52 results about "Orphan receptor" patented technology

Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor γ (RORγ) activity. This modulation has numerous effects, including inhibition of T_H-17 cell function and/or T_H-17 cell activity, and inhibition of re-stimulation of T_H-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of RORγ results in stimulation of T_H-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).

Mitogen induced nuclear orphan receptor (MINOR) is described as inducing apoptosis in dendritic cells (DCs). Downregulation of its expression results in a downregulation of apoptosis. A novel approach of inhibiting DC apoptosis is described employing small interfering RNA (siRNA) that targets MINOR. Improved DC-based vaccines exhibiting longer lifespan of DCs, increased potency of DCs, and enhanced immunogenicity are described.

Disclosed are substituted benzene and the application thereof to be used as agonist for receptor TR3, relating to substituted benzene. The invention provides a substituted phenol derivative compound and the application thereof to be used as agonist for orphan receptor TR3, in particular to the application in preparing the medicine for curing hypoglycemia and diseases related to abnormal apoptosis of cells, such as cancer. The substituted benzene and the substituted phenol derivative compound are respectively denoted by structural formula I and structural formula II; wherein R1 is nitrophthalimides or other alcoxyl-acyl or alcoxyl-acyl-alkyl, R2 is n-octanoyl, or other alkyl-acyl, or alkyl-acyl-alkyl, or alkyl, and R3, R4, R5 and R6 are H, OH, NH2 or halogen atoms.

The present invention makes available rapid, effective assays for screening and identifying pharmaceutically effective compounds that specifically interact with and modulate the activity of a cellular receptor or ion channel. The subject assays enable rapid screening of large numbers of polypeptides in a library to identify those polypeptides which induce or antagonize receptor bioactivity. The subject assays are particularly amenable for identifying agonists and antagonists for orphan receptors. In particular the present invention makes available novel ligand agonists of human formyl peptide receptor like-1 (FPRL-1) receptors. These novel ligand agonists are used in the assays of the invention to identify modulators of FPRL-1 receptor.

The invention relates to medical therapy using an agonist of the retinoic acid receptor-related orphan receptor gamma (ROR gamma) and provides adoptive cellular therapies using an agonist of ROR gamma, populations of lymphocyte cells that have been exposed to an agonist of ROR gamma, populations of dendritic cells that have been exposed to an agonist of ROR gamma, pharmaceutical compositions, and methods for enhancing therapeutic effects of lymphocyte cells and/or dendritic cells in a patient by administering an agonist of ROR gamma to a patient.

The present invention aims at providing a method of determining a ligand to an orphan receptor. Specifically, the present invention provides a method of determining a ligand to a receptor protein, to which no ligand has been determined, which comprises using a fusion protein of the receptor protein and a fluorescent protein.

The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.

The present invention relates to a compound which can be used as a retinoid-related orphan receptor γ (RORγ) modifier, a pharmaceutical composition of said compound, the use of said compound in the manufacture of pharmaceuticals, and a method for using said compound for treatment and/or prophylaxis of a RORγ-mediated disease in a mammal (especially a human). The compound has the structural formula I.

The invention relates to antibodies, and in particular, to antibodies exhibiting specificity for Receptor tyrosine kinase-like Orphan Receptors (ROR), and to uses thereof for example in the treatment of cancer. The invention extends to polynucleotide and polypeptide sequences encoding the antibodies, and therapeutic uses thereof, and to diagnostic kits comprising these molecules. The invention also extends to antibody-drug conjugates and to uses thereof in therapy.

