Resources Contact Us Home
Browse by: INVENTOR PATENT HOLDER PATENT NUMBER DATE
 
 
Systems for sensitive detection of G-protein coupled receptor and orphan receptor function using reporter enzyme mutant complementation










Image Number 14 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
Electrical conduit containing a fire-resisting thermoplastic composition
Apparatus, method and program for image receipt, processing, conversion, and delivery to and from a plurality of external apparatuses
Method and CTDevice for computer tomographic spiral scanning of a patient
Taste receptors of the T1R family from domestic cat
Adsorptive molded parts and the use thereof
Fluid conduit with PTC fabric heating
Sub-LUN input/output profiling for SSD devices
  Randomly Featured Patents
Steering force control apparatus for power steering system
Holster for personal security alarm
Remote initiator for the remote initiation of explosive charges
Tilt-telescope steering column
Electrical connector housing
1-cycloalkyl-1,8-naphthyridin-4-one derivative as type IV phosphodiesterase inhibitor
Circuit, disk controller and method for calibrating a high precision delay of an input signal
Memory system and method for protecting the contents of a ROM type memory
Tool positioning pad
Method and apparatus for generating high-density uniform plasma