Potency of ligands correlates with affinity measured against agonist and inverse agonists but not against neutral ligand in constitutively active chemokine receptor

Molecular Pharmacology

Volumn 57, Issue 3, 2000, Pages 602-609

  Rosenkilde, Mette M ^a,b   Schwartz, Thue W ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

[No Author keywords available]

Indexed keywords

CHEMOKINE RECEPTOR; RADIOLIGAND;

ARTICLE; BINDING AFFINITY; BINDING SITE; DRUG MECHANISM; DRUG POTENCY; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; LIGAND BINDING; PRIORITY JOURNAL; RADIOACTIVITY;

EID: 0034006475     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.57.3.602     Document Type: Article

References (40)

1. Ahuja SK and Murphy PM (1993) Molecular piracy of mammalian interleukin-8 receptor type B by herpesvirus saimiri. J Biol Chem 288:20691-20694.
2. Ahuja SK and Murphy PM (1996) The CXC chemokines growth-regulated oncogene (GRO) α, GROβ, GRO-γ, neutrophil-activating peptide-2, and epithelial cell-derived neutrophil-activating peptide-78 are potent agonists for the type B, but not the type A, human interleukin-8 receptor. J Biol Chem 271:20545-20550.
3. Arvanitakis L, Geras-Raaka E, Varma A, Gershengorn MC and Cesarman E (1997) Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation. Nature (Lond) 385:347-350.
4. Bais C, Santomasso B, Coso O, Arvanitakis L, Raaka EG, Gutkind JS, Asch AS, Cesarman E, Gerhengorn MC and Mesri EA (1998) G-protein-coupled receptor of Kaposi's sarcoma-associated herpesvirus is a viral oncogene and angiogenesis activator. Nature (Lond) 391:86-89.
5. Barker EL, Westphal RS, Schmidt D and Sanders-Bush E (1994) Constitutive active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands. J Biol Chem 269:11687-11690.
6. Beisser PS, Vink C, Van Dam JG, Grauls G, Vannerle SJ and Bruggeman CA (1998) The R33 G-protein-coupled receptor gene of rat cytomegalovirus plays an essential role in the pathogenesis of viral infection. J Virology 72:2352-2363.
7. Berridge MJ, Dawson MC, Downes CP, Heslop JP and Irvin RF (1983) Changes in the level of inositol phosphates after agonist-dependent hydrolysis of membrane phosphoinositides. Biochem J 212:473-482.
8. Cesarman E, Nador RG, Bai F, Bohenzky RA, Russo JJ, Moore PS, Chang Y and Knowles DM (1996) Kaposi's sarcoma-associated herpesvirus contains G protein-coupled receptors and cyclin D homologs which are expressed in Kaposi's sarcoma and malignant lymphoma. J Virology 70:8218-8223.
9. Chang Y, Cesarman E, Pessin MS, Lee F, Culpepper J, Knowles DM and Moore PS (1994) Identification of herpesvirus-like DNA sequences in AIDS-associated Kaposi's sarcoma. Science (Wash DC) 266:1865-1869.
10. Chidiac P, Hebert TE, Valiquette M, Dennis M and Bouvier M (1994) Inverse agonist activity of B-adrenergic antagonists. Mol Pharmacol 45:490-499.
11. Clore GM, Appella E, Yamada M, Matsushima K and Gronenborn AM (1990) Three-dimensional structure of interleukin 8 in solution. Biochemistry 29:1689-1696.
12. Costa T and Herz A (1989) Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA 86: 7321-7325.
13. Dairaghi DJ, Greaves DR and Schall TJ (1998) Abduction of chemokine elements by herpesviruses. Semin Viral 8:377-385.
14. Damon I, Murphy PM and Moss B (1998) Broad spectrum chemokine antagonistic activity of a human poxvirus chemokine homolog. Proc Natl Acad Sci USA 95: 6403-6407.
15. Davis-Poynter NJ, Lynch DM, Vally H, Shellam GR, Rawlinson WD, Barrell BG and Farrell HE (1997) Identification and characterization of a G protein-coupled receptor homolog encoded by murine cytomegalovirus. J Virology 71:1521-1529.
16. De Lean A, Stadel JM and Lefkowitz RJ (1980) A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase coupled beta-adrenergic receptor. J Biol Chem 255:7108-7117.
17. Deblasi A, O'Reilly K and Motulsky HJ (1989) Calculation of receptor number from binding experiments using the same compound as radioligand and competitor. Trends Pharmacol Sci 10:227-229.
18. Fields BN, Knipe DM, Howley PM, Chanock RM, Melnick JL, Monath TP, Roizman B, Straus SE (1995) Fields Virology, 3rd ed., Lippincott-Raven Publishers, Philadelphia.