The invention relates to polypeptides derived from the retinoic acid-related orphan receptor (ROR) in mammals, characterized in that they are delimited in their N-terminal extremity by an amino-acid located between positions 1 to 209, and in their C-terminal extremity by an amino-acid located between positions 450 to 452 of the rat RORbeta, alpha, or gamma, or by an amino-acid located at corresponding positions in nuclear receptor ROR of other subtypes than alpha, beta and gamma, and/or of the other mammals. The invention also relates to the use of these polypeptides, or of the molecular complexes or the crystals containing them, for carrying out:-a process for the screening of a ROR-LBD ligand which is an agonist, or an antagonist of said receptor,-or a process for the analysis of the tridimensional structure of the complexes formed with said polypeptides, molecular complexes or crystals and a particular compound.

The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ

The present invention relates to novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.

Provided herein are compounds of the formula (I):

as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.

In one aspect, the present disclosure describes new estrogen receptor-related orphan receptor (EER) inverse agonist compounds. Also described are pharmaceutical formulations, methods of synthesis and uses thereof.

Described is a method of identifying antibodies against hitherto unknown ligands of orphan receptors or other orphan ligands, i.e., receptors or other ligands where the counter-ligand has not yet been identified. The availability of antibodies binding to the unknown ligand significantly facilitates their isolation and characterization, and the identified antibodies can themselves be useful for treating patients with cancer or autoimmune diseases, or other disorders. An exemplary embodiment provides for a method designated Identification of Therapeutic Antibodies by Competitive Screening (ITACS). Described are also fusion proteins comprising a soluble portion of an orphan receptor, such as NKp30, and the Fc portion of an antibody. The fusion proteins typically comprise a Flexible Transmembrane Linker (FTL), i.e., a linker comprising a portion of a transmembrane domain of the orphan receptor.

The invention discloses a Schistosoma japonicum recombinant antigen. The recombinant antigen is prepared through expressing a recombinant vector containing first extramembrane fragment gene at the N-end of a Schistosoma japonicum trispanning orphan receptor. The invention also discloses a preparation method of the Schistosoma japonicum recombinant antigen, and an application of the Schistosoma japonicum recombinant antigen in preparation of schistosomiasis prevention or treatment vaccines or drugs. The Schistosoma japonicum recombinant antigen in mouse immunization experiments can induce generation of anti-recombinant antigen specific IgG, IgG1 and IgG2a antibodies and allows the antibodies to reach a high level, and the Schistosoma japonicum recombinant antigen in animal protection experiments induces the worm reduction rate of 32.4% and the ovum reduction rate of 41.41%, so the recombinant antigen is suitable for being used as an anti-schistosomiasis candidate vaccine, and has very good application prospect.

Provided herein are compounds of the formulas (I) and (II):

as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.

The invention relates to an anticancer application of sesquiterpene, particularly provides application of sesquiterpene ths-cy-7 in preparing anticancer drugs and application of orphan receptor Nur77 as a target in screening marine living resources. The sesquiterpene ths-cy-7 can induce apoptosis of cancer cells and expression of orphan receptor Nur77, and the apoptotic effect on cancer cells is dependent on the extranuclear expression of Nur77. The sesquiterpene ths-cy-7, as a regulatory factor targeting Nur77 apoptotic pathway, becomes a very effective therapeutic drug on cancer. The anticancer drugs use the orphan receptor Nur77 as an action target.

Provided herein are compounds of the formulas (I) and (II):

as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.

Provided herein are compounds of the formulas (I) and (II):

as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.

Provided herein are compounds of the formula (I):

as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.

The present invention relates to tetrahydro-tetrazolo[1,5-a]pyrazine compounds of formula (I), wherein R¹ denotes —R³, —CH₂—R³ or —CO—R³; R² denotes Ar², Hetar² or C_3-7-cycloalkyl; and R³ denotes Ar³, Hetar³ or C_3-7-cycloalkyl. These compounds are useful for inhibiting the retinoid-related orphan receptor γ (ROR γ, ROR-gamma) and for the prevention and/or treatment of medical conditions affected by ROR γ activity such as rheumatoid arthritis, multiple sclerosis, psoriasis, ulcerative colitis, asthma, autoimmune hepatitis or type 1 and type 2 diabetes.