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PDB: 303 件

4XTA
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MECHANISMS OF PPARgamma ACTIVATION BY NON-STEROIDAL ANTI-INFLAMMATORY DRUGS
分子名称: 2-[2,6-DICHLOROPHENYL)AMINO]BENZENEACETIC ACID, Peroxisome proliferator-activated receptor gamma
著者Puhl, A.C, Webb, P, Polikarpov, I.
登録日2015-01-23
公開日2015-11-11
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Mechanisms of peroxisome proliferator activated receptor gamma regulation by non-steroidal anti-inflammatory drugs.
Nucl Recept Signal, 13, 2015
1ZEO
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Crystal Structure of Human PPAR-gamma Ligand Binding Domain Complexed with an Alpha-Aryloxyphenylacetic Acid Agonist
分子名称: (2S)-(4-ISOPROPYLPHENYL)[(2-METHYL-3-OXO-5,7-DIPROPYL-2,3-DIHYDRO-1,2-BENZISOXAZOL-6-YL)OXY]ACETATE, Peroxisome proliferator activated receptor gamma
著者Shi, G.Q, Dropinski, J.F, McKeever, B.M, Adams, A.D, MacNaul, K.L, Elbrecht, A, Berger, J.P, Zhou, G, Doebber, T.W.
登録日2005-04-19
公開日2006-04-25
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Design and Synthesis of alpha-Aryloxyphenylacetic Acid Derivatives: A Novel Class of PPAR alpha/gamma Dual Agonists with Potent Antihyperglycemic and Lipid Modulating Activity
J.Med.Chem., 48, 2005
7RLE
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Crystal structure of PPAR gamma in complex with CREB-binding protein and agonist GW1929
分子名称: (2~{S})-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]-2-[[2-(phenylcarbonyl)phenyl]amino]propanoic acid, CREB-binding protein, Peroxisome proliferator-activated receptor gamma
著者Nemetchek, M.D, Sprang, S.R, Hughes, T.S.
登録日2021-07-23
公開日2022-08-03
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献A structural mechanism of nuclear receptor biased agonism.
Proc.Natl.Acad.Sci.USA, 119, 2022
4JL4
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Crystal structure of the complex between PPARgamma LBD and the ligand LJ570 [(2S)-3-(biphenyl-4-yl)-2-(biphenyl-4-yloxy)propanoic acid]
分子名称: (2S)-3-(biphenyl-4-yl)-2-(biphenyl-4-yloxy)propanoic acid, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Capelli, D.
登録日2013-03-12
公開日2014-03-12
最終更新日2024-05-22
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Identification of the First PPAR alpha / gamma Dual Agonist Able To Bind to Canonical and Alternative Sites of PPAR gamma and To Inhibit Its Cdk5-Mediated Phosphorylation.
J.Med.Chem., 61, 2018
8DSZ
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PPARg bound to partial agonist H3B-487
分子名称: (2R)-2-{5-[(5-{[(1R)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-2-chlorophenoxy}propanoic acid, Peroxisome proliferator-activated receptor gamma
著者Larsen, N.A.
登録日2022-07-24
公開日2022-09-07
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Biochemical and structural basis for the pharmacological inhibition of nuclear hormone receptor PPAR gamma by inverse agonists.
J.Biol.Chem., 298, 2022
4E4K
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Crystal Structure of PPARgamma with the ligand JO21
分子名称: (2S)-3-phenyl-2-{[2'-(propan-2-yl)biphenyl-4-yl]oxy}propanoic acid, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Loiodice, F, Fracchiolla, G, Laghezza, A, Carbonara, G, Piemontese, L, Lavecchia, A, Novellino, E.
登録日2012-03-13
公開日2013-01-23
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献New 2-(Aryloxy)-3-phenylpropanoic Acids as Peroxisome Proliferator-Activated Receptor alpha/gamma Dual Agonists Able To Upregulate Mitochondrial Carnitine Shuttle System Gene Expression.
J.Med.Chem., 56, 2013
4E4Q
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Crystal structure of PPARgamma with the ligand FS214
分子名称: (2R)-3-phenyl-2-{[2'-(propan-2-yl)biphenyl-4-yl]oxy}propanoic acid, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Loiodice, F, Fracchiolla, G, Laghezza, A, Carbonara, G, Piemontese, L, Lavecchia, A, Novellino, E.
登録日2012-03-13
公開日2013-01-23
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献New 2-(Aryloxy)-3-phenylpropanoic Acids as Peroxisome Proliferator-Activated Receptor alpha/gamma Dual Agonists Able To Upregulate Mitochondrial Carnitine Shuttle System Gene Expression.
J.Med.Chem., 56, 2013
1KNU
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LIGAND BINDING DOMAIN OF THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA IN COMPLEX WITH A SYNTHETIC AGONIST
分子名称: (S)-3-(4-(2-CARBAZOL-9-YL-ETHOXY)-PHENYL)-2-ETHOXY-PROPIONIC ACID, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA
著者Svensson, L.A, Mortensen, S.B, Fleckner, J, Woeldike, H.F.
