Resources Contact Us Home
Systems for sensitive detection of G-protein coupled receptor and orphan receptor function using reporter enzyme mutant complementation

Image Number 11 for United States Patent #6800445.

Methods for detecting G-protein coupled receptor (GPCR) activity; methods for assaying GPCR activity; and methods for screening for GPCR ligands, G-protein-coupled receptor kinase (GRK) activity, and compounds that interact with components of the GPCR regulatory process are described. Included are methods for expanding ICAST technologies for assaying GPCR activity with applications for ligand fishing, and agonist or antagonist screening. These methods include: engineering seronine/threonine phosphorylation sites into known or orphan GPCR open reading frames in order to increase the affinity of arrestin for the activated form of the GPCR or to increase the reside time of arrestin on the activated GPCR; engineering mutant arrestin proteins that bind to activated GPCRs in the absence of G-protein coupled receptor kinases which may be limiting; and engineering mutant super arrestin proteins that have an increased affinity for activated GPCRs with or without phosphorylation. These methods are intended to increase the robustness of the GPCR/ICAST technology in situations in which G-protein coupled receptor kinases are absent or limiting, or in which the GPCR is not efficiently down-regulated or is rapidly resensitized (thus having a labile interaction with arrestin). Included are also more specific methods for using ICAST complementary enzyme fragments to monitor GPCR homo- and hetero-dimerization with applications for drug lead discovery and ligand and function discovery for orphan GPCRs.

  Recently Added Patents
Hydrogen generation device and fuel cell system
Resin composition and display device using the same
Systems and methods for facilitating communication with foundation fieldbus linking devices
Systems and methods for detecting and rejecting defective absorbent articles from a converting line
Vehicle inertial sensor systems
Generator with a segmented stator
Magnetic impedance element and magnetic sensor using the same
  Randomly Featured Patents
Lock alignment tool
Scavenging phosphorus, sulfur, and lead from combustion exhaust using tungsten compounds and lubricant
Air grain conveyor system
Systems and methods for immobilization using a compliance signal group
Electromotive curtain for drying clothes
Multitest-tube for clinical chemistry analysis for several simultaneous tests
Device for transferring crosswound coils from a crosswound coil delivery location of a textile machine into a box-shaped conveyance
Method and apparatus for measuring a characteristic of a plastic container
Riveting system
Digital logic module for mounting in a control panel