63 results about "Aryl hydrocarbon receptor" patented technology

Compounds and compositions including 6-bromo-indirubin, 5-amino-indirubin and N-methyl-indirubins and related indirubin derivatives are provided that are useful as selective modulators of glycogen synthase kinase-3, cyclin-dependent protein kinases or aryl hydrocarbon receptors. Methods of inhibiting or modulating cell growth or cell cycling are provided using the compounds of the invention. In other aspects, compounds and methods for the treatment of protozoan-mediated diseases, Alzheimer's disease and diabetes are provided.

The invention relates to application of evodiamine in preparing a medicine for inhibiting an aryl hydrocarbon receptor. The medicine for inhibiting the aryl hydrocarbon receptor has the anti-tumor and immunoregulation effects by inhibiting the aryl hydrocarbon receptor, wherein the tumors are breast cancer, endometrial cancer, prostate cancer, lung cancer, gastric cancer, liver cancer, colon cancer and the like; and the immunoregulation is performed aiming at various inflammatory related diseases, such as sepsis, sepsis shock, rheumatic arthritis, rheumatoid arthritis, asthma, acute and chronic glomerulonephritis, and systemic lupus erythematosus. In the application, the evodiamine is an alkaloid component in a traditional Chinese medicine, namely medicinal evodia fruit, has the molecular formula of C19H17NO3 and the molecular weight of 303.4Da, is insoluble, can be dissolved in organic solvents such as dimethyl sulfoxide, ethanol, diethyl ether and chloroform, and has the melting point of 278 to 279 DEG C.

Provided herein are novel agents that modulate AhR activity for use in therapeutic compositions and methods thereof for inhibiting cancer cell proliferation and tumor cell invasion and metastasis. The agents comprise AhR inhibitors or non-constitutive AhR agonists of Formula (I) and (II) for the inhibition of cancer cell growth and parameters that characterize tumor metastasis, such as tumor cell invasiveness.

The invention provides neuron-derived cells obtained by transfecting a receptor-expressing nucleic acid having an aryl hydrocarbon receptor gene, wherein outgrowth of neurites is not observed without adding a substance for the aryl hydrocarbon receptor, and outgrowth of neurites is observed by adding the substance for the aryl hydrocarbon receptor. The invention also provides a method for determining the presence of neurotoxicity of a test substance, a method for acquiring a marker for determining the presence of neurotoxicity of the test substance, a method for acquiring a marker for neurological dysfunction, and a method for determining the effect of the test substance on neurological dysfunction using such cells.

The present invention relates to a method of screening compounds for binding to hsp90 by exposing a compound to hsp90 or a polypeptide fragment thereof containing amino acid residues 538-728 of the full length protein and determining whether the compound binds to hsp90 of the polypeptide fragment thereof. Also disclosed is a method of screening compounds for inhibition of hsp90 activity. The present invention further relates to a method of screening compounds as a cancer therapeutic and a method of treating cancerous conditions. Also disclosed is a method of inhibiting transcription-inducing activity of an aryl hydrocarbon receptor in a cell and a method of modifying expression of a gene that is-activated by an aryl hydrocarbon receptor.

A previously unknown T cell receptor (TCR) activation pathway dependent on the aryl hydrocarbon receptor conferring resistance to calcineurin inhibitors and mTOR inhibitors is disclosed, including application of this pathway to the diagnosis and treatment of certain disease states refractory to treatment with calcineurin inhibitors. This alternative TCR activation pathway uniquely exists in a subset of CD8 T cells expanded in the setting of chronic rejection or rheumatoid arthritis. Expansion of this newly discovered calcineurin and mTOR inhibitor resistant CD8 T cell subset in humans can be quantified by measuring levels of certain biomarkers in the circulating CD8 T cell pool, such as Pla2g4a, to diagnose disease states mediated thereby. Additionally, methods for diagnosing ongoing active inflammation mediated by this resistant CD8 T cell subset in either chronic rejection or rheumatoid arthritis are provided, which comprise measuring levels of the biomarker Scin in the circulating CD8 T cell pool.

Compositions and methods for treating skin conditions, ailments or diseases, such as autoinflammatory skin diseases such as psoriasis, dermatitis, pyoderma gangrenosum, palmoplantar pustulosis, prurigo nodularis and/or hidradenitis suppurativa, are described. The compositions comprise an agent that modulates the aryl hydrocarbon receptor, in particular an agent that agonizes the receptor. In one embodiment, the agent is indigo or a derivative of indigo, such as indirubin.

The present invention provides compounds of the following structure,

methods of using such compounds, and pharmaceutical compositions containing such compounds. In addition, this invention provides methods for the treatment and/or prevention of disease states mediated by Aryl Hydrocarbon receptor pathways.

The invention provides a starch-indolic acid derivative, a preparation method and application thereof, and relates to the technical field of modified starch. According to the invention, the starch-indolic acid derivative is esterified starch generated by esterification reaction of starch and indolic acid under the action of a condensing agent and and alkali, has relatively high resistance, can resist degradation of the stomach and the small intestine, can release indolic acid beneficial to intestinal health through fermentation of intestinal flora after reaching the colon part, has obvious advantages compared with traditional administration modes such as intragastric administration, intraperitoneal injection and the like, and can obviously increase the content of indolic acid in colon and hepatic portal venous blood; and indoleic acid can activate an aromatic hydrocarbon receptor to play an immunoregulation role, and the indoleic acid and the regulation role of short-chain fatty acid released by fermentation of starch with intestinal flora are superposed, so that a product which synergistically plays the immunoregulation role through a plurality of immune system signal pathways is provided.

Pharmaceutical formulation comprising at least one aryl hydrocarbon receptor ligand and at least one cyclodextrin for the prevention and/or treatment of carcinomas, preferably squamous cell carcinomas, more preferably oral squamous cell carcinomas.

The present invention provides freebase and salt forms, and compositions and methods thereof, useful for treating various conditions in which the aryl hydrocarbon receptor (AHR) is implicated, by the administration of small molecule therapeutics which act as inhibitors of AHR.