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1G1U
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THE 2.5 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE RXRALPHA LIGAND BINDING DOMAIN IN TETRAMER IN THE ABSENCE OF LIGAND
Descriptor:RETINOIC ACID RECEPTOR RXR-ALPHA
Authors:Gampe Jr., R.T., Montana, V.G., Lambert, M.H., Wisely, G.B., Milburn, M.V., Xu, H.E.
Deposit date:2000-10-13
Release date:2001-04-25
Last modified:2017-10-04
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix.
Genes Dev., 14, 2000
1G5Y
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THE 2.0 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE RXRALPHA LIGAND BINDING DOMAIN TETRAMER IN THE PRESENCE OF A NON-ACTIVATING RETINOIC ACID ISOMER.
Descriptor:RETINOIC ACID RECEPTOR RXR-ALPHA, RETINOIC ACID
Authors:Gampe Jr., R.T., Montana, V.G., Lambert, M.H., Wisely, G.B., Milburn, M.V., Xu, H.E.
Deposit date:2000-11-02
Release date:2001-05-02
Last modified:2018-04-25
Method:X-RAY DIFFRACTION (2 Å)
Cite:Structural basis for autorepression of retinoid X receptor by tetramer formation and the AF-2 helix.
Genes Dev., 14, 2000
1KKQ
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CRYSTAL STRUCTURE OF THE HUMAN PPAR-ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH AN ANTAGONIST GW6471 AND A SMRT COREPRESSOR MOTIF
Descriptor:PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR, NUCLEAR RECEPTOR CO-REPRESSOR 2, N-((2S)-2-({(1Z)-1-METHYL-3-OXO-3-[4-(TRIFLUOROMETHYL) PHENYL]PROP-1-ENYL}AMINO)-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL)PROPANAMIDE
Authors:Xu, H.E., Stanley, T.B., Montana, V.G., Lambert, M.H., Shearer, B.G., Cobb, J.E., McKee, D.D., Galardi, C.M., Nolte, R.T., Parks, D.J.
Deposit date:2001-12-10
Release date:2002-02-20
Last modified:2017-10-11
Method:X-RAY DIFFRACTION (3 Å)
Cite:Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha.
Nature, 415, 2002
1C25
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HUMAN CDC25A CATALYTIC DOMAIN
Descriptor:CDC25A
Authors:Fauman, E.B., Cogswell, J.P., Lovejoy, B., Rocque, W.J., Holmes, W., Montana, V.G., Piwnica-Worms, H., Rink, M.J., Saper, M.A.
Deposit date:1998-04-17
Release date:1998-08-19
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Crystal structure of the catalytic domain of the human cell cycle control phosphatase, Cdc25A.
Cell(Cambridge,Mass.), 93, 1998
1FM6
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THE 2.1 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE HETERODIMER OF THE HUMAN RXRALPHA AND PPARGAMMA LIGAND BINDING DOMAINS RESPECTIVELY BOUND WITH 9-CIS RETINOIC ACID AND ROSIGLITAZONE AND CO-ACTIVATOR PEPTIDES.
Descriptor:RETINOIC ACID RECEPTOR RXR-ALPHA, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA, STEROID RECEPTOR COACTIVATOR, ...
Authors:Gampe Jr., R.T., Montana, V.G., Lambert, M.H., Miller, A.B., Bledsoe, R.K., Milburn, M.V., Kliewer, S.A., Willson, T.M., Xu, H.E.
Deposit date:2000-08-16
Release date:2001-02-16
Last modified:2017-10-04
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.
Mol.Cell, 5, 2000
1FM9
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THE 2.1 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE HETERODIMER OF THE HUMAN RXRALPHA AND PPARGAMMA LIGAND BINDING DOMAINS RESPECTIVELY BOUND WITH 9-CIS RETINOIC ACID AND GI262570 AND CO-ACTIVATOR PEPTIDES.
