8WFE
 
 | | The Crystal Structure of PPARg from Biortus. | | Descriptor: | 1,2-ETHANEDIOL, DI(HYDROXYETHYL)ETHER, Peroxisome proliferator-activated receptor gamma | | Authors: | Wang, F, Cheng, W, Lv, Z, Guo, S, Lin, D. | | Deposit date: | 2023-09-19 | | Release date: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | The Crystal Structure of PPARg from Biortus.
To Be Published
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2Q59
 | | Crystal Structure of PPARgamma LBD bound to full agonist MRL20 | | Descriptor: | (2S)-2-(2-{[1-(4-METHOXYBENZOYL)-2-METHYL-5-(TRIFLUOROMETHOXY)-1H-INDOL-3-YL]METHYL}PHENOXY)PROPANOIC ACID, Peroxisome Proliferator-Activated Receptor gamma | | Authors: | Bruning, J.B, Nettles, K.W. | | Deposit date: | 2007-05-31 | | Release date: | 2007-10-23 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Partial Agonists Activate PPARgamma Using a Helix 12 Independent Mechanism
Structure, 15, 2007
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7CXK
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2VV1
 | | hPPARgamma Ligand binding domain in complex with 4-HDHA | | Descriptor: | (4S,5E,7Z,10Z,13Z,16Z,19Z)-4-hydroxydocosa-5,7,10,13,16,19-hexaenoic acid, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA | | Authors: | Itoh, T, Fairall, L, Schwabe, J.W.R. | | Deposit date: | 2008-06-02 | | Release date: | 2008-08-19 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids
Nat.Struct.Mol.Biol., 15, 2008
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8B93
 | | Crystal structure of PPARG and NCOR2 with an inverse agonist (compound 15b) | | Descriptor: | 4-chloranyl-6-fluoranyl-~{N}1-[[4-fluoranyl-2-(2-methoxyethoxymethyl)phenyl]methyl]-~{N}3-[2-methyl-4-(trifluoromethyl)phenyl]benzene-1,3-dicarboxamide, Nuclear receptor corepressor 2, Peroxisome proliferator-activated receptor gamma | | Authors: | Friberg, A, Orsi, D.L, Pook, E, Siegel, S, Lemke, C.T, Stellfeld, T, Puetter, V, Goldstein, J. | | Deposit date: | 2022-10-05 | | Release date: | 2022-12-28 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.21 Å) | | Cite: | Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Bioorg.Med.Chem., 78, 2022
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6T1V
 | | Structure of PPARg H494Y mutant in complex with GW1929 | | Descriptor: | (2~{S})-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]-2-[[2-(phenylcarbonyl)phenyl]amino]propanoic acid, Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor gamma coactivator 1-alpha | | Authors: | Rochel, N. | | Deposit date: | 2019-10-06 | | Release date: | 2021-04-14 | | Last modified: | 2024-02-07 | | Method: | X-RAY DIFFRACTION (2.21 Å) | | Cite: | Structure of a PPARg mutant complex
To Be Published
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8FKD
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4R06
 | | Crystal Structure of SR2067 bound to PPARgamma | | Descriptor: | 1-(naphthalen-1-ylsulfonyl)-N-[(1S)-1-phenylpropyl]-1H-indole-5-carboxamide, Peroxisome proliferator-activated receptor gamma, SULFATE ION | | Authors: | Marrewijk, L, Kamenecka, T, Griffin, P.R, Bruning, J.B. | | Deposit date: | 2014-07-30 | | Release date: | 2016-01-27 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.22 Å) | | Cite: | SR2067 Reveals a Unique Kinetic and Structural Signature for PPAR gamma Partial Agonism.
