Agonist binding: A multistep process

Molecular Pharmacology

Volumn 65, Issue 5, 2004, Pages 1060-1062

  Kobilka, Brian ^a,b  

^a STANFORD UNIVERSITY MEDICAL CENTER   (United States)

^b STANFORD UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADRENALIN; AMINO ACID; BETA 2 ADRENERGIC RECEPTOR; DOPAMINE; G PROTEIN COUPLED RECEPTOR; PHENETHYLAMINE; TACHYKININ RECEPTOR;

BINDING AFFINITY; FLUORESCENCE SPECTROSCOPY; MOLECULAR INTERACTION; MOLECULAR MECHANICS; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN PURIFICATION; RECEPTOR BINDING; REVIEW;

ADRENERGIC AGONISTS; BINDING SITES; RECEPTORS, ADRENERGIC, BETA-2; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 2142823785     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.65.5.1060     Document Type: Review

References (9)

1. Azzi M, Charest PG, Angers S, Rousseau G, Kohout T, Bouvier M, and Pineyro G (2003) Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc Natl Acad Sci USA 100:11406-11411.
2. Ghanouni P, Gryczynski Z, Steenhuis JJ, Lee TW, Farrens DL, Lakowicz JR, and Kobilka BK (2001) Functionally different agonists induce distinct conformations in the G protein coupling domain of the β2 adrenergic receptor. J Biol Chem 276: 24433-24436.
3. Liapakis G, Ballesteros JA, Papachristou S, Chan WC, Chen X, and Javitch JA (2000) The forgotten serine. A critical role for Ser-2035.42 in ligans binding to and activation of the β2-adrenergic receptor. J Biol Chem 275:37779-37788.
4. Liapakis G, Chan WC, Papadokostaki M, and Javitch JA (2004) Synergistic contributions of the functional groups of epinephrine to its affinity and efficacy at the β2 adrenergic receptor. Mol Pharmacol 65:1181-1190.
5. Luttrell LM and Lefkowitz RJ (2002) The role of beta-arrestins in the termination and transduction of G-protein-coupled receptor signals. J Cell Sci 115:455-465.
6. Palanche T, Ilien B, Zoffmann S, Reck MP, Bucher B, Edelstein SJ, and Galzi JL (2001) The neurokinin A receptor activates calcium and cAMP responses through distinct conformational states. J Biol Chem 276:34853-34861.
7. Strader C, Sigal I, and Dixon R (1989) Structural basis of β-adrenergic receptor function. FASEB J 3:1825-1832.
8. Swaminath G, Xiang Y, Lee TW, Steenhuis J, Parnot C, and Kobilka BK (2004) Sequential binding of agonists to the β2 adrenoceptor: kinetic evidence for intermediate conformational states. J Biol Chem 279:686-691.
9. Wieland K, Zuurmond HM, Krasel C, Ijzennan AP, and Lohse MJ (1996) Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor. Proc Natl Acad Sci USA 93:9276-9281.