Peroxisome Proliferator-Activated Receptors

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Crystal Structure of Human PAPRα complex with agonist ([[1i7g]])


3D Structures of PPAR

Updated on 02-September-2014


1k7l – hPPARα LBD + G2409544 + SRC-1 - human
3e94 – hPPARα LBD + tributyltin
4bcr - hPPARα LBD + ligand
1kkq – hPPARα LBD + GW6471 Antagonist + SMRT
2npa - hPPARα LBD+ propanoic acid derivative + SRC-1
2p54 - hPPARα LBD + SRC-1
2rew - hPPARα LBD + azetidinone derivative activator
2znn, 2zno, 2znp, 2znq, 3kdu, 3vi8, 1i7g - hPPARα LBD+ agonist
3fei, 3fej, 3g8i, 3sp6 - hPPARα LBD+ agonist + SRC-1
3et1 - hPPARα LBD + SRC-1 + indole derivative


3prg, 2qmv, 1prg – hPPARγ LBD
2zk0, 2zk1, 2zk2, 2zk3, 2zk4, 2zk5, 2zk6, 3vjh, 3vji, 4e4k, 4e4q, 4jl4 – hPPARγ LBD + ligand
3po9 - hPPARγ LBD + tripropyltin
3r8i - hPPARγ LBD + ureidofibrate derivative
3sz1 - hPPARγ LBD + luteolin
2f4b, 1zeo, 2ath, 2hwq, 2hwr, 2i4j, 2q59, 2q8s, 3b3k, 3bc5, 3cds, 3g9e, 3gbk, 3gz9, 3ia6, 3kdt, 3an3, 3an4, 3noa, 3r5n, 3r8a, 3vso, 3vsp, 2xkw, 3b0q, 3ho0, 3hod, 1knu, 1i7i, 1nyx, 2pob – hPPARγ LBD+ agonists
2g0h, 2g0g, 2i4p, 2i4z, 2q5g, 2q5p, 2q5s, 2q61, 2q6r, 3cdp, 3d6d, 4em9, 4ema, 4prg, 2q6s - hPPARγ LBD+ partial agonists
2om9 - hPPARγ LBD + cannabinoid
3b0r - hPPARγ LBD + antagonist
3osi, 3osw, 3pba - hPPARγ LBD + bisphenol derivative
2p4y, 3adt, 3adu, 3adw, 3et3, 2hfp - hPPARγ LBD+ modulator
2zvt - hPPARγ LBD (mutant) + modulator
2vsr, 2vst, 2vv0, 2vv1, 2vv2, 2vv3, 2vv4 - hPPARγ LBD + fatty acid activator
3ads, 3adx - hPPARγ LBD + indomethacin
3adv - hPPARγ LBD + serotonin
3k8s, 3et0, 2yfe, 4a4v, 4a4w, 4jaz - hPPARγ LBD + antidiabetic drug

PPARγ complex with polypeptide

1wm0 – hPPARγ LBD+ NCAO2 peptide + agonist
1zgy – hPPARγ LBD+ antidiabetic drug + nuclear receptor peptide
2gtk, 3qt0 - hPPARγ LBD+ SRC-1 peptide
3cs8, 3u9q- hPPARγ LBD + PGC-1A peptide
3cwd - hPPARγ LBD + SRC1-2 peptide
3fur, 3kmg, 3v9t, 3v9v, 3v9y, 4f9m, 3b1m - hPPARγ LBD + SRC-1 peptide + modulator
4fgy, 2prg - hPPARγ LBD + antidiabetic agent + NCOA1 peptide
3s9s, 3t03, 2fvj- hPPARγ LBD + SRC-1 peptide + partial agonist
3h0a - hPPARγ LBD + SRC 1 + retinoic acid receptor α + retinoic acid + partial agonist
1k74, 1rdt, 1fm9 - hPPARγ LBD + SRC-1 + retinoic acid receptor α + retinoic acid + agonist
3dzu, 3e00, 3dzy - hPPARγ LBD + DNA + retinoic acid receptor α + NCOA2 peptide + retinoic acid
1fm6 - hPPARγ LBD + antidiabetic drug + retinoic acid receptor α + NCOA2 peptide + retinoic acid
3vn2, 4hee, 4prg - hPPARγ LBD + NCOA1 peptide + activator


2baw, 2b50, 2awh – hPPARδ + Vaccenic Acid
2gwx – hPPARδ LBD
3gwx –hPPARδ LBD + 5,8,11,14,17-Eicosapentaenoic Acid
1y0s – hPPARδ LBD + GW2331
3dy6 –hPPARδ LBD + anthranilic acid
3et2, 1gwx – PPARδ + fatty acid
2env – hPPARδ zinc finger domain
2j14, 2xyj, 2xyw, 2xyx, 3oz0, 3sp9 - hPPARδ LBD + agonist
3peq - hPPARδ LBD + partial agonist
3d5f - hPPARδ LBD +phenoxy derivative

