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

Image Number 10 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
System and method for determining payroll related insurance premiums
Method and apparatus for visual neural stimulation
Compound semiconductor device and manufacturing method therefor
Driver circuit for driving semiconductor switches
Method and apparatus for executing load distributed printing
Methods and apparatus for achieving multiple bit rates in passive optical networks
Image forming apparatus and warming up method thereof
  Randomly Featured Patents
Network router search engine using compressed tree forwarding table
Cable drive system for carriage movement and method of use
Wind turbine
Surface-emission laser diode, surface-emission laser diode array, optical scanning apparatus and image forming apparatus
High-pressure discharge lamp with miniature discharge vessel and integrated circuitry
Method, apparatus and program storage device for providing data path optimization
Switch arrangement for door closers
Toy motorcycle
Dispensing container sleeve
Blinking annotation callouts highlighting cross language search results