19. Geras-Raaka E, Arvanitakis L, Bais C, Cesarman E, Mesri EA and Gershengorn MC (1998a) Inhibition of constitutive signaling of Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor by protein kinases in mammalian cells in culture. J Exp Med 187:801-806.
20. Geras-Raaka E, Varma A, Ho H, Clark-Lewis I and Gershengorn MC (1998b) Human interferon-γ-inducible protein 10 (IP-10) inhibits constitutive signaling of Kaposi's sarcoma-associated herpesvirus G protein-coupled receptor. J Exp Med 188:405-408.
21. Gether U, Johansen TE, Snider RM, Lowe JA III, Nakanishi S and Schwartz TW (1993) Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist. Nature (Lond) 362:345-348.
22. Hastrup H and Schwartz TW (1996) Septide and neurokinin A are high-affinity ligands on the NK-1 receptor: Evidence from homologous versus heterologous binding analysis. FEES Lett 399:264-266.
23. Hjorth SA, Thirstrup K and Schwartz TW (1996) Radioligand-dependent discrepancy in agonist affinities enhanced by mutations in the κ-opioid receptor. Mol Pharmacol 50:977-984.
24. Horuk R (1998) Chemokines beyond inflammation. Nature (Lond) 393:524-525.
25. Johansen TE, Schøller MS, Tolstroy S and Schwartz TW (1990) Biosynthesis of peptide precursors and protease inhibitors using new constitutive and inducible eukaryotic expression vectors. FEBS Lett 267:289-294.
26. Kenakin TP (1993) The pharmacological analysis of drug-receptor interaction. Raven Press, New York.
27. Kledal TN, Rosenkilde MM, Coulin F, Simmons G, Johnsen AH, Alouani S, Power CA, Luttichau HR, Gerstoft J, Clapham PR, Clark LI, Wells TC and Schwartz TW (1997) A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science (Wash DC) 277:1656-1659.
28. Lefkowitz RJ, Cotecchia S, Samama P and Costa T (1993) Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci 14:303-307.
29. Leong SR, Kabakoff RC and Hébert CA (1994) Complete mutagenesis of the extracellular domain of interleukin-8 (IL-8) type A receptor identifies charged residues mediating IL-8 binding and signal transduction. J Biol Chem 269:19343-19348.
30. Moore BB, Arenberg DA and Strieter RM (1998) The role of CXC chemokines in the regulation of angiogenesis in association with lung cancer. Trends Cardiovasc Sci 8:51-58.
31. Rosenkilde MM, Cahir M, Gether U, Hjorth SA and Schwartz TW (1994) Mutations along transmembrane segment II of the NK-1 receptor affect substance P competition with non-peptide antagonists but not substance P binding. J Biol Chem 269:28160-28164.
32. Rosenkilde MM, Kledal TN, Bräuner-Osborne H and Schwartz TW (1999) Agonist and inverse agonist for the herpesvirus 8-encoded constitutively active seven-transmembrane oncogene product, ORF-74. J Biol Chem 274:956-961.
33. 11]substance P(7-11), a tritiated septide-like peptide, in Chinese hamster ovary cells expressing human neurokinin-1 receptors and in rat submandibular glands. Mol Pharmacol 52:120-127.
34. Samama P, Pei G, Costa T, Cotecchia S and Lefkowitz RJ (1994) Negative antagonists promote an inactive conformation of the β2-adrenergic receptor. Mol Pharmacol 45:390-394.
35. Simas JP and Efstathiou S (1998) Murine gamma herpes 68: A model for the study of gammaherpesvirus pathogenesis. Trends Microbiol 7:276-282.
36. Strieter RM, Polverini PJ, Kunkel SL, Arenberg DA, Burdick MD, Kasper J, Dzuiba J, Van DJ, Walz A, Marriott D, Chan S-Y, Roczniak S and Shanafelt AB (1995) The functional role of the ELR motif in CXC chemokine-mediated angiogenesis. J Biol Chem 270:27348-27357.
37. Tachibana K, Hirota S, Iizaaa H, Yoshida H, Kawabata K, Kataoka Y, Kitamura Y, Matsushima K, Yoshida N, Hishikawa S, Kishimoto T and Nagasawa T (1998) The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract. Nature (Lond) 393:591-595.
38. Wells TNC and Schwartz TW (1997) Plagiarism of the host immune system: Lessons about chemokine immunology from viruses. Curr Opin Biotech 8:741-748.
39. Williams LT and Lefkowitz RJ (1977) Slowly reversible binding of catecholamine to a nucleotide-sensitive state of the beta-adrenergic receptor. J Biol Chem 252: 7207-7213.
40. Zlotnik A, Morales J and Hedrick JA (1999) Recent advances in chemokines and chemokine receptors. Crit Rev Immunol 19:1-47.