Recombinant human PPAR-β/δ ligand-binding domain is locked in an activated conformation by endogenous fatty acids

Journal of Molecular Biology

Volumn 356, Issue 4, 2006, Pages 1005-1013

  Fyffe, Stewart A ^a   Alphey, Magnus S ^a   Buetow, Lori ^a   Smith, Terry K ^a   Ferguson, Michael A J ^a   Sørensen, Morten D ^b   Björkling, Fredrik ^b,c   Hunter, William N ^a  

^a UNIVERSITY OF DUNDEE   (United Kingdom)

^b LEO PHARMA A S   (Denmark)

^c BioAlliance Pharma   (France)

Author keywords

Crystal structure; Fatty acid; Ligand binding domain; Mass spectrometry; Nuclear receptor

Indexed keywords

FATTY ACID; GLUCOPYRANOSIDE; N HEPTYL BETA DEXTRO GLUCOPYRANOSIDE; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA; RECOMBINANT RECEPTOR; UNCLASSIFIED DRUG; VACCENIC ACID;

ARTICLE; BINDING SITE; CONFORMATION; CRYSTALLIZATION; FATTY ACID ANALYSIS; GENE EXPRESSION SYSTEM; MASS SPECTROMETRY; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN FOLDING; PROTEIN INTERACTION;

BACTERIA (MICROORGANISMS);

EID: 31344456486     PISSN: 00222836     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.jmb.2005.12.047     Document Type: Article

References (29)

1. J. Berger, and D.E. Moller The mechanisms of action of PPARs Annu. Rev. Med. 53 2002 409 435
2. T.M. Willson, P.J. Brown, D.D. Sternbach, and B.R. Henke The PPARs: from orphan receptors to drug discovery J. Med. Chem. 43 2000 527 550
3. J.K. Reddy, and T. Hashimoto Peroxisomal β-oxidation and peroxisome proliferator-activated recepto α: an adaptive metabolic system Annu. Rev. Nutr. 21 2001 193 230
4. C.A.N. Palmer, M. Hsu, K.J. Griffin, J.L. Raucy, and E.F. Johnson Peroxisome proliferator activated receptor-α expression in human liver Mol. Pharm. 53 1998 14 22
5. R.T. Nolte, G.B. Wisely, S. Westin, J.E. Cobb, M.H. Lambert, and R. Kurokawa Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma Nature 395 1998 137 143
6. J.P. Berger, T.E. Akiyama, and P.T. Meinke PPARs: therapeutic targets for metabolic disease Trends Pharm. Sci. 26 2005 244 251
7. A. Fredenrich, and P.A. Grimaldi PPAR delta: an uncompletely known nuclear receptor Diabetes Metab. 31 2005 23 27
8. H.E. Xu, M.H. Lambert, V.G. Montana, D.J. Parks, S.G. Blanchard, and P.J. Brown Molecular recognition of fatty acids by peroxisome proliferator-activated receptors Mol. Cell 3 1999 397 403
9. D. Wang, H. Wang, Q. Shi, S. Katkuri, W. Walhi, and B. Desvergne Prostaglandin E(2) promotes colorectal adenoma growth via transactivation of the nuclear peroxisome proliferator-activated receptor δ Cancer Cell 6 2004 285 295
10. J.M. Wallace, M. Schwarz, P. Coward, J. Houze, J.K. Sawyer, and K.L. Kelley Effects of peroxisome proliferator-activated receptor alpha/delta agonists on HDL-cholesterol in vervet monkeys J. Lipid Res. 46 2005 1009 1016
11. P. Cronet, J.F. Petersen, R. Folmer, N. Blomberg, K. Sjoblom, and U. Karlsson Structure of the PPAR alpha and gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family Structure 9 2001 699 706
12. Y. Li, M.H. Lambert, and H.E. Xu Activation of nuclear receptors: a perspective from structural genomics Structure 11 2003 741 746
13. F. Molnár, M. Matilainen, and C. Carlberg Structural determinants of the agonist-independent association of human peroxisome proliferator- activated receptors with coactivators J. Biol. Chem. 280 2005 26543 26556
14. D. Moras, and H. Gronemeyer The nuclear receptor ligand-binding domain: structure and function Curr. Opin. Cell Biol. 10 1998 384 391
15. C. Ratledge, and S.G. Wilkinson Microbal Lipids 1 1988 Academic Press New York, USA
16. S. Ebdrup, I. Pettersson, H.B. Rasmussen, H.J. Deussen, A. Frost Jensen, and S.B. Mortensen Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar J. Med. Chem. 46 2003 1306 1317
17. B.P. Klaholz, and D. Moras Structural role of a detergent molecule in retinoic acid nuclear receptor crystals Acta Crystallog. sect. D 56 2000 933 935
18. S. Dhe-Paganon, K. Duda, M. Iwamoto, Y.I. Chi, and S.E. Shoelson Crystal structure of the HNF4 alpha ligand binding domain in complex with endogenous fatty acid ligand J. Biol. Chem. 277 2002 37973 37976
19. G.B. Wisely, A.B. Miller, R.G. Davis, A.D. Thornquest Jr, R. Johnson, and T. Spitzer Hepatocyte nuclear factor 4 is a transcription factor that constitutively binds fatty acids Structure 10 2002 1225 1234
20. I.N. Krylova, E.P. Sablin, J. Moore, R.X. Xu, G.M. Waitt, and J.A. MacKay Structural analyses reveal phosphatidyl inositols as ligands for the NR5 orphan receptors SF-1 and LRH-1 Cell 120 2005 343 355
21. W. Bourguet, V. Vivat, J.M. Wurtz, P. Chambon, H. Gronemeyer, and D. Moras Crystal structure of a heterodimeric complex of RAR and RXR ligand-binding domains Mol. Cell 5 2000 289 298
22. I.M.L. Billas, L. Moulinier, N. Rochel, and D. Moras Crystal structure of the ligand-binding domain of the ultraspiracle protein USP, the ortholog of retinoid X receptors in insects J. Biol. Chem. 276 2001 7465 7474
23. Y.X. Wang, C.L. Zhang, R.T. Yu, H.K. Cho, M.C. Nelson, and C.R. Bayuga-Ocampo Regulation of muscle fiber type and running endurance by PPARδ PLoS Biol. 2 2004 1 8
24. H.R. Powell The Rossmann Fourier autoindexing algorithm in MOSFLM Acta Crystallog. sect. D 55 1999 1690 1695
25. Collaborative Computational Project, Number 4 CCP4 suite: programs for protein crystallography Acta Crystallog. sect. D 50 1994 760 763
26. A. Vagin, and A. Teplyakov An approach to multi-copy search in molecular replacement Acta Crystallog. sect. D 56 2000 1622 1624
27. T.A. Jones, J.Y. Zou, S.W. Cowan, and M. Kjeldgaard Improved methods for building protein models in electron density maps and the location of errors in these models Acta Crystallog. sect. A 47 1991 110 119
28. G.N. Murshudov, A.A. Vagin, A. Lebedev, K.S. Wilson, and E.J. Dodson Efficient anisotropic refinement of macromolecular structures using FFT Acta Crystallog. sect. D 55 1999 247 255
29. D.W.J. Cruikshank Remarks about protein structure precision Acta Crystallog. sect. D 55 1999 583 601