Co-evolving stability and conformational homogeneity of the human adenosine A2a receptor

Proceedings of the National Academy of Sciences of the United States of America

Volumn 105, Issue 31, 2008, Pages 10744-10749

  Magnani, Francesca ^a   Shibata, Yoko ^a   Serrano Vega, Maria J ^a   Tate, Christopher G ^a  

^a MRC LABORATORY OF MOLECULAR BIOLOGY   (United Kingdom)

Author keywords

Conformational thermostabilization; G protein coupled receptor; Membrane protein

Indexed keywords

ADENOSINE A2A RECEPTOR; ADENOSINE A2A RECEPTOR AGONIST; ADENOSINE A2A RECEPTOR ANTAGONIST;

ARTICLE; CONTROLLED STUDY; HUMAN; MUTAGENESIS; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN STABILITY; PROTEIN STRUCTURE; THERMOSTABILITY;

DETERGENTS; HUMANS; MODELS, MOLECULAR; MUTAGENESIS; MUTATION; PROTEIN CONFORMATION; PROTEIN DENATURATION; RADIOLIGAND ASSAY; RECEPTOR, ADENOSINE A2A; TEMPERATURE;

MAMMALIA;

EID: 49449114407     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.0804396105     Document Type: Article

References (28)

1. Hopkins AL, Groom CR (2002) The druggable genome. Nat Rev Drug Discov 1:727-730.
2. Baldwin JM (1994) Structure and function of receptors coupled to G proteins. Curr Opin Cell Biol 6:180-190.
3. Li J, Edwards PC, Burghammer M, Villa C, Schertler GF (2004) Structure of bovine rhodopsin in a trigonal crystal form. J Mol Biol 343:1409-1438.
4. Palczewski K, et al. (2000) Crystal structure of rhodopsin: A G protein-coupled receptor. Science 289:739-745.
5. Kusnetzow AK, Altenbach C, Hubbell WL (2006) Conformational states and dynamics of rhodopsin in micelles and bilayers. Biochemistry 45:5538-5550.
6. Christopoulos A, Kenakin T (2002) G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54:323-374.
7. Kobilka BK, Deupi X (2007) Conformational complexity of G-protein-coupled receptors. Trends Pharmacol Sci 28:397-406.
8. Gether U, et al. (1997) Structural instability of a constitutively active G protein-coupled receptor. Agonist-independent activation due to conformational flexibility. J Biol Chem 272:2587-2590.
9. Ghanouni P, et al. (2001) Functionally different agonists induce distinct conformations in the G protein coupling domain of the beta 2 adrenergic receptor. J Biol Chem 276:24433-24436.
10. De Grip WJ (1982) Thermal stability of rhodopsin and opsin in some novel detergents. Methods Enzymol 81:256-265.
11. Lau FW, Nauli S, Zhou Y, Bowie JU (1999) Changing single side-chains can greatly enhance the resistance of a membrane protein to irreversible inactivation. J Mol Biol 290:559-564.
12. Faham S, et al. (2004) Side-chain contributions to membrane protein structure and stability. J Mol Biol 335:297-305.
13. Zhou Y, Bowie JU (2000) Building a thermostable membrane protein. J Biol Chem 275:6975-6979.
14. Standfuss J, et al. (2007) Crystal structure of a thermally stable rhodopsin mutant. J Mol Biol 372:1179-1188.
15. Serrano-Vega MJ, Magnani F, Shibata Y, Tate CG (2008) Conformational thermostabilisation of the β-adrenergic receptor in a detergent resistant form. Proc Natl Acad Sci USA 105:877-882.
16. Weiss HM, Grisshammer R (2002) Purification and characterization of the human adenosine A(2a) receptor functionally expressed in Escherichia coli. Eur J Biochem 269:82-92.
17. Ji XD, Jacobson KA (1993) Solubilized rabbit striatal A2a-adenosine receptors: Stability and antagonist binding. Arch Biochem Biophys 305:611-617.
18. Gao ZG, Jiang Q, Jacobson KA, Ijzerman AP (2000) Site-directed mutagenesis studies of human A(2A) adenosine receptors: Involvement of glu(13) and his(278) in ligand binding and sodium modulation. Biochem Pharmacol 60:661-668.
19. Guan L, Smirnova IN, Verner G, Nagamori S, Kaback HR (2006) Manipulating phospholipids for crystallization of a membrane transport protein. Proc Natl Acad Sci USA 103:1723-1726.
20. Palsdottir H, Hunte C (2004) Lipids in membrane protein structures. Biochim Biophys Acta 1666:2-18.
21. Yao Z, Kobilka B (2005) Using synthetic lipids to stabilize purified beta2 adrenoceptor in detergent micelles. Anal Biochem 343:344-346.
22. Rasmussen SG, et al. (2007) Crystal structure of the human beta(2) adrenergic G-protein-coupled receptor. Nature 450:383-387.
23. Cherezov V, et al. (2007) High-resolution crystal structure of an engineered human {beta}2-adrenergic G protein coupled receptor. Science 318:1258-1265.
24. Jiang Q, et al. (1996) Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition. Mol Pharmacol 50:512-521.
25. Seifert R, Wenzel-Seifert K, Gether U, Kobilka BK (2001) Functional differences between full and partial agonists: evidence for ligand-specific receptor conformations. J Pharmacol Exp Ther 297:1218-1226.
26. Knierim B, Hofmann KP, Ernst OP, Hubbell WL (2007) Sequence of late molecular events in the activation of rhodopsin. Proc Natl Acad Sci USA 104:20290-20295.
27. Inoue H, Nojima H, Okayama H (1990) High efficiency transformation of Escherichia coli with plasmids. Gene 96:23-28.
28. Warne T, Chirnside J, Schertler GF (2003) Expression and purification of truncated, non-glycosylated turkey beta-adrenergic receptors for crystallization. Biochim Biophys Acta 1610:133-140.