Acs Chem.Biol., 11, 2016
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8B8Z
 | | Crystal structure of mutant PPARG (C313A) and NCOR2 with an inverse agonist (compound 7e) | | Descriptor: | 4,5-bis(chloranyl)-~{N}3-phenyl-~{N}1-(phenylmethyl)benzene-1,3-dicarboxamide, Nuclear receptor corepressor 2, Peroxisome proliferator-activated receptor gamma | | Authors: | Friberg, A, Orsi, D.L, Pook, E, Siegel, S, Lemke, C.T, Stellfeld, T, Puetter, V, Goldstein, J. | | Deposit date: | 2022-10-05 | | Release date: | 2022-12-28 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.22 Å) | | Cite: | Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Bioorg.Med.Chem., 78, 2022
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4XUH
 | | PPARgamma ligand binding domain in complex with sulindac sulfide | | Descriptor: | 2-[(3Z)-6-fluoranyl-2-methyl-3-[(4-methylsulfanylphenyl)methylidene]inden-1-yl]ethanoic acid, Peroxisome proliferator-activated receptor gamma | | Authors: | Puhl, A.C, Polikaporv, I, Webb, P. | | Deposit date: | 2015-01-25 | | Release date: | 2016-07-27 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.22 Å) | | Cite: | Mechanisms of peroxisome proliferator activated receptor gamma regulation by non-steroidal anti-inflammatory drugs.
Nucl Recept Signal, 13, 2015
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3VJH
 | | Human PPAR GAMMA ligand binding domain in complex with JKPL35 | | Descriptor: | (2S)-2-[4-methoxy-3-({[4-(trifluoromethyl)benzoyl]amino}methyl)benzyl]pentanoic acid, Peroxisome proliferator-activated receptor gamma | | Authors: | Tomioka, D, Kuwabara, N, Hashimoto, H, Sato, M, Shimizu, T. | | Deposit date: | 2011-10-20 | | Release date: | 2012-08-29 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (2.22 Å) | | Cite: | Peroxisome proliferator-activated receptors (PPARs) have multiple binding points that accommodate ligands in various conformations: phenylpropanoic acid-type PPAR ligands bind to PPAR in different conformations, depending on the subtype.
J.Med.Chem., 55, 2012
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8B91
 | | Crystal structure of mutant PPARG (C313A) and NCOR2 with an inverse agonist (compound SI-1) | | Descriptor: | Nuclear receptor corepressor 2, Peroxisome proliferator-activated receptor gamma, ~{N}3-[4-[bis(fluoranyl)methoxy]-3-fluoranyl-phenyl]-4-chloranyl-6-fluoranyl-~{N}1-[(2-methoxyphenyl)methyl]benzene-1,3-dicarboxamide | | Authors: | Friberg, A, Orsi, D.L, Pook, E, Siegel, S, Lemke, C.T, Stellfeld, T, Puetter, V, Goldstein, J. | | Deposit date: | 2022-10-05 | | Release date: | 2022-12-28 | | Last modified: | 2024-05-01 | | Method: | X-RAY DIFFRACTION (2.23 Å) | | Cite: | Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Bioorg.Med.Chem., 78, 2022
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6MD4
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5TTO
 | | X-ray crystal structure of PPARgamma in complex with SR1643 | | Descriptor: | 4-bromo-N-{3,5-dichloro-4-[(quinolin-3-yl)oxy]phenyl}-2,5-difluorobenzene-1-sulfonamide, Peroxisome proliferator-activated receptor gamma | | Authors: | Bruning, J.B, Frkic, R.L, Griffin, P, Kamenecka, T, Abell, A. | | Deposit date: | 2016-11-04 | | Release date: | 2017-05-24 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.246 Å) | | Cite: | Structure-Activity Relationship of 2,4-Dichloro-N-(3,5-dichloro-4-(quinolin-3-yloxy)phenyl)benzenesulfonamide (INT131) Analogs for PPAR gamma-Targeted Antidiabetics.
J. Med. Chem., 60, 2017
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5F9B
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2P4Y
 | | Crystal structure of human PPAR-gamma-ligand binding domain complexed with an indole-based modulator | | Descriptor: | (2R)-2-(4-CHLORO-3-{[3-(6-METHOXY-1,2-BENZISOXAZOL-3-YL)-2-METHYL-6-(TRIFLUOROMETHOXY)-1H-INDOL-1-YL]METHYL}PHENOXY)PROPANOIC ACID, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Peroxisome proliferator-activated receptor gamma | | Authors: | McKeever, B.M. | | Deposit date: | 2007-03-13 | | Release date: | 2008-01-08 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | The differential interactions of peroxisome proliferator-activated receptor gamma ligands with Tyr473 is a physical basis for their unique biological activities.
