54 results about "Retinoid X receptor" patented technology

The present invention relates to a method of treatment of cachexia in a subject in need of treatment. More specifically, the present invention relates to the use of retinoid compounds that act on retinoid X receptors (RXRs) for the treatment of cachexia in a subject in need of treatment. The cachexia is associated with, in other words a complication of, a primary disease, condition or disorder. Primary diseases, conditions and disorders include, but are not limited to, cancer, AIDS, liver cirrhosis, diabetes mellitus, chronic renal failure, chronic obstructive pulmonary disease, chronic cardiac failure, immune system diseases (e.g., rheumatoid arthritis and systemic lupus erythematosus), tuberculosis, cystic fibrosis, gastrointestinal disorders (e.g., irritable bowel syndrome and inflammatory bowel disease), Parkinson's disease, anorexia nervosa, dementia, major depression, an aged condition and sarcopenia.

Methods of stimulating or increasing differentiation to regulatory T cells, cultures of regulatory T cells and methods of reducing or decreasing an immune response, inflammation or an inflammatory response, among other things, are provided. Methods include, among other things, contacting blood cells or T cells with an amount of TGF-beta or a TGF-beta analogue and a retinoic acid receptor agonist, or an amount of a retinoid X receptor (RXR) or peroxisome proliferator activated receptor-gamma (PPARgamma) agonist, sufficient to stimulate or increase differentiation to regulatory T cells. Cultures of regulatory T cells include T cells that express a marker associated with regulatory T cells, such as cultures in which regulatory T cells represent, for example, 30% or more of the total number of cells in the culture.

This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to a novel ecdysone receptor / chimeric retinoid X receptor-based inducible gene expression system and methods of modulating gene expression in a host cell for applications such as gene therapy, large-scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.

This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to a novel ecdysone receptor / chimeric retinoid X receptor-based inducible gene expression system and methods of modulating gene expression in a host cell for applications such as gene therapy, large-scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.

This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to a novel ecdysone receptor / invertebrate retinoid X receptor-based inducible gene expression system and methods of modulating gene expression in a host cell for applications such as gene therapy, large-scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

A polypeptide is identified as being functionally included in a signal transduction pathway having a biological effect. Contemplated polypeptides are different from a retinoic acid receptor, a retinoid X receptor, or a cellular retinoic acid binding protein, however bind a retinoid or retinoid metabolite, and binding of the retinoid or retinoid metabolite lead to a modulation of the biological effect. In particularly contemplated methods, a retinoid or retinoid metabolite is administered to a cell or mammal in a concentration effective to modulate the biological effect.

Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R1 is selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group and an aryl group. R2 is selected from the group consisting of an alkoxy group, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. W is NR3 or CR3; and R3 is selected from a hydrogen, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. X1 and Y1 are selected from CH or N. X2 and Y2 are selected from CH, CR4 or N. R4 is selected from an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen, a nitro group and an amino group. Z is selected from a carboxylic acid, a carboxylate ester or a hydroxamic acid, which is bound directly or via an alkyl group, an alkenyl group or an alkynyl group.]

The present invention is directed to compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof: (I). The invention is also directed to pharmaceutical compositions, methods of use and methods of making compounds represented by Structural Formula (I) and pharmaceutically acceptable salts, solvates and hydrates thereof.

Combination therapy comprising RXR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.

Application of triptolide, triptolide derivant and triptolide analogue in preparation of antitumor drugs relates to triptolide. A method for utilizing tRXRZ (truncated retinoid X receptor) alpha as a target spot to screen the triptolide, the triptolide derivant and the triptolide analogue which is tripdiolide includes a following step of acting the triptolide into a tumor cell line containing the tRXR alpha so as to obtain the triptolide, the triptolide derivant and the triptolide analogue which are screened by utilizing the tRXR alpha as the acting target spot. After the triptolide, the triptolide derivant and the triptolide analogue which are screened by utilizing the tRXR alpha as the acting target spot act to the tumor cell line, the tRXR alpha can be targeted, mutual actions of the tRXR alpha and p85 can be inhibited, then AKT (threonine kinase) activation induced by TNF (tumor necrosis factor) alpha can be inhibited, a caspase 8 apoptosis signal channel induced by the TNF alpha can be activated, and cancer cell apoptosis can be induced.

The present invention describes genomic biomarkers that have been discovered to correlate with varied individual responses (efficacy, adverse effect, and other end points) to therapeutic retinoid X receptor modulator, such as bexarotene, in treating diseases such as, non small cell lung cancer. The newly discovered biomarkers and others in linkage disequilibrium with them can be used in companion diagnostic tests which can help to predict drug responses and apply drugs only to those who will be benefited, or exclude those who might have adverse effects, by the treatment.

The invention discloses multiple-target-point tamibarotene derivatives, a preparation method and purposes thereof. More specifically speaking, the invention provides a compound represented by a structural general formula (I), wherein the definition of R is referred to an instruction book; the derivatives are multiple-target-point compounds which are obtained by connecting tamibarotene as an RAR (retinoic acid receptors) excitant with various histone deacetylase inhibitors, various RXR (retinoid X receptors) excitants or other pharmacophoric groups directly through ester bonds or amido bonds or indirectly through connecting groups; and the derivatives are suitable to be used as antitumor drugs to be used for treating various malignant tumors, and are particularly suitable for treating various leukemia.

The present invention provides methods of treating proteinuria, and treating renal disorders associated with proteinuria, the methods generally involving administering to an individual having such a disorder an effective amount of retinoic acid receptor agonist or a retinoid X receptor agonist.

