摘要:
The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要:
Peptide antagonists of &agr;-melanocyte stimulating hormone are disclosed, together with methods of inhibiting the effects of &agr;-melanocyte stimulating hormone on cells or tissues sensitive to that hormone. In particular, methods for lightening the pigmentation of skin and for treating malignant melanoma, as well as kits for practicing the invention are also disclosed.
摘要:
The invention exploits the evolutionary principles responsible for the development of the broad spectrum general odorant detector system, to create a cell-surface receptor based system capable of detecting and discriminating between thousands of chemicals. This is accomplished by subjecting a defined set of cell-surface receptors such as G-protein coupled receptors, tyrosine kinase receptors, and/or ion channels, to the types of evolutionary forces that have created the array of approximately 1,000 natural receptors used in general olfaction by higher animals. This goal is further accomplished by a ‘directed evolution-in-a-test-tube’ method, imposing very high rates of mutation and extremely strict selection criteria to create a sensor. The novel sensor of the present invention is selected using a sensitive melanophore-based functional bioassay.
摘要:
A method for detecting the interaction between an oligomeric molecule and a target is provided. A plurality of beads is applied to a substrate, each bead having associated therewith multiple copies of only a single oligomeric molecule. The beads are substantially spaced-apart from one another and are substantially immobilized on the substrate. Conditions are applied such that a substantial portion of the multiple copies associated with each bead can disassociate from and diffuse into the substrate, the substrate constructed and arranged to permit only substantially localized diffusion. A localized signal occurring as a result of the diffusion is detected. Coated beads and libraries of coated beads also are provided.
摘要:
A method for identifying a chemical that acts as an agonist for a G-protein coupled cell surface (GPC) receptor. The method comprises introducing to test cells of a pigment cell line capable of dispersing or aggregating their pigment in response to a specific stimulus and expressing an exogenous clone coding for the GPC receptor, a stimulant that sets an initial state of pigment disposition wherein the pigment is aggregated within the test cells if activation of the exogenous GPC receptor induces pigment dispersion, or introducing a stimulant that sets an initial state of pigment disposition wherein the pigment is dispersed within the test cells if activation of the exogenous GPC receptor induces pigment aggregation; contacting the test cells set in an initial state of pigment disposition with the test chemical; and determining whether the pigment disposition in the test cells treated with the chemical is changed from the initial state of pigment disposition, wherein a change in pigment disposition observed in the test cells expressing the exogenous GPC receptor indicates that the chemical is an agonist for the exogenous GPC receptor.
摘要:
A method for identifying a chemical that acts as an agonist for a G-protein coupled cell surface (GPC) receptor. The method comprises introducing to test cells of a pigment cell line capable of dispersing or aggregating their pigment in response to a specific stimulus and expressing an exogenous clone coding for the GPC receptor, a stimulant that sets an initial state of pigment disposition wherein the pigment is aggregated within the test cells if activation of the exogenous GPC receptor induces pigment dispersion, or introducing a stimulant that sets an initial state of pigment disposition wherein the pigment is dispersed within the test cells if activation of the exogenous GPC receptor induces pigment aggregation; contacting the test cells set in an initial state of pigment disposition with the test chemical; and determining whether the pigment disposition in the test cells treated with the chemical is changed from the initial state of pigment disposition, wherein a change in pigment disposition observed in the test cells expressing the exogenous GPC receptor indicates that the chemical is an agonist for the exogenous GPC receptor.
摘要:
Disclosed is a therapeutic device including an optical source including means for generating ultraviolet (UV) radiation, and a light delivery apparatus. The light delivery apparatus includes a body member and a plurality of optical fibers extending therefrom. Each of the optical fibers includes a proximal tip affixed to the body member, a distal tip at the end of the fiber opposite the proximal tip, and means for coupling the generated radiation from the proximal tips of the fibers through the fibers, and to the distal tips. The distal tips are characterized by a radius of curvature in the range 0.25 to 2.0 mm. The coupling means includes a flexible central core disposed within a flexible outer cladding. The central core has a diameter in the range of 0.1 mm to 1.0 mm, and the cladding has a refraction less than the index of refraction of the core.
摘要:
Purified DNA comprising a sequence encoding chrysoptin.Chrysoptin can be used to alter the hemodynamic or hemostatic properties of an animal's blood by administering to the animal an effective amount of chrysoptin.