Mol.Pharmacol., 73, 2008
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3ADS
 | | Human PPARgamma ligand-binding domain in complex with indomethacin | | Descriptor: | INDOMETHACIN, Peroxisome proliferator-activated receptor gamma | | Authors: | Waku, T, Shiraki, T, Oyama, T, Morikawa, K. | | Deposit date: | 2010-01-29 | | Release date: | 2010-12-22 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.25 Å) | | Cite: | The nuclear receptor PPARgamma individually responds to serotonin- and fatty acid-metabolites
Embo J., 29, 2010
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2I4Z
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6C1I
 | | Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with T0070907 | | Descriptor: | 2-chloro-5-nitro-N-(pyridin-4-yl)benzamide, Peroxisome proliferator-activated receptor gamma, nonanoic acid | | Authors: | Shang, J, Fuhrmann, J, Brust, R, Kojetin, D.J. | | Deposit date: | 2018-01-04 | | Release date: | 2018-12-12 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (2.26 Å) | | Cite: | A structural mechanism for directing corepressor-selective inverse agonism of PPAR gamma.
Nat Commun, 9, 2018
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2ZK2
 | | Human peroxisome proliferator-activated receptor gamma ligand binding domain complexed with glutathion conjugated 15-deoxy-delta12,14-prostaglandin J2 | | Descriptor: | (5E,14E)-11-oxoprosta-5,9,12,14-tetraen-1-oic acid, GLUTATHIONE, Peroxisome proliferator-activated receptor gamma | | Authors: | Waku, T, Shiraki, T, Oyama, T, Fujimoto, Y, Morikawa, K. | | Deposit date: | 2008-03-12 | | Release date: | 2009-02-24 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.26 Å) | | Cite: | Structural insight into PPARgamma activation through covalent modification with endogenous fatty acids
J.Mol.Biol., 385, 2009
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6VZO
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3BC5
 | | X-ray crystal structure of human ppar gamma with 2-(5-(3-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)benzyl)-2-phenyl-2h-1,2,3-triazol-4-yl)acetic acid | | Descriptor: | (5-{3-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]benzyl}-2-phenyl-2H-1,2,3-triazol-4-yl)acetic acid, Peroxisome proliferator-activated receptor gamma | | Authors: | Muckelbauer, J.K. | | Deposit date: | 2007-11-12 | | Release date: | 2008-11-18 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.27 Å) | | Cite: | Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.
Bioorg.Med.Chem.Lett., 19, 2009
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3ADV
 | | Human PPARgamma ligand-binding domain in complex with serotonin | | Descriptor: | Peroxisome proliferator-activated receptor gamma, SEROTONIN | | Authors: | Waku, T, Shiraki, T, Oyama, T, Morikawa, K. | | Deposit date: | 2010-01-29 | | Release date: | 2010-12-22 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.27 Å) | | Cite: | The nuclear receptor PPARgamma individually responds to serotonin- and fatty acid-metabolites
Embo J., 29, 2010
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4L98
 | | Crystal structure of the complex of F360L PPARgamma mutant with the ligand LT175 | | Descriptor: | (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid, Peroxisome proliferator-activated receptor gamma | | Authors: | Pochetti, G, Montanari, R, Consalvi, V, Chiaraluce, R, Pasquo, A, Capelli, D, Loiodice, F, Laghezza, A, Lori, C. | | Deposit date: | 2013-06-18 | | Release date: | 2014-06-25 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Structural basis of the transactivation deficiency of the human PPAR gamma F360L mutant associated with familial partial lipodystrophy.
Acta Crystallogr.,Sect.D, 70, 2014
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2ATH
 | | Crystal structure of the ligand binding domain of human PPAR-gamma im complex with an agonist | | Descriptor: | 2-{5-[3-(7-PROPYL-3-TRIFLUOROMETHYLBENZO[D]ISOXAZOL-6-YLOXY)PROPOXY]INDOL-1-YL}ETHANOIC ACID, Peroxisome proliferator activated receptor gamma | | Authors: | Mahindroo, N, Huang, C.-F, Wu, S.-Y, Hsieh, H.-P. | | Deposit date: | 2005-08-25 | | Release date: | 2006-08-25 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.28 Å) | | Cite: | Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities
J.Med.Chem., 48, 2005
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