Disclosed is a compound represented by the general formula shown below, which can bind to a retinoid X receptor (RXR), which is one of nuclear receptors, and exhibit an agonistic or antagonistic action. [Wherein, R1 is selected from the group consisting of an alkyl group, an alkenyl group, an alkynyl group and an aryl group. R2 is selected from the group consisting of an alkoxy group, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. W is NR3 or CR3; and R3 is selected from a hydrogen, an alkyl group, an alkenyl group, an alkynyl group and an aryl group. X1 and Y1 are selected from CH or N. X2 and Y2 are selected from CH, CR4 or N. R4 is selected from an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogen, a nitro group and an amino group. Z is selected from a carboxylic acid, a carboxylate ester or a hydroxamic acid, which is bound directly or via an alkyl group, an alkenyl group or an alkynyl group.]

The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a retinoid X receptor as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

Nucleic acids encoding NRIF3 are described. Polypeptides having amino acid sequences of NRIF3 proteins are also provided. A method is also provided for isolating and cloning NRIF3 cDNA. NRIF3 is useful in development / implementation of high throughput screens to identify novel thyroid hormone receptor (TR) and retinoid X receptor (RXR) agonists and antagonists. Methods are also provided for identifying compounds that directly interfere with the interaction of NRIF3 and TR or RXR. Finally, therapies based on modulation of NRIF3 activity are disclosed.

Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

By using a fluorescent ligand for a retinoid X receptor (RXR), said ligand being indicated by one of the following formulas (1)-(3), an evaluative test of ability to bind with RXR can be easily performed. (In the formulas, R1 is methyl, alkoxyl, or styryl, R2 is hydroxyl, alkoxyl, or alkyl amino, A is N or CH, B is NH or O, R3 is isopropyl or tertiary butyl, and R4 is isopropyl or isobutyl.)

The invention relates to the field of biological medicine, in particular to an application of RXR (Retinoid X receptor) in screening medicine for treatment of vesicular stomatitis virus. Not only the application of RXR (Retinoid X receptor) in screening the medicine for treatment of vesicular stomatitis virus but also a method for building an infection cell model of vesicular stomatitis virus caused by over-expression of RXR are provided; besides, it is found that COX infection pathway plays a key role in host defense to vesicular stomatitis virus in a RXR-dependent manner; and further, application of MHV68 in screening the medicine for treatment of vesicular stomatitis virus is verified.

This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to a novel ecdysone receptor / invertebrate retinoid X receptor-based inducible gene expression system and methods of modulating gene expression in a host cell for applications such as gene therapy, large-scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.

In accordance with the present invention, there are provided methods to modulate processes mediated by retinoid receptors, employing high affinity, high specificity ligands for such receptors. In one aspect of the present invention, there are provided ligands which are more selective for the retinoid X receptor than is retinoic acid (i.e., rexoids). In another aspect of the present invention, alternative ligands (other than retinoic acid) have been discovered which are capable of inducing retinoic acid receptor mediated processes. In yet another aspect, methods have been developed for the preparation of such retinoid receptor ligands from readily available compounds.

PCT No. PCT / US94 / 05746 Sec. 371 Date Jun. 27, 1995 Sec. 102(e) Date Jun. 27, 1995 PCT Filed May 18, 1994 PCT Pub. No. WO94 / 26100 PCT Pub. Date Nov. 24, 1994The present invention provides mice which are deficient in the normal expression of one or more members of the RAR or RXR class of receptors, mice which are heterozygous for such deficiency, and to cell lines, preferably pluripotent or totipotent cell lines, which are heterozygous or homozygous for such deficiency. The present invention further provides the use of any of the above mice and cell lines in situations where the absence of at least one RAR or RXR receptor(s), or the normal expression thereof, is desirable.

The present invention provides methods for treating cancer using modulators of retinoid X receptor gamma (RXRG). The ability of RXRG antagonists to disrupt the association of complexes comprising RXRG is demonstrated.

The invention provides an alkannin and a derivative thereof that are used for preparing drugs for adjusting and controlling the activity and the function of a retinol X receptor, the retinol X receptor is used for screening the alkannin and the derivative thereof and the retinoid X receptor is served as a receptor target for guiding the structure modification of the alkannin and the derivative thereof. The retinol X receptor provided by the invention is used as the receptor target, which can be used for screening the alkannin and the derivative thereof to obtain a compound drug for adjusting the activity of RXR Alpha and also can be used for guiding the structure modification of the alkannin and the derivative thereof so as to obtain a compound with higher activity.

Methods and compositions for the treatment of anti-estrogen resistant breast cancer using retinoid compounds which are modulators of Retinoid X Receptors.

The present provides compounds capable of modulating IL-4 receptor-mediated IgE production, as well as IL-4 induced processes associated therewith, methods and kits for identifying such compounds that utilize a retinoid X receptor as a surrogate analyte and methods of using the compounds in a variety of in vitro, in vitro and ex vivo contexts.

The present invention relates to microbial infection, and in particular, the reduction of apoptosis associated with microbial infection, the screening of Liver X Receptor agonist and / or Retinoid X Receptor agonist that reduce apoptosis, and the treatment and analysis of microbial infection in vivo. In one embodiment, the present invention relates to Liver X Receptor agonist and / or Retinoid X Receptor agonist including but not limited to an agonist increasing the activity of Liver X Receptor and / or Retinoid X Receptor.

Embodiments provided herein relate to methods and compositions for treating cancer. Some embodiments relate to certain compounds having activity against retinoid X receptor-alpha (RXRα). Some embodiments included designing or identifying a compound that binds to human RXRa protein, such as the ligand binding domain (LBD) of human RXRa protein.