登録日2001-12-19
公開日2002-12-19
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity
J.MED.CHEM., 45, 2002
4HEE
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Crystal structure of PPARgamma in complex with compound 13
分子名称: 5-benzyl-2-ethyl-3-{(1S)-5-[2-(1H-tetrazol-5-yl)phenyl]-2,3-dihydro-1H-inden-1-yl}-3,5-dihydro-4H-imidazo[4,5-c]pyridin-4-one, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Han, S.
登録日2012-10-03
公開日2013-08-21
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-gamma
Bioorg.Med.Chem.Lett., 23, 2013
7CXE
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The ligand-free structure of human PPARgamma LBD R280C mutant
分子名称: Peroxisome proliferator-activated receptor gamma
著者Jang, D.M, Han, B.W.
登録日2020-09-01
公開日2021-09-01
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.5 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
6O67
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Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Mitoglitazone
分子名称: Mitoglitazone, Peroxisome proliferator-activated receptor gamma, nonanoic acid
著者Shang, J, Kojetin, D.J.
登録日2019-03-05
公開日2019-11-06
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.52 Å)
主引用文献Quantitative structural assessment of graded receptor agonism.
Proc.Natl.Acad.Sci.USA, 116, 2019
7WGP
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X-ray structure of human PPAR gamma ligand binding domain-fenofibric acid co-crystals obtained by co-crystallization
分子名称: 15-meric peptide from Nuclear receptor coactivator 1, 2-[4-(4-chlorobenzene-1-carbonyl)phenoxy]-2-methylpropanoic acid, Isoform 1 of Peroxisome proliferator-activated receptor gamma
著者Kamata, S, Honda, A, Akahane, M, Machida, Y, Uchii, K, Shiiyama, Y, Masuda, R, Oyama, T, Ishii, I.
登録日2021-12-28
公開日2022-05-25
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.53 Å)
主引用文献Functional and Structural Insights into Human PPAR alpha / delta / gamma Subtype Selectivity of Bezafibrate, Fenofibric Acid, and Pemafibrate.
Int J Mol Sci, 23, 2022
2G0G
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Structure-based drug design of a novel family of PPAR partial agonists: virtual screening, x-ray crystallography and in vitro/in vivo biological activities
分子名称: 3-FLUORO-N-[1-(4-FLUOROPHENYL)-3-(2-THIENYL)-1H-PYRAZOL-5-YL]BENZENESULFONAMIDE, Peroxisome proliferator-activated receptor gamma
著者Lu, I.L, Peng, Y.H, Huang, C.F, Lin, Y.T, Hsu, J.T.A, Wu, S.Y.
登録日2006-02-13
公開日2006-05-16
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.54 Å)
主引用文献Structure-Based Drug Design of a Novel Family of PPARgamma Partial Agonists: Virtual Screening, X-ray Crystallography, and in Vitro/in Vivo Biological Activities
J.Med.Chem., 49, 2006
4EMA
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Human peroxisome proliferator-activated receptor gamma in complex with rosiglitazone
分子名称: 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), Peroxisome proliferator-activated receptor gamma
著者Liberato, M.V, Nascimento, A.S, Polikarpov, I.
登録日2012-04-11
公開日2013-03-06
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.545 Å)
主引用文献Medium chain fatty acids are selective peroxisome proliferator activated receptor (PPAR) Gamma activators and pan-PPAR partial agonists
Plos One, 7, 2012
6JQ7
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The ligand-free structure of human PPARgamma LBD in the presence of the SRC-1 coactivator peptide
分子名称: 16-mer peptide from Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Jang, J.Y, Han, B.W.
登録日2019-03-29
公開日2019-10-16
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献Structural basis for the inhibitory effects of a novel reversible covalent ligand on PPAR gamma phosphorylation.
Sci Rep, 9, 2019
5U5L
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X-ray Crystal Structure of the PPARgamma Ligand Binding Domain in Complex with Rivoglitazone
分子名称: (5S)-5-({4-[(6-methoxy-1-methyl-1H-benzimidazol-2-yl)methoxy]phenyl}methyl)-1,3-thiazolidine-2,4-dione, Peroxisome proliferator-activated receptor gamma
著者Bruning, J.B, Rajapaksha, H, Wegener, K, Bhatia, H.
登録日2016-12-06
公開日2017-08-23
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献X-ray crystal structure of rivoglitazone bound to PPAR gamma and PPAR subtype selectivity of TZDs.
Biochim. Biophys. Acta, 1861, 2017
2VV0
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hPPARgamma Ligand binding domain in complex with DHA
分子名称: DOCOSA-4,7,10,13,16,19-HEXAENOIC ACID, PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR GAMMA
著者Itoh, T, Fairall, L, Schwabe, J.W.R.
