Assessing receptor affinity for inverse agonists: Schild and Cheng-Prusoff methods revisited

Current Drug Targets

Volumn 8, Issue 1, 2007, Pages 197-202

  Giraldo, Jesús ^a   Serra, Juan ^a   Roche, David ^a   Rovira, Xavier ^a  

^a UNIVERSITAT AUTÒNOMA DE BARCELONA   (Spain)

Author keywords

Classical Cheng Prusoff equation; Gaddum equation; Neutral antagonist; Schild regression

Indexed keywords

DRUG; G PROTEIN COUPLED RECEPTOR;

ALGORITHM; ALLOSTERISM; ANALYTIC METHOD; ANALYTICAL ERROR; BINDING SITE; CHEMICAL REACTION KINETICS; CONCENTRATION (PARAMETERS); DISSOCIATION CONSTANT; DRUG RECEPTOR BINDING; DRUG RESEARCH; LIGAND BINDING; MATHEMATICAL ANALYSIS; MATHEMATICAL COMPUTING; MATHEMATICAL MODEL; PROTEIN DETERMINATION; PROTEIN FUNCTION; QUANTITATIVE ANALYSIS; RECEPTOR AFFINITY; RECEPTOR BLOCKING; REGRESSION ANALYSIS; REVIEW; SIMULATION; STOICHIOMETRY;

EID: 33846026023     PISSN: 13894501     EISSN: None     Source Type: Journal    
DOI: 10.2174/138945007779315687     Document Type: Review

References (41)

1. Drews, J. (2000) Science 287, 1960-1964.
2. Kenakin, T.P. (1997) Competitive antagonism. In Pharmacologic analysis of drug-receptor interaction pp. 331-373. Lippincott-Raven, Philadelphia.
3. Gaddum, J.H. (1937) J. Physiol. (London) 89, 7P-9P.
4. Arunlakshana, O. & Schild, H. O. (1959) Br. J. Pharmacol. 14, 48-58.
5. Barlow, R.B. (1993) Trends Pharmacol. Sci. 14, 296.
6. Cheng, Y.-C. & Prusoff, W. H. (1973) Biochem. Pharmacol. 22, 3099-3108.
7. Black, J.W. & Leff, P. (1983) Proc. R. Soc. Lond. B. Biol. Sci. 220, 141-162.
8. Craig, D.A. (1993) Trends. Pharmacol. Sci. 14, 89-91.
9. Leff, P. & Dougall, I. G. (1993) Trends Pharmacol. Sci. 14, 110-112.
10. Giraldo, J.; Vivas, N. M.; Vila, E.; Badia, A. (2002) Pharmacol. & Ther. 95, 21-45.
11. Lazareno, S. & Birdsall, N. J. (1993) Br. J. Pharmacol. 109, 1110-1119.
12. Lew, M.J. & Angus, J. A. (1995) Trends. Pharmacol. Sci. 16, 328-337.
13. Barlow, R.B.; Bond, S. M.; Bream, E.; Macfarlane, L.; McQueen, D. S. (1997) Br. J. Pharmacol. 120, 13-18.
14. Lazareno, S. & Birdsall, N. J. (1993) Trends. Pharmacol. Sci. 14, 237-239.
15. Calderone, V. (1998) J. Pharmacol. Toxicol. Methods 39, 129-135.
16. Cheng, H.C. (2002) J. Pharmacol. Toxicol. Methods 46, 61-71.
17. Cheng, H.C. (2004) Pharmacol. Res. 50, 21-40.
18. Costa, T. & Herz, A. (1989) Proc. Natl. Acad. Sci. U. S. A. 86, 7321-7325.
19. Kjelsberg, M.A.; Cotecchia, S.; Ostrowski, J.; Caron, M. G.; Lefkowitz, R. J. (1992) J. Biol. Chem. 267, 1430-1433.
20. Samama, P.; Cotecchia, S.; Costa, T.; Lefkowitz, R. J. (1993) J. Biol. Chem. 268, 4625-4636.
21. de Ligt, R.A.; Kourounakis, A. P.; Ijzerman, A. P. (2000) Br. J. Pharmacol. 130, 1-12.
22. Milligan, G. (2003) Mol. Pharmacol. 64, 1271-1276.
23. Strange, P.G. (2002) Trends Pharmacol. Sci. 23, 89-95.
24. Chidiac, P. (2002) Methods Enzymol. 343, 3-16.
25. Costa, T.; Ambrosio, C.; Riitano, D.; Molinari, P. (2003) Different mechanisms of negative efficacy. Distinguishing inverse agonists from negative antagonists. In Inverse agonism (Ijzerman,A.P., ed), pp. 1-13. Elsevier, Amsterdam.
26. Kenakin, T. (2004) Mol. Pharmacol. 65, 2-11.
27. Costa, T. & Cotecchia, S. (2005) Trends Pharmacol. Sci. 26, 618-624.
28. del Castillo, J. & Katz, B. (1957) Proc. R. Soc. Lond. B. 146, 369-381.
29. Monod, J.; Wyman, J.; Changeux, J. P. (1965) J. Mol. Biol. 12, 88-118.
30. Karlin, A. (1967) J. Theor. Biol. 16, 306-320.
31. Thron, C.D. (1973) Mol. Pharmacol. 9, 1-9.
32. Colquhoun, D. (1973) The relationship between classical and cooperative models for drug action. In A symposium on drug receptors (Rang,H.P., ed), pp. 149-182. University Park Press, Baltimore.
33. Leff, P. (1995) Trends Pharmacol. Sci. 16, 89-97.
34. Giraldo, J. (2004) FEBS Lett. 556, 13-18.
35. De Lean, A.; Stadel, J. M.; Lefkowitz, R. J. (1980) J. Biol. Chem. 255, 7108-7117.
36. Costa, T.; Ogino, Y.; Munson, P. J.; Onaran, H. O.; Rodbard, D. (1992) Mol. Pharmacol. 41, 549-560.
37. Kenakin, T.P. (2004) Drug antagonism. In A pharmacology primer: Theory, applications and methods pp. 93-122. Elsevier Academic Press, San Diego.
38. Kenakin, T. (2005) Trends Pharmacol. Sci. 26, 603-605.
39. Bond, R.A. & Ijzerman, A. P. (2006) Trends Pharmacol. Sci. 27, 92-96.
40. Kenakin, T. (2004) Trends Pharmacol. Sci. 25, 186-192.
41. Urban, J.D.; Clarke, W. P.; von Zastrow, M.; Nichols, D. E.; Kobilka, B. K.; Weinstein, H.; Javitch, J. A.; Roth, B. L.; Christopoulos A.; Sexton, P.; Miller, K.; Spedding, M.; Mailman, R. B. (2006) J. Pharmacol. Exp. Ther. advanced online publication June 27, 2006; DOI:10.1124/jpet.106.104463