyl groups and H, X<1> is selected from C1-10 alkylene groups or is deleted, X<2> is selected from -(CH2CH2O)n- (n is 1-5) or is deleted, X<3> is selected from C1-5 alkyl groups, X<4> is selected from oxygen, sulfur and a methylene group, and Ln is selected from Gd and Eu. The compounds have a gadolinium and europium chelating structure formed by combining with a dopamine D2 receptor and depending on intramolecular chelating groups, and specifically enhance the contrast of dopamine D2 receptor expression tissues on images in magnetic resonance imaging.

The method of the invention pertains to determining the signal transduction activity in a tissue section by immunohistochemistry techniques. The expression level of the receptor of interest is determined as well as the expression levels of one or more effector molecules of the receptor signal transduction pathway. Furthermore a combined ratio of expression levels of effector molecules in subcellular compartments with the receptor expression was found to have prognostic significance.

The invention concerns active substances modulating the expression of the receptors of the products of the POMC gene (MC-IR, MC-2R, and the μ opioid receptor), and possibly modulating the expression of POMC in cutaneous cells, notably to modulate the proliferation and differentiation of epidermal cells in order to re-epithelial, maintain innervation, irrigate the skin, or to fight against aging, or to modulate pigmentation independently or not of cutaneous aging. The invention also concerns a method of screening such active substances.

The present invention relates to methods for modulating the activity of one or more Vps10p-domain receptors selected from the group consisting of Sortilin, SorLA, SorCS1, SorCS2 and SorCS3, in an animal and methods for preparation of a medicament for the treatment of abnormal plasma lipid concentrations and associated diseases and / or disorders. The modulation is carried out by inhibiting or promoting the binding of ligands to the Vps10p-domain receptor. In vitro and in vivo methods for screening for agents capable of modulation of said Vps10p-domain receptor activity are also provided. The invention furthermore relates to methods of altering expression of said receptors in vivo.

The present invention relates to methods for modulating the activity of one or more Vps10p-domain receptors selected from the group consisting of Sortilin, SorLA, SorCS1, SorCS2 and SorCS3, in an animal and methods for preparation of a medicament for the treatment of mental and behavioral disorders. The modulation is carried out by inhibiting or promoting the binding of ligands to the Vps10p-domain receptor. In vitro and in vivo methods for screening for agents capable of modulation of said Vps10p-domain receptor activity are also provided. The invention further-more relates to methods of altering expression of said receptors in vivo.

The invention discloses a multifunctional targeting drug delivery system with combined action of chemotherapy and phototherapy and a preparation method thereof. The method comprises the following steps: preparation of drug-loaded nanoparticles; synthesis of HA-NH2; synthesis of DOX-ss-HA-NH2; and preparation of a targeting drug delivery system Ce6@PDA-HA-ss-DOX. The multifunctional targeting drugdelivery system disclosed by the invention has good biocompatibility, biodegradability and low toxicity, and can respond to the biological characteristics of low pH environment, high glutathione concentration and high CD44 receptor expression of tumor cells to release drugs. The chemotherapy is carried out together with photothermal therapy and photodynamic therapy so as to obviously improve the killing effect on the tumor cells, and to provide a better treatment method for tumor.