Ligand-specific conformation determines agonist activation and antagonist blockade in purified human thromboxane A2 receptor

Biochemistry

Volumn 48, Issue 14, 2009, Pages 3157-3165

  Ruan, Ke He ^a   Cervantes, Vanessa ^a   Wu, Jiaxin ^a  

^a UNIVERSITY OF HOUSTON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CIRCULAR DICHROISMS; CONFORMATIONAL CHANGES; FLUORESCENCE STUDIES; HELICAL CONFORMATIONS; MOLECULAR INTERACTION FIELDS; MOLECULAR MECHANISMS; NMR SPECTROSCOPIES; PROTEIN-COUPLED RECEPTORS; SHEET STRUCTURES; STRUCTURAL CHANGES; STRUCTURAL FLEXIBILITIES; TRP FLUORESCENCES; TRYPTOPHAN RESIDUES;

AMINO ACIDS; BIOACTIVITY; DICHROISM; FLUORESCENCE; LIGANDS; LIPOSOMES; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PH EFFECTS; PHOSPHOLIPIDS; PURIFICATION;

BINDING SITES;

15 HYDROXY 11ALPHA,9ALPHA EPOXYMETHANOPROSTA 5,13 DIENOIC ACID; ETHANOLAMINE DERIVATIVE; G PROTEIN COUPLED RECEPTOR; LIGAND; LIPOSOME; PHOSPHATIDYLCHOLINE; PHOSPHATIDYLSERINE; PHOSPHATYDYLETHANOLAMINE; THROMBOXANE A2 RECEPTOR BLOCKING AGENT; THROMBOXANE A2 RECEPTOR STIMULATING AGENT; TRYPTOPHAN; UNCLASSIFIED DRUG;

ARTICLE; BETA SHEET; BINDING SITE; CHEMICAL ANALYSIS; CIRCULAR DICHROISM; CONFORMATION; FLUORESCENCE ANALYSIS; HUMAN; MOLECULAR INTERACTION; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PH; PRIORITY JOURNAL; PROTEIN STRUCTURE;

CIRCULAR DICHROISM; HUMANS; HYDROGEN-ION CONCENTRATION; LIGANDS; LIPOSOMES; MAGNETIC RESONANCE SPECTROSCOPY; PHOSPHOLIPIDS; PROTEIN CONFORMATION; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, THROMBOXANE A2, PROSTAGLANDIN H2; TRYPTOPHAN;

EID: 65249179456     PISSN: 00062960     EISSN: None     Source Type: Journal    
DOI: 10.1021/bi801443g     Document Type: Article

References (25)