Descriptor:RETINOIC ACID RECEPTOR RXR-ALPHA, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA, STEROID RECEPTOR COACTIVATOR, ...
Authors:Gampe Jr., R.T., Montana, V.G., Lambert, M.H., Miller, A.B., Bledsoe, R.K., Milburn, M.V., Kliewer, S.A., Willson, T.M., Xu, H.E.
Deposit date:2000-08-16
Release date:2001-02-16
Last modified:2018-01-31
Method:X-RAY DIFFRACTION (2.1 Å)
Cite:Asymmetry in the PPARgamma/RXRalpha crystal structure reveals the molecular basis of heterodimerization among nuclear receptors.
Mol.Cell, 5, 2000
1GWX
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MOLECULAR RECOGNITION OF FATTY ACIDS BY PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS
Descriptor:PROTEIN (PPAR-DELTA), 2-(4-{3-[1-[2-(2-CHLORO-6-FLUORO-PHENYL)-ETHYL]-3-(2,3-DICHLORO-PHENYL)-UREIDO]-PROPYL}-PHENOXY)-2-METHYL-PROPIONIC ACID
Authors:Xu, H.E., Lambert, M.H., Montana, V.G., Park, D.J., Blanchard, S., Brown, P., Sternbach, D., Lehmann, J., Bruce, G.W., Willson, T.M., Kliewer, S.A., Milburn, M.V.
Deposit date:1999-03-17
Release date:2000-03-17
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.
Mol.Cell, 3, 1999
1K74
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THE 2.3 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE HETERODIMER OF THE HUMAN PPARGAMMA AND RXRALPHA LIGAND BINDING DOMAINS RESPECTIVELY BOUND WITH GW409544 AND 9-CIS RETINOIC ACID AND CO-ACTIVATOR PEPTIDES.
Descriptor:Retinoic acid receptor RXR-alpha, Peroxisome proliferator activated receptor gamma, steroid receptor coactivator, ...
Authors:Xu, H.E., Lambert, M.H., Montana, V.G., Moore, L.B., Collins, J.L., Oplinger, J.A., Kliewer, S.A., Gampe Jr., R.T., McKee, D.D., Moore, J.T., Willson, T.M.
Deposit date:2001-10-18
Release date:2001-12-05
Last modified:2012-12-26
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
1K7L
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THE 2.5 ANGSTROM RESOLUTION CRYSTAL STRUCTURE OF THE HUMAN PPARALPHA LIGAND BINDING DOMAIN BOUND WITH GW409544 AND A CO-ACTIVATOR PEPTIDE.
Descriptor:Peroxisome proliferator activated receptor alpha, steroid receptor coactivator, 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, ...
Authors:Xu, H.E., Lambert, M.H., Montana, V.G., Moore, L.B., Collins, J.L., Oplinger, J.A., Kliewer, S.A., Gampe Jr., R.T., McKee, D.D., Moore, J.T., Willson, T.M.
Deposit date:2001-10-19
Release date:2001-12-05
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
1M2Z
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CRYSTAL STRUCTURE OF A DIMER COMPLEX OF THE HUMAN GLUCOCORTICOID RECEPTOR LIGAND-BINDING DOMAIN BOUND TO DEXAMETHASONE AND A TIF2 COACTIVATOR MOTIF
Descriptor:glucocorticoid receptor, nuclear receptor coactivator 2, B-OCTYLGLUCOSIDE, ...
Authors:Bledsoe, R.B., Montana, V.G., Stanley, T.B., Delves, C.J., Apolito, C.J., Mckee, D.D., Consler, T.G., Parks, D.J., Stewart, E.L., Willson, T.M., Lambert, M.H., Moore, J.T., Pearce, K.H., Xu, H.E.