Additional Resources


  1. 1.0 1.1 1.2 1.3 Berger J, Moller DE. The mechanisms of action of PPARs. Annu Rev Med. 2002;53:409-35. PMID:11818483 doi:10.1146/
  2. Qi C, Zhu Y, Reddy JK. Peroxisome proliferator-activated receptors, coactivators, and downstream targets. Cell Biochem Biophys. 2000;32 Spring:187-204. PMID:11330046
  3. Guan HP, Ishizuka T, Chui PC, Lehrke M, Lazar MA. Corepressors selectively control the transcriptional activity of PPARgamma in adipocytes. Genes Dev. 2005 Feb 15;19(4):453-61. Epub 2005 Jan 28. PMID:15681609 doi:10.1101/gad.1263305
  4. Lee SS, Pineau T, Drago J, Lee EJ, Owens JW, Kroetz DL, Fernandez-Salguero PM, Westphal H, Gonzalez FJ. Targeted disruption of the alpha isoform of the peroxisome proliferator-activated receptor gene in mice results in abolishment of the pleiotropic effects of peroxisome proliferators. Mol Cell Biol. 1995 Jun;15(6):3012-22. PMID:7539101
  5. Lee SK, Jung SY, Kim YS, Na SY, Lee YC, Lee JW. Two distinct nuclear receptor-interaction domains and CREB-binding protein-dependent transactivation function of activating signal cointegrator-2. Mol Endocrinol. 2001 Feb;15(2):241-54. PMID:11158331
  6. Chen D, Ma H, Hong H, Koh SS, Huang SM, Schurter BT, Aswad DW, Stallcup MR. Regulation of transcription by a protein methyltransferase. Science. 1999 Jun 25;284(5423):2174-7. PMID:10381882
  7. Fajas L, Auboeuf D, Raspe E, Schoonjans K, Lefebvre AM, Saladin R, Najib J, Laville M, Fruchart JC, Deeb S, Vidal-Puig A, Flier J, Briggs MR, Staels B, Vidal H, Auwerx J. The organization, promoter analysis, and expression of the human PPARgamma gene. J Biol Chem. 1997 Jul 25;272(30):18779-89. PMID:9228052
  8. Girroir EE, Hollingshead HE, He P, Zhu B, Perdew GH, Peters JM. Quantitative expression patterns of peroxisome proliferator-activated receptor-beta/delta (PPARbeta/delta) protein in mice. Biochem Biophys Res Commun. 2008 Jul 4;371(3):456-61. Epub 2008 Apr 28. PMID:18442472 doi:10.1016/j.bbrc.2008.04.086
  9. Leone TC, Weinheimer CJ, Kelly DP. A critical role for the peroxisome proliferator-activated receptor alpha (PPARalpha) in the cellular fasting response: the PPARalpha-null mouse as a model of fatty acid oxidation disorders. Proc Natl Acad Sci U S A. 1999 Jun 22;96(13):7473-8. PMID:10377439
  10. Gottlicher M, Widmark E, Li Q, Gustafsson JA. Fatty acids activate a chimera of the clofibric acid-activated receptor and the glucocorticoid receptor. Proc Natl Acad Sci U S A. 1992 May 15;89(10):4653-7. PMID:1316614
  11. Amri EZ, Bonino F, Ailhaud G, Abumrad NA, Grimaldi PA. Cloning of a protein that mediates transcriptional effects of fatty acids in preadipocytes. Homology to peroxisome proliferator-activated receptors. J Biol Chem. 1995 Feb 3;270(5):2367-71. PMID:7836471
  12. 12.0 12.1 12.2 Nolte RT, Wisely GB, Westin S, Cobb JE, Lambert MH, Kurokawa R, Rosenfeld MG, Willson TM, Glass CK, Milburn MV. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma. Nature. 1998 Sep 10;395(6698):137-43. PMID:9744270 doi:10.1038/25931
  13. Fyffe SA, Alphey MS, Buetow L, Smith TK, Ferguson MA, Sorensen MD, Bjorkling F, Hunter WN. Recombinant human PPAR-beta/delta ligand-binding domain is locked in an activated conformation by endogenous fatty acids. J Mol Biol. 2006 Mar 3;356(4):1005-13. Epub 2006 Jan 4. PMID:16405912 doi:10.1016/j.jmb.2005.12.047
  14. Yang W, Rachez C, Freedman LP. Discrete roles for peroxisome proliferator-activated receptor gamma and retinoid X receptor in recruiting nuclear receptor coactivators. Mol Cell Biol. 2000 Nov;20(21):8008-17. PMID:11027271
  15. 15.0 15.1 15.2 15.3 15.4 Zoete V, Grosdidier A, Michielin O. Peroxisome proliferator-activated receptor structures: ligand specificity, molecular switch and interactions with regulators. Biochim Biophys Acta. 2007 Aug;1771(8):915-25. Epub 2007 Jan 18. PMID:17317294 doi:10.1016/j.bbalip.2007.01.007
  16. 16.0 16.1 16.2 Gampe RT Jr, Montana VG, Lambert MH, Miller AB, Bledsoe RK, Milburn MV, Kliewer SA, Willson TM, Xu HE. Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors. Mol Cell. 2000 Mar;5(3):545-55. PMID:10882139
  17. Xu HE, Lambert MH, Montana VG, Plunket KD, Moore LB, Collins JL, Oplinger JA, Kliewer SA, Gampe RT Jr, McKee DD, Moore JT, Willson TM. Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors. Proc Natl Acad Sci U S A. 2001 Nov 20;98(24):13919-24. Epub 2001 Nov 6. PMID:11698662 doi:10.1073/pnas.241410198
  18. Wahli W, Braissant O, Desvergne B. Peroxisome proliferator activated receptors: transcriptional regulators of adipogenesis, lipid metabolism and more.... Chem Biol. 1995 May;2(5):261-6. PMID:9383428
  19. Chandra V, Huang P, Hamuro Y, Raghuram S, Wang Y, Burris TP, Rastinejad F. Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA. Nature. 2008 Nov 20;456(7220):350-6. PMID:19043829 doi:10.1038/nature07413
  20. 20.0 20.1 Berger J, Wagner JA. Physiological and therapeutic roles of peroxisome proliferator-activated receptors. Diabetes Technol Ther. 2002;4(2):163-74. PMID:12079620

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