摘要:
A method of identifying an agent which modulates 2-oxoglutarate dependent oxygenase activity, the method comprising contacting a 2-oxoglutarate dependent oxygenase and a test agent in the presence of a substrate comprising one or more ankyrin repeat, or fragment thereof, in conditions under which the substrate is hydroxylated in the absence of the test agent; and determining hydroxylation of the substrate.
摘要:
The invention provides isolated nucleic acid molecules, host cells that contain an isolated nucleic acid molecule, and substantially pure polypeptides. For example, the invention provides isolated nucleic acid molecules that encode polypeptides having mu3 opiate receptor activity, host cells that contain an isolated nucleic acid molecule that encodes a polypeptide having mu3 opiate receptor activity, and substantially pure polypeptides that have mu3 opiate receptor activity. In addition, the invention provides methods and materials for identifying mu3 opiate receptor agonists and antagonists.
摘要:
The present invention provides assays for determining the activity of an enzyme that uses or produces prostaglandin endoperoxide H2 (PGH2), methods of using the assays to screen for potential modulators of such enzymes, and kits for practice of the assays.
摘要:
The present invention relates to a method of identifying an agent (e.g., petide, small molecule) that alters (partially, completely ) the activity (function, expression) of HIF. In one embodiment, the method of identifying an agent that alters (e.g., inhibits, enhances) the activity of HIF comprises contacting a molecule in the HIF biosynthetic pathway (e.g., a precursor of HIF, such as a steroid precursor; an enzyme) with an agent to be assessed and determining whether the activity of the molecule (function, expression) is altered in the presence of the agent when compared to the activity of the molecule in the absence of the agent. The invention is also related method of treatment using such agents; and methods of monitoring the biosynthetic pathway of OLC/HIF. In particular, the invention is related to agent, treatments, and diagnostics for diseases such a hypertension and heart failure.
摘要:
A method for measuring human CYP3A inducibility upon administration of a test drug, characterized in that a non-human animal to which a test drug is administered or a population of human cells cultured in a medium containing a test drug is infected with viruses (A) and (B); virus (A) being an adenovirus which is used as a vector and engineered by incorporating thereto a detectable reporter gene and at least 3 human PXR binding regions falling within an untranslated region of a human CYP3A gene, and virus (B) being an adenovirus which is used as a vector and engineered by incorporating thereto a human PXR cDNA; and subsequently expression level of the reporter gene is determined in the non-human animal or the cultured human cells. The present invention ensures convenient and accurate evaluation of human CYP3A inducibility upon administration of a test drug to a human subject, providing accurate evaluation in terms of the efficacy of the test drug, occurence of side effects, disappearance of the drug effect, etc.
摘要:
The discovery that CYP1B1 protein is detectable in a wide range of human cancers of different histogenetic types, but is not detectable in non-cancerous tissues, gives rise to diagnostic methods for detecting tumours based on this protein as a marker, and to the possibility of tumour therapies involving the protein. A diagnostic method may include the steps of: (a) obtaining from a patient a tissue sample to be tested for the presence of cancer cells; (b) producing a prepared sample in a sample preparation process; (c) contacting the prepared sample with an antibody that reacts with human CYP1B1 protein; and (d) detecting binding of the antibody to CYP1B1 protein in the prepared sample.
摘要:
The present invention relates to methods and compositions for modulating genes which are controlled by the FXR orphan nuclear hormone receptor. In a preferred embodiment the method involves modulation of the gene encoding Cyp7a, the enzyme responsible for a major pathway in the elimination of cholesterol. The invention also relates to methods for screening compounds which bind to and activate or inhibit the FXR nuclear hormone receptor.