Reverse pharmacology and the de-orphanization of 7TM receptors

Drug Discovery Today: Technologies

Volumn 1, Issue 2, 2004, Pages 99-104

  Kotarsky, Knut ^a   Nilsson, Niclas E ^a  

^a LUND UNIVERSITY   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; LIGAND; NEW DRUG; SEVEN TRANSMEMBRANE G PROTEIN COUPLED RECEPTOR; UNCLASSIFIED DRUG;

ARTICLE; DRUG INDUSTRY; DRUG TARGETING; GENE LIBRARY; GENE SEQUENCE; GENETIC CODE; GENETIC IDENTIFICATION; HUMAN; KNOCKOUT GENE; NUCLEOTIDE SEQUENCE; OPEN READING FRAME; PROTEIN EXPRESSION; PROTEIN PROTEIN INTERACTION; PROTEIN TARGETING; RECEPTOR INTRINSIC ACTIVITY; SIGNAL TRANSDUCTION;

EID: 13244253657     PISSN: 17406749     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ddtec.2004.07.003     Document Type: Review

References (19)

1. J. Drews Drug discovery: A historical perspective Science 287 5460 2004 1960-1964
2. D.K. Vassilatis et al. The G protein-coupled receptor repertoires of human and mouse Proc. Natl. Acad. Sci. USA 100 8 2003 4903-4908
3. R. Fredriksson et al. The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints Mol. Pharmacol. 63 6 2003 1256-1272
4. F. Libert et al. Current developments in G-protein-coupled receptors Curr. Opin. Cell. Biol. 3 2 1991 218-223
5. A.J. Brown et al. The Orphan G protein-coupled receptors GPR41 and GPR43 are activated by propionate and other short chain carboxylic acids J. Biol. Chem. 278 13 2003 11312-11319
6. O. Civelli et al. Orphan receptors, novel neuropeptides and reverse pharmaceutical research Brain Res. 848 1/2 1999 63-65
7. S. Tunaru et al. PUMA-G and HM74 are receptors for nicotinic acid and mediate its anti-lipolytic effect Nat. Med. 3 3 2003 3
8. K. Kotarsky et al. A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs Biochem. Biophys. Res. Commun. 301 2 2003 406-410
9. A. Wise et al. Molecular identification of high and low affinity receptors for nicotinic acid J. Biol. Chem. 9 2003 9
10. G. Milligan et al. Inverse agonism at adrenergic and opioid receptors: studies with wild type and constitutively active mutant receptors Receptors Channels 5 3/4 1997 209-213
11. K.L. Pierce et al. Seven-transmembrane receptors Nat. Rev. Mol. Cell. Biol. 3 9 2002 639-650
12. R.A. Hall R.J. Lefkowitz Regulation of G protein-coupled receptor signaling by scaffold proteins Circ. Res. 91 8 2002 672-680
13. P.G. Szekeres Functional assays for identifying ligands at orphan G protein-coupled receptors Receptors Channels 8 5/6 2002 297-308
14. J.H. Zhang et al. A simple statistical parameter for use in evaluation and validation of high throughput screening assays J. Biomol. Screen. 4 2 1999 67-73
15. G. Milligan Strategies to identify ligands for orphan G-protein-coupled receptors Biochem. Soc. Trans. 30 4 2002 789-793
16. E. Kostenis Is Galpha16 the optimal tool for fishing ligands of orphan G-protein-coupled receptors? Trends Pharmacol. Sci. 22 11 2001 560-564
17. K. Kotarsky et al. Progress in methodology. Improved reporter gene assays used to identify ligands acting on orphan seven-transmembrane receptors Pharmacol. Toxicol. 93 6 2003 249-258
18. M. Kojima et al. Ghrelin is a growth-hormone-releasing acylated peptide from stomach Nature 402 6762 1999 656-660
19. R. Fujii et al. Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7 J. Biol. Chem. 277 37 2002 34010-34016