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

Image Number 16 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
Crosslinked core/shell polymer particles
Digital broadcast receiver and method for processing caption thereof
Method and apparatus for generating images using a color field sequential display
Storage device performance alignment notification
Vacuum cleaner filter adapter ring
Organic metal complex and its use in organic electroluminescent device
Multicolored light converting LED with minimal absorption
  Randomly Featured Patents
Document authentication using a mark that is separate from document information
Method and system for improving performance of broadcast/multicast transmissions
Combined stream auxiliary copy system and method
Electric power steering system
Die-mounting paddle for mechanical stress reduction in plastic IC packages
Preparation of sulfur-containing organosilicon compounds
Method of making printed circuit boards
Loudspeaker wall bracket
Preparation of trimethylaluminum
Gainboost biasing circuit for low voltage operational amplifier design