Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving antigen-antibody binding – specific binding protein...
Reexamination Certificate
2005-06-07
2005-06-07
Kunz, Gary (Department: 1646)
Chemistry: molecular biology and microbiology
Measuring or testing process involving enzymes or...
Involving antigen-antibody binding, specific binding protein...
C435S007200, C435S007210, C435S069100, C435S235100, C435S320100, C435S375000, C530S300000, C530S350000, C536S023100
Reexamination Certificate
active
06902902
ABSTRACT:
The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
REFERENCES:
patent: 5514578 (1996-05-01), Hogness et al.
patent: 5532157 (1996-07-01), Fink
patent: 5573944 (1996-11-01), Kirschner et al.
patent: 5639616 (1997-06-01), Liao et al.
patent: 5750353 (1998-05-01), Kopin et al.
patent: 5861309 (1999-01-01), Bard et al.
patent: 5891720 (1999-04-01), Moore et al.
patent: 5955308 (1999-09-01), Bergsma et al.
patent: 2002/0137063 (2002-09-01), Glucksmann et al.
patent: 2003/0078218 (2003-04-01), Jaral et al.
patent: 2135253 (1996-05-01), None
patent: 0 612 845 (1994-08-01), None
patent: 0 878 542 (1998-11-01), None
patent: 0 892 051 (1999-01-01), None
patent: 1 090 989 (2001-04-01), None
patent: 1 094 076 (2001-04-01), None
patent: 0109028.1 (2001-05-01), None
patent: 0126637.8 (2002-01-01), None
patent: 2 365 868 (2002-02-01), None
patent: WO 96/05302 (1996-02-01), None
patent: WO 97/11159 (1996-09-01), None
patent: WO 97/21731 (1997-06-01), None
patent: WO 98/00552 (1998-01-01), None
patent: WO 98/29439 (1998-07-01), None
patent: WO 98/34948 (1998-08-01), None
patent: WO 98/38217 (1998-09-01), None
patent: WO 98/46620 (1998-10-01), None
patent: WO 98/46995 (1998-10-01), None
patent: WO 98/56820 (1998-12-01), None
patent: WO 98/56820 (1998-12-01), None
patent: WO 99/06552 (1999-02-01), None
patent: WO 99/32519 (1999-07-01), None
patent: WO 99/48921 (1999-09-01), None
patent: WO 99/52927 (1999-10-01), None
patent: WO 00/14229 (2000-03-01), None
patent: WO 00/22129 (2000-04-01), None
patent: WO 00/22131 (2000-04-01), None
patent: WO 00/49046 (2000-08-01), None
patent: WO 01/07606 (2001-02-01), None
patent: WO 01/09184 (2001-02-01), None
patent: WO 01/12673 (2001-02-01), None
patent: WO 01/14577 (2001-03-01), None
patent: WO 01/16159 (2001-03-01), None
patent: WO 01/31014 (2001-05-01), None
patent: WO 01/36471 (2001-05-01), None
patent: WO 01/36473 (2001-05-01), None
patent: WO01/36476 (2001-05-01), None
patent: WO01/61359 (2001-05-01), None
patent: WO01/73029 (2001-10-01), None
patent: WO01/74904 (2001-10-01), None
patent: WO01/77320 (2001-10-01), None
patent: WO01/87937 (2001-11-01), None
patent: WO01/94385 (2001-12-01), None
patent: WO02/13845 (2002-02-01), None
patent: WO 02/18579 (2002-03-01), None
patent: WO 02/18579 (2002-03-01), None
patent: WO02/18938 (2002-03-01), None
patent: WO 02/072765 (2002-09-01), None
patent: WO 02/064298 (2002-10-01), None
patent: WO 02/083736 (2002-10-01), None
patent: WO02/084298 (2002-10-01), None
Szapary, et al, “Pharmacological management of high triglycerides and low high-density lipoprotein cholesterol,” Curr. Opin. Pharmacol. (2001) 1:113-120.
PCT International Search Report, for International Application PCT/US01/44615, issued Sep. 9, 2002.
Soga T., et al.; “Molecular identification of nicotinic acid receptor”; Academic Press; Biochemical and Biophysical Research Communications 303 (2003) 364-69; 0006-291X/03/$; 2003 Elsevier Science (USA): doi:10.1016/S0006-291X(03)00342-5.
Hosoi, T., et al.; “Identification of a Novel Human Elcosanold Receptor Coupled to Gi/o”; The Journal of Biological Chemistry; vol. 277, No. 35, Issue of Aug. 30, pp. 31465-31465, 2002; The American Society for biochemistry and Molecular Biology, Inc., USA.
