Quantifying biological activity in chemical terms: A pharmacology primer to describe drug effect

ACS Chemical Biology

Volumn 4, Issue 4, 2009, Pages 249-260

  Kenakin, Terry ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

5 CYANOTRYPTAMINE; APLAVIROC; CARBACHOL; CELL RECEPTOR; ESTRADIOL; HISTAMINE H2 RECEPTOR ANTAGONIST; IFENPRODIL; ISOPRENALINE; N BENZYL 5 METHOXYTRYPTAMINE; N,N DIMETHYLTRYPTAMINE; OXOTREMORINE; PRENALTEROL; PROPRANOLOL; SEROTONIN AGONIST; TRYPTAMINE DERIVATIVE; UNCLASSIFIED DRUG; DRUG; PROTEIN BINDING;

ALLOSTERISM; BINDING AFFINITY; BIOLOGICAL ACTIVITY; DRUG ACTIVITY; DRUG ANTAGONISM; DRUG BINDING; DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG TARGETING; GENETIC VARIABILITY; HUMAN; KINETICS; MULTIVARIATE ANALYSIS; NONHUMAN; PHARMACODYNAMICS; PHYSIOLOGY; PRIORITY JOURNAL; REVIEW; STRUCTURE ACTIVITY RELATION; THERAPY EFFECT; TISSUE SPECIFICITY; ADSORPTION; ANIMAL; BIOLOGY; CHEMICAL STRUCTURE; CHEMISTRY; PHARMACOLOGY; PROCEDURES; PROTEIN CONFORMATION;

ADSORPTION; ANIMALS; COMPUTATIONAL BIOLOGY; KINETICS; MODELS, MOLECULAR; PHARMACEUTICAL PREPARATIONS; PHARMACOLOGY; PROTEIN BINDING; PROTEIN CONFORMATION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 65649123378     PISSN: 15548929     EISSN: None     Source Type: Journal    
DOI: 10.1021/cb800299s     Document Type: Review

References (23)

1. Kenakin, T. P., and Beek, D. (1984) The measurement of the relative efficacy of agonists by selective potentiation of tissue responses: studies with isoprenaline and prenalterol in cardiac tissue, J. Auton. Pharmacol. 4, 153-159. (Pubitemid 14043215)
2. Kenakin, T. P. (1985) Prenalterol as a selective cardiostimulant: differences between organ and receptor selectivity, J. Cardiovasc. Pharmacol. 7, 208-210. (Pubitemid 15162266)
3. Stephenson, R. P. (1956) A modification of receptor theory, Br. J. Pharmacol. 11, 379-393. (Pubitemid 127732575)
4. Leff, P., Martin, G. R., and Morse, J. M. (1986) Br. J. Pharmacol. 89, 493-499.
5. Black, J. W., and Leff, P. (1983) Operational models of pharmacological agonist, Proc. R. Soc. London, Ser. B 220, 141-162.
6. Kenakin, T. P. (2003) Predicting therapeutic value in the lead optimization phase of drug discovery, Nat. Rev. Drug Discovery 2, 429-437.
7. Kenakin, T. P. (1985) Prenalterol as a selective cardiostimulant: differences between organ and receptor selectivity, J. Cardiovasc. Pharmacol. 7, 208-210. (Pubitemid 15162266)
8. Kenakin, T. P. (1997) The Pharmacologic Analysis of Drug Receptor Interaction 3rd ed., p 1491, Lippincott-Raven, NY.
9. Black, J. W. (1996) A personal view of pharmacology, Annu. Rev. Pharmacol. Toxicol. 36, 1-33. (Pubitemid 26168692)
10. Black, J. W., Duncan, W. A., and Shanks, R. G. (1965) Comparison of some properties of pronethalol and propranolol, Br. J. Pharmacol. Chemo. 25, 577. (Pubitemid 127732599)
11. Azzi, M., Charest, P. G., Angers, S., Rousseau, G., Kohout, T., Bouvier, M., and Piñeyro, G. (2003) β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G-protein-coupled receptors, Proc. Natl. Acad. Sci. U.S.A. 100, 11406-11411. (Pubitemid 37205948)
12. Kenakin, T. P. (2008) Pharmacological onomastics: what's in a name? Br. J. Pharmacol. 153, 432-438.
13. 2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy, Mol. Pharmacol. 70, 1575-1584.
14. Christopolous, A., and Kenakin, T. P. (2002) G-Protein coupled receptor allosterism and complexing, Pharmacol. Rev. 54, 323-374. (Pubitemid 34575719)
15. Sabroe, I., Peck, M. J., Van Keulen, B. J., Jorritsma, A., Simmons, G., Clapham, P. R., Williams, T. J., and Pease, J. E. (2000) A small molecule antagonist of chemokine receptors CCR1 and CCR3, J. Biol. Chem. 275, 25985-25992.
16. Hejnova, L., Tucek, S., and El-Fakahany, E. E. (1995) Positive and negative allosteric interactions on muscarinic receptors, Eur. J. Pharmacol. 291, 427-430. (Pubitemid 3014613)
17. Gonzalez, E., Kulkarni, H., Bolivar, H., Mangano, A., Sanchez, R., Catano, G., Nibbs, R. J., Freedman, B. I., Quinones, M. P., Bamshad, M. J., Murthy, K. K., Rovin, B. H., Bradley, W., Clark, R. A., Anderson, S. A., O'connell, R. J., Agan, B. K., Ahuja, S. S., Bologna, R., Sen, L., Dolan, M. J., and Ahuja, S. K. (2005) The influence of CCL3L1 gene-containing segmental duplications on HIV-1/AIDS susceptibility, Science 307, 1434-1440.
18. Muniz-Medina, V. M., Jones, S., Maglich, J. M., Galardi, C., Hollingsworth, R. E., Kazmierski, W. M., Ferris, R. G., Edelstein, M. P., Chiswell, K. E., and Kenakin, T. P. (2009) The relative activity of 'function sparing' HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property, Mol. Pharmacol. In press.
19. Watson, C., Jenkinson, S., Kazmierski, W., and Kenakin, T. P. (2005) The CCR5 receptor-based mechanism of action of 873140, a potent allosteric non-competitive HIV entry-inhibitor, Mol. Pharmacol. 67, 1268-1282. (Pubitemid 40410427)
20. Kew, J. N. C., Trube, G., and Kemp, J. A. (1996) A novel mechanism of activity-dependent NMDA receptor antagonism describes the effects of ifenprodil in rat cultured cortical neurons, J. Physiol. 497, 761-772. (Pubitemid 27032913)
21. Tucek, S., and Proska, J. (1995) Allosteric modulation of muscarinic acdetylcholine receptors, Trends Pharmacol. Sci. 16, 205-212.
22. Copeland, R. A., Pompliano, D. L., and Meek, T. D. (2006) Drug target residence time and its implications for lead optimization, Nat. Rev. Drug Discovery 5, 730-739. (Pubitemid 44323700)
23. Manas, E. S., Unwalla, R. J., Xu, Z. B., Malamas, M. S., Miller, C. P., Harris, H. A., Hsiao, C., Akopian, T., Hum, W-T., Malakian, K., Wolfrom, S., Bapat, A., Bhat, R. A., Stahl, M. L., Somers, M. S., and Alvarez, J. C. (2004) Structure-based design of estrogen receptor-β- selective ligands, J. Am. Chem. Soc. 126, 15106-15119. (Pubitemid 39557270)