Deposit date:2002-06-26
Release date:2003-07-15
Last modified:2017-10-11
Method:X-RAY DIFFRACTION (2.5 Å)
Cite:Crystal Structure of the Glucocorticoid Receptor Ligand Binding Domain Reveals a Novel Mode of Receptor Dimerization and Coactivator Recognition
Cell(Cambridge,Mass.), 110, 2002
1RDT
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CRYSTAL STRUCTURE OF A NEW REXINOID BOUND TO THE RXRALPHA LIGAND BINDING DOAMIN IN THE RXRALPHA/PPARGAMMA HETERODIMER
Descriptor:Retinoic acid receptor RXR-alpha, LxxLL motif coactivator, Peroxisome proliferator activated receptor gamma, ...
Authors:Haffner, C.D., Lenhard, J.M., Miller, A.B., McDougald, D.L., Dwornik, K., Ittoop, O.R., Gampe Jr., R.T., Xu, H.E., Blanchard, S., Montana, V.G.
Deposit date:2003-11-06
Release date:2004-11-09
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:Structure-based design of potent retinoid X receptor alpha agonists.
J.Med.Chem., 47, 2004
1Y0S
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CRYSTAL STRUCTURE OF PPAR DELTA COMPLEXED WITH GW2331
Descriptor:Peroxisome proliferator activated receptor delta, IODIDE ION, (2S)-2-(4-[2-(3-[2,4-DIFLUOROPHENYL]-1-HEPTYLUREIDO)ETHYL]PHENOXY)-2-METHYLBUTYRIC ACID, ...
Authors:Takada, I., Yu, R.T., Xu, H.E., Xu, R.X., Lambert, M.H., Montana, V.G., Kliewer, S.A., Evans, R.M., Umesono, K.
Deposit date:2004-11-16
Release date:2005-03-29
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.65 Å)
Cite:Alteration of a Single Amino Acid in Peroxisome Proliferator-Activated Receptor-alpha (PPARalpha) Generates a PPAR delta Phenotype
MOL.ENDOCRINOL., 14, 2000
2GWX
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MOLECULAR RECOGNITION OF FATTY ACIDS BY PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS
Descriptor:PROTEIN (PPAR-DELTA)
Authors:Xu, H.E., Lambert, M.H., Montana, V.G., Park, D.J., Blanchard, S., Brown, P., Sternbach, D., Lehmann, J., Bruce, G.W., Willson, T.M., Kliewer, S.A., Milburn, M.V.
Deposit date:1999-03-11
Release date:2000-03-11
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.
Mol.Cell, 3, 1999
2P54
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A CRYSTAL STRUCTURE OF PPAR ALPHA BOUND WITH SRC1 PEPTIDE AND GW735
Descriptor:Peroxisome proliferator-activated receptor alpha, Nuclear receptor coactivator 1, 2-METHYL-2-(4-{[({4-METHYL-2-[4-(TRIFLUOROMETHYL)PHENYL]-1,3-THIAZOL-5-YL}CARBONYL)AMINO]METHYL}PHENOXY)PROPANOIC ACID
Authors:Xu, R.X., Xu, H.E., Sierra, M.L., Montana, V.G., Lambert, M.H., Pianetti, P.M.
Deposit date:2007-03-14
Release date:2007-04-24
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (1.79 Å)
Cite:Substituted 2-[(4-Aminomethyl)phenoxy]-2-methylpropionic Acid PPAR Agonists. 1.Discovery of a Novel Series of Potent HDLc Raising Agents.
J.Med.Chem., 50, 2007
3GWX
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MOLECULAR RECOGNITION OF FATTY ACIDS BY PEROXISOME PROLIFERATOR-ACTIVATED RECEPTORS
Descriptor:PROTEIN (PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR (PPAR-DELTA)), 5,8,11,14,17-EICOSAPENTAENOIC ACID
Authors:Xu, H.E., Lambert, M.H., Montana, V.G., Parks, D.J., Blanchard, S.G., Brown, P.J., Sternbach, D.D., Lehmann, J.M., Wisely, G.B., Willson, T.M., Kliewer, S.A., Milburn, M.V.