1. Majerus, P. W. (1983) Arachidonate metabolism in vascular disorders. J. Clin. Invest. 72, 1521-1525.
2. Samuelson, B., Goldyne, M., Granstrom, E., Hamberg, M., Hammarstrom, S., and Malmsten, C. (1978) Prostaglandins and thromboxanes. Annu. Rev. Biochem. 47, 994-1030.
3. Ushikubi, F., Nakajima, M., Hirata, M., Okuma, M., Fujiwara, M., and Narumiya, S. (1989) Purification of the thromboxane A2/ prostaglandin H2 receptor from human blood platelets. J. Biol. Chem. 264, 16496-16501.
4. 2 receptor. Nature 349, 617-620.
5. Raychowdhury, M. K., Yukawa, M., Collins, L. J., McGrail, S. H., Kent, K. C., and Ware, J. A. (1994) Alternative splicing produces a divergent cytoplasmic tail in the human endothelial thromboxane A2 receptor. J. Biol. Chem. 269, 19256-19261.
6. Hirata, T., Ushikubi, F., Kakizuka, A., Okuma, M., and Narumiya, S. (1996) Opposite coupling to adenylyl cyclase with different sensitivity to Arg60 to Leu mutation. J. Clin. Invest. 97, 949-956.
7. Wu, J., Feng, M., and Ruan, K. H. (2007) Assembling NMR structures for the intracellular loops of the human thromboxane A(2) receptor: Implication of the G. protein-coupling pocket. Arch. Biochem. Biophys. 470, 73-82.
8. Ruan, K. H., Wu, J., So, S. P., Jenkins, L. A., and Ruan, C. H. (2004) NMR structure of the thromboxane A2 receptor ligand recognition pocket. Eur. J. Biochem. 271, 3006-3016.
9. Geng, L., Wu, J., So, S. P., Huang, G., and Ruan, K. H. (2004) Structural and functional characterization of the first intracellular loop of human thromboxane A2 receptor. Arch. Biochem. Biophys. 423, 253-265.
10. Wu, J., So, S. P., and Ruan, K. H. (2003) Solution structure of the third extracellular loop of human thromboxane A2 receptor. Arch. Biochem. Biophys. 414, 287-293.
11. So, S. P., Wu, J., Huang, G., Huang, A., Li, D., and Ruan, K. H. (2003) Identification of residues important for ligand binding of thromboxane A2 receptor in the second extracellular loop using the NMR experiment-guided mutagenesis approach. J. Biol. Chem. 278, 10922-10927.
12. Ruan, K. H., So, S. P., Wu, J., Li, D., Huang, A., and Kung, J. (2001) Solution structure of the second extracellular loop of human thromboxane A2 receptor. Biochemistry 40, 275-280.
13. Cherezov, V., Rosenbaum, D. M., Hanson, M. A., Rasmussen, S. G., Thian, F. S., Kobilka, T. S., Choi, H. J., Kuhn, P., Weis, W. I., Kobilka, B. K., and Stevens, R. C. (2007) High-resolution crystal structure of an engineered human beta 2-adrenergic G. protein-coupled receptor. Science 318, 1258-1265.
14. Ranganathan, R. (2007) Biochemistry. Signaling across the cell membrane. Science 318, 1253-1254.
15. Rosenbaum, D. M., Cherezov, V., Hanson, M. A., Rasmussen, S. G., Thian, F. S., Kobilka, T. S., Choi, H. J., Yao, X. J., Weis, W. I., Stevens, R. C., and Kobilka, B. K. (2007) GPCR engineering yields high-resolution structural insights into beta 2-adrenergic receptor function. Science 318, 1266-1273.
16. Rasmussen, S. G., Choi, H. J., Rosenbaum, D. M., Kobilka, T. S., Thian, F. S., Edwards, P. C., Burghammer, M., Ratnala, V. R., Sanishvili, R., Fischetti, R. F., Schertler, G. F., Weis, W. I., and Kobilka, B. K. (2007) Crystal structure of the human beta 2 adrenergic G-protein-coupled receptor. Nature 450, 383-387.
17. Ruan, K. H., Cervantes, V., and Wu, J. (2008) A simple, quick, and high yield preparation of the human thromboxane A2 receptor in full size for structural studies. Biochemistry 47, 6819-6826.
18. Chiang, N., and Tai, H. H. (1998) The role of N-Glycosylation of human thromboxane A2 receptor in ligand binding. Arch. Biochem. Biophys. 352, 207-213.
19. Chiang, N., Kan, W. M., and Tai, H. H. (1996) Site-directed mutagenesis of cysteinyl and serine residues of human thromboxane A2 receptor in insect cells. Arch. Biochem. Biophys. 334, 9-17.
20. Zhou, H., Yan, F., and Tai, H. H. (2001) Phosphorylation and desensitization of the human thromboxane receptor-alpha by G. protein-coupled receptor. J. Pharmacol. Exp. Ther. 298, 1243-1251.
21. Zhang, L., Huang, G., Wu, J., and Ruan, K. H. (2005) A profile of the residues in the first intracellular loop critical for Gs-mediated signaling of human prostacyclin receptor characterized by an integrative approach of NMR-experiment and mutagenesis. Biochemistry 44, 11389-11401.
22. Lin, Y., Wu, K. K., and Ruan, K-H. (1998) Characterization of the secondary structure and membrane interaction of the putative membrane anchor domain of prostaglandin I2 synthase and cytochrome P450 2C1. Arch. Biochem. Biophys. 352, 78-84.
23. Callihan, D., West, J., Kumar, S., Schweitzer, B. I., and Logan, T. M. (1996) Simple, distortion-free homonuclear spectra of peptides and nucleic acids in water using excitation sculpting. J. Magn. Reson., Ser. B 112, 82-85.
24. Ruan, K. H., So, S. P., Zheng, W., Wu, J., Li, D., and Kung, J. (2002) Solution structure and topology in membrane-bound prostacyclin synthase. Biochem. J. 368, 721-728.
25. Dahms, T. E., and Szabo, A. G. (1995) Probing local secondary structure by fluorescence: time-resolved and circular dichroism studies of highly purified neurotoxins. Biophys. J. 69, 569-576.