Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...
Reexamination Certificate
2007-06-26
2007-06-26
Ulm, John (Department: 1649)
Chemistry: molecular biology and microbiology
Measuring or testing process involving enzymes or...
Involving antigen-antibody binding, specific binding protein...
C435S007210, C435S069700, C536S023400
Reexamination Certificate
active
10959611
ABSTRACT:
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.
REFERENCES:
patent: 4931569 (1990-06-01), Edwards et al.
patent: 4978614 (1990-12-01), Bronstein
patent: 5145772 (1992-09-01), Voyta et al.
patent: 5326882 (1994-07-01), Bronstein et al.
patent: 5538847 (1996-07-01), Bronstein et al.
patent: 5851771 (1998-12-01), Bronstein et al.
patent: 5891646 (1999-04-01), Barak et al.
patent: 6110693 (2000-08-01), Barak et al.
patent: 6342345 (2002-01-01), Blau et al.
patent: 6800445 (2004-10-01), Palmer et al.
patent: 6893827 (2005-05-01), Palmer et al.
patent: WO 98/44350 (1998-10-01), None
patent: WO 01/37896 (2001-05-01), None
patent: WO 01/59451 (2001-08-01), None
V. Gurevich et al., “Arrestin Interactions With G Protein-Coupled Receptors”, The Journal of Biological Chemistry, vol. 270, No. 2, Jan. 13, 1995, pp. 720-731.
S. Vishnivetskiy et al., “How Does Arrestin Respond to The Phosphorylated State of Rhodopsin”?, The Journal of Biological Chemistry, vol. 274, No. 17, Apr. 23, 1999, pp. 11451-11454.
R. Oakley et al., Association of β-Arrestin With G Protein-Coupled Receptors During Clathrin-Mediated Endocytosis Dictates The Profile Of Receptor Resensitization, The Journal of Biological Chemistry, vol. 274, No. 45, Nov. 5, 1999, pp. 32248-32257.
B Blakely et al., “Epidermal Growth Factor Receptor Dimerization Monitored In Live Cells”, Nature Biotechnology, vol. 18, Feb. 2000, pp. 218-222.
Supplementary European Search Report issued in European Patent Application No. 01906531 on Aug. 17, 2005, 4 pages Dated Aug. 3, 2005.
Angers et al., “Detection of β2-adrenergic receptor dimerization in living cells using bioluminescence resonance energy transfer (BRET)”, Proc. Nat. Acad. Sci. USA, 97(7) :3684-3689 (2000).
Gurevich et al., “Mechanism of Phosphorylation-Recognition by Visual Arrestin and the Transition of Arrestin into a High Affinity Binding State”, Mol. Pharmacol., 51:161-169 (1997).
Rossi et al., “Monitoring Protein-Protein Interactions in Intact Eukaryotic Cells by β-galactosidase complementation”, Proc. Natl. Acad. Sci., 94:8405-8410 (1997).
Barak et al., “A β-Arrestin/Green Fluorescent Protein Biosensor for Detecting G Protein-coupled Receptor Activation”, the Journal of Biological Chemistry, 272 (44) :27497-27500 (1997).
Ferguson et al., “G-protein-coupled receptor regulation: role of G-protein-coupled receptor Kinases and arrestins”, Can. J. Physiol Pharmacol., 74:1095-110 (1996).
Pitcher et al., “G-protein-coupled receptor kinases”, Annu. Rev. Biochem., 67:653-692 (1998).
Lefkowitz et al., “Adenylate cyclase-coupled beta-adrenergic receptors: structure and mechanisms of activation and desensitization”, Annul. Rev. Biochem., 52:159-186 (1983).
Germino et al., “Screening for in vivo protein-protein interactions”, Proc. Natl. Acad. Sci., 90:933-937 (1993).
Phizicky et al., “Protein-protein interactions: methods for detection and analysis”, Microbiol. Rev., 59(1) :94-123 (1995).
Offermanns et al., “Gα15 and gα16 couple a wide variety of receptors to phospholipase C”, J. Biol. Chem., 270(25) :15175-15180 (1995).
AbdAlla et al., “AT1-Receptor heterodimers show enhanced G-protein activation and altered receptor sequestration”, Nature, 407:94-98 (2000).
Bockaert et al., “Molecular tinkering of G protein-coupled receptors: an evolutionary success”, The EMBO Journal, 18(7)1723-1729 (1999).
Jordan et al., “G-protein-coupled receptor heterodimerization modulates receptor function”, Nature, 399:697-700 (1999).
Ng et al., “Dopamine D2 receptor dimers and receptor-blocking peptides” Bioch. Biophys. Res. Commun., 227:200-204 (1996).
Hebert et al., “A peptide derived from a β2-adrenergic receptor transmembrane domain inhibits both receptor dimerization and activation”, J. Biol. Chem. 271(27) :16384-16392 (1996).
Krupnick et al., “The role of receptor kinases and arrestins in G protein-coupled receptor regulation” Ann. Rev. Pharmacol. Toxicol., 38:289-319 (1998).
Hamm “The many faces of G-protein Signaling”, J. Biol. Chem., 273(2) :669-672 (1998).
Zhang et al., “Cellular trafficking of G protein-coupled receptor/β-arrestin endocytic complexes”, J. Biol. Chem., 274(16) :10999-11006 (1999).
Kovoor et al., “Targeted construction of phosphorylation-independent β-arrestin mutants with constitutive activity in cells”, J. Biol. Chem., 274(11) :6831-6834 (1999).
Chang Xiao-jia
Gee Melissa
Palmer Michelle A. J.
Tillotson Bonnie
Applera Corporation
Finn Andrew
Ulm John
LandOfFree
Systems for sensitive detection of G-protein coupled... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Systems for sensitive detection of G-protein coupled..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Systems for sensitive detection of G-protein coupled... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3852882