登録日2008-06-02
公開日2008-08-19
最終更新日2023-12-13
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献Structural Basis for the Activation of Pparg by Oxidised Fatty Acids
Nat.Struct.Mol.Biol., 15, 2008
3OSW
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Crystal structure of PPARgamma ligand binding domain in complex with tetrabromo-bisphenol A (TBBPA)
分子名称: 4,4'-propane-2,2-diylbis(2,6-dibromophenol), Peroxisome proliferator-activated receptor gamma, S-1,2-PROPANEDIOL
著者le Maire, A, Bourguet, W.
登録日2010-09-10
公開日2011-05-25
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献Peroxisome proliferator-activated receptor Gamma is a target for halogenated analogs of bisphenol A.
Environ.Health Perspect., 119, 2011
3S9S
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Ligand binding domain of PPARgamma complexed with a benzimidazole partial agonist
分子名称: 1-(3,4-dichlorobenzyl)-2-methyl-N-[(1R)-1-phenylpropyl]-1H-benzimidazole-5-carboxamide, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Lambert, M.H, Xu, R.X.
登録日2011-06-02
公開日2012-06-06
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARgamma partial agonist.
Bioorg.Med.Chem.Lett., 21, 2011
3K8S
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Crystal Structure of PPARg in complex with T2384
分子名称: 2-chloro-N-{3-chloro-4-[(5-chloro-1,3-benzothiazol-2-yl)sulfanyl]phenyl}-4-(trifluoromethyl)benzenesulfonamide, Peroxisome proliferator-activated receptor gamma
著者Wang, Z.
登録日2009-10-14
公開日2009-11-03
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.55 Å)
主引用文献T2384, a novel antidiabetic agent with unique peroxisome proliferator-activated receptor gamma binding properties
J.Biol.Chem., 283, 2008
2ZK4
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Human peroxisome proliferator-activated receptor gamma ligand binding domain complexed with 15-oxo-eicosatetraenoic acid
分子名称: (5E,8E,11Z,13E)-15-oxoicosa-5,8,11,13-tetraenoic acid, Peroxisome proliferator-activated receptor gamma
著者Waku, T, Shiraki, T, Oyama, T, Fujimoto, Y, Morikawa, K.
登録日2008-03-12
公開日2009-02-24
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.57 Å)
主引用文献Structural insight into PPARgamma activation through covalent modification with endogenous fatty acids
J.Mol.Biol., 385, 2009
2ZK3
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Human peroxisome proliferator-activated receptor gamma ligand binding domain complexed with 8-oxo-eicosatetraenoic acid
分子名称: (5E,11E,14E)-8-oxoicosa-5,9,11,14-tetraenoic acid, Peroxisome proliferator-activated receptor gamma
著者Waku, T, Shiraki, T, Oyama, T, Fujimoto, Y, Morikawa, K.
登録日2008-03-12
公開日2009-02-24
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.58 Å)
主引用文献Structural insight into PPARgamma activation through covalent modification with endogenous fatty acids
J.Mol.Biol., 385, 2009
6DBH
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Crystal structure of PPAR gamma in complex with NMP422
分子名称: 4-{2-[(2,3-dioxo-1-pentyl-2,3-dihydro-1H-indol-5-yl)sulfanyl]ethyl}benzoic acid, CHLORIDE ION, Peroxisome proliferator-activated receptor gamma
著者Mou, T.C, Chrisman, I.M, Hughes, T.S, Sprang, S.R.
登録日2018-05-03
公開日2019-05-08
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.597 Å)
主引用文献Crystal structure of PPAR gamma in complex with NMP422
To Be Published
7SQB
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PPAR gamma LBD bound to Inverse Agonist SR10221
分子名称: (2S)-2-{5-[(5-{[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-2-chlorophenoxy}propanoic acid, Peroxisome proliferator-activated receptor gamma
著者Frkic, R.L, Pederick, J.L, Bruning, J.B.
登録日2021-11-05
公開日2023-05-10
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献PPAR gamma Corepression Involves Alternate Ligand Conformation and Inflation of H12 Ensembles.
Acs Chem.Biol., 18, 2023
8DK4
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Peroxisome proliferator-activated receptor gamma in complex with VSP-51-2
分子名称: 5-(benzylcarbamoyl)-1-[(4-chloro-3-fluorophenyl)methyl]-1H-indole-2-carboxylic acid, Peroxisome proliferator-activated receptor gamma, Peroxisome proliferator-activated receptor gamma coactivator 1-alpha
著者Ma, L, Zhou, X.E, Suino-Powell, K, Hou, N, Zhou, Z, Luo, J, Xu, H.E, Yi, W.
登録日2022-07-02
公開日2023-07-05
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献Identification of VSP-51-2 as the Novel and Safe PPAR gamma Modulator: Structure-Based Design, Biological Validation and Crystal Analysis
To Be Published

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