Wise, A, et al.; “Molecular identification of high and low affinity receptors for nicotinic acid”; JBC Papers in Press; Published on Jan. 9, 2003 as Manuscript M210695200; The American Socidety for Biochemistry and Molecular Biology, Inc.; 2003.
Tunaru, S., et al.; “PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect”; Nature Medicine; Advance Online Publication; Feb. 3, 2003, dol:10, 1038
m824; 2003 Nature Publishing Group; http://www.nature.com
aturemedicine.
Lorenzen, A, et al.; “G protein-coupled receptor for nicotinic acid in mouse macrophages”; Biochemical Pharmacology 64 (2002) 645-648; 0006-2952/02/$; 2002 Elsevier Science Inc.; PII:S0006-2952(02)01220-0.
Lorenzen, A., et al.; “Characterization of a G Protein-Coupled Receptor for Nicotinic Acid”; Mol. Pharmacol. 59:349-357, 2001; 0026-895x/01/5902-349-357$3.00; Molecular Pharmacology; 2001 The American Society for Pharmacology and Experimental Therapeutics; vol. 59, No. 2; 136/882146; Online: http://molpharm.aspetjournals.org.
Jones, C. et al.; Expression and Characterization of a 5-oxo-6E, 8Z, 11Z, 14Z-Eicosatetraenoic Acid Receptor Highly Expressed on Human Eosinophils and Neutrophils; Molar Pharmacology; pp. 471-477; vol. 63, No. 3; The American Society for Pharmacology and Experimental Therapeutics; 2003.
Alla, S.A. et al., “Extracellular domains of the bradykinin B2 receptor involved in ligand binding and agonist sensing defined by anti-peptide antibodies,”J. Biol. Chem., 1996, 271, 1748-1755.
Advenier, C. et al., “Effects on the isolated human bronchus of SR 48968, a potent and selective nonpeptide antagonist of the neurokinin A (NK2) receptors,”Am. Rev. Respir. Dis., 1992, 146(5, Pt. 1), 1177-1181.
Alexander, W.S. et al., “Point mutations within the dimer interfact homology domain of c-MpI induce constitutive receptor activity and tumorigenicity,”Embo J., 1995, 14(22), 5569-5578.
Arvanitikis, L. et al., “Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation,”Nature, 1997, 385, 347-349.
Barker, E.L. et al., “Constitutively active 5-hydroxytryptamine2creceptors reveal novel inverse agonist activity of receptor ligands,”J. Biol. Chem., 1994, 269(16), 11687-11690.
Baxter, G., “5-HT2receptors: a family re-united?”Trends Pharmacol. Sci., 1995, 16, 105-110.
Besmer, P. et al., “A new acute transforming feline retrovirus and relationship of its oncogene v-kit with the protein kinase gene family,”Nature, 1986, 320, 415-421.
Blin, N. et al., “Mapping of single amino acid residues required for selective activation of Gq/11by the m3 muscarinic acetylcholine receptor,”J. Biol. Chem., 1995, 270, 17741-17748.
Bond, R.A. et al., “Inverse agonists and G-protein-coupled receptors,” inReceptor-Based Drug Design, Leff, P. (ed.), New York, M. Dekker, 1998, 363-377.
Boone, C. et al., “Mutations that alter the third cytoplasmic loop of the a-factor receptor lead to a constitutive and hypersensitive phenotype,”Proc. Natl. Acad. Sci. USA, 1993, 90(21), 9921-9925.
Burstein, E.S. et al., “Constitutive activation of chimeric m2/m5 muscarinic receptors and delineation of G-protein coupling selectivity domains,”Biochem. Pharmacol., 1996, 51(4), 539-544.
Burstein, E.S. et al., “Amino acid side chains that define muscarinic receptor/G-protein coupling. Studies of the third intracellular loop,”J. Biol. Chem., 1996, 271(6), 2882-2885.
Burstein, E.S. et al., “Constitutive activation of muscarinic receptors by the G-protein Gq,”FEBS Lett., 1995, 363(3), 261-263.
Bylund, D., “International union of pharmacology nomenclature of adrenoceptors,”Pharmacol. Rev., 1994, 46, 121-136.
Cheatham, B. et al., “Substitution of the erbB-2 oncoprotein transmembrane domain activates the insulin receptor and modu
Behan Dominic P.
Chalmers Derek T.
Chen Ruoping
Connolly Daniel T.
Hakak Yaron
Arena Pharmaceuticals Inc.
Basi Nirmal S.
Clark Melody E.
Kunz Gary
O'Connor Cozen
LandOfFree
Human G protein-coupled receptors and modulators thereof for... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Human G protein-coupled receptors and modulators thereof for..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Human G protein-coupled receptors and modulators thereof for... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3482763