Deposit date:1999-04-26
Release date:2000-04-26
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:Molecular recognition of fatty acids by peroxisome proliferator-activated receptors.
Mol.Cell, 3, 1999
3B3K
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CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN PPARGAMMA AND THE FULL AGONIST LT175
Descriptor:Peroxisome proliferator-activated receptor gamma, (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid
Authors:Pochetti, G., Montanari, R., Mazza, F., Loiodice, F., Fracchiolla, G., Crestani, M., Godio, C.
Deposit date:2007-10-22
Release date:2008-10-28
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.6 Å)
Cite:Crystal Structure of the Peroxisome Proliferator-Activated Receptor gamma (PPARgamma) Ligand Binding Domain Complexed with a Novel Partial Agonist: A New Region of the Hydrophobic Pocket Could Be Exploited for Drug Design
J.Med.Chem., 51, 2008
2BAW
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HUMAN NUCLEAR RECEPTOR-LIGAND COMPLEX 1
Descriptor:Peroxisome proliferator activated receptor delta, HEPTYL-BETA-D-GLUCOPYRANOSIDE, VACCENIC ACID
Authors:Fyffe, S.A., Alphey, M.S., Buetow, L., Smith, T.K., Ferguson, M.A.J., Sorensen, M.D., Bjorkling, F., Hunter, W.N.
Deposit date:2005-10-15
Release date:2006-01-24
Last modified:2011-09-28
Method:X-RAY DIFFRACTION (2.3 Å)
Cite:Reevaluation of the PPAR-beta/delta Ligand Binding Domain Model Reveals Why It Exhibits the Activated Form
Mol.Cell, 21, 2006
3CDP
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CRYSTAL STRUCTURE OF PPAR-GAMMA LBD COMPLEXED WITH A PARTIAL AGONIST, ANALOGUE OF CLOFIBRIC ACID
Descriptor:Peroxisome proliferator-activated receptor gamma, (2S)-2-(4-chlorophenoxy)-3-phenylpropanoic acid
Authors:Pochetti, G., Montanari, R., Mazza, F.
Deposit date:2008-02-27
Release date:2009-01-13
Last modified:2013-12-25
Method:X-RAY DIFFRACTION (2.8 Å)
Cite:Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors alpha/gamma dual agonists
Bioorg.Med.Chem., 20, 2012
3CDS
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CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN PPAR-GAMMA AND THE AGONIST LT248 (CLOFIBRIC ACID ANALOGUE)
Descriptor:Peroxisome proliferator-activated receptor gamma, (2S)-2-(4-ethylphenoxy)-3-phenylpropanoic acid
Authors:Pochetti, G., Montanari, R., Mazza, F.
Deposit date:2008-02-27
Release date:2008-12-30
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.65 Å)
Cite:Crystal Structure of the Peroxisome Proliferator-Activated Receptor gamma (PPARgamma) Ligand Binding Domain Complexed with a Novel Partial Agonist: A New Region of the Hydrophobic Pocket Could Be Exploited for Drug Design
J.Med.Chem., 51, 2008
3D6D
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CRYSTAL STRUCTURE OF THE COMPLEX BETWEEN PPARGAMMA LBD AND THE LT175(R-ENANTIOMER)
Descriptor:Peroxisome proliferator-activated receptor gamma, (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid
Authors:Pochetti, G., Montanari, R.
Deposit date:2008-05-19
Release date:2008-12-30
Last modified:2011-07-13
Method:X-RAY DIFFRACTION (2.4 Å)
Cite:Crystal Structure of the Peroxisome Proliferator-Activated Receptor gamma (PPARgamma) Ligand Binding Domain Complexed with a Novel Partial Agonist: A New Region of the Hydrophobic Pocket Could Be Exploited for Drug Design
J.Med.Chem., 51, 2008