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PDB: 316 件

1PRG
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LIGAND BINDING DOMAIN OF THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA
分子名称: PROTEIN (PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA)
著者Nolte, R.T, Wisely, G.B, Milburn, M.V.
登録日1998-07-02
公開日2001-01-13
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.2 Å)
主引用文献Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma.
Nature, 395, 1998
1I7I
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CRYSTAL STRUCTURE OF THE LIGAND BINDING DOMAIN OF HUMAN PPAR-GAMMA IN COMPLEX WITH THE AGONIST AZ 242
分子名称: (2S)-2-ETHOXY-3-[4-(2-{4-[(METHYLSULFONYL)OXY]PHENYL}ETHOXY)PHENYL]PROPANOIC ACID, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA
著者Petersen, J.F.W, Cronet, P, Folmer, R, Blomberg, N, Sjoblom, K, Karlsson, U, Lindstedt, E.-L, Bamberg, K.
登録日2001-03-09
公開日2002-03-09
最終更新日2023-08-09
実験手法X-RAY DIFFRACTION (2.35 Å)
主引用文献Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family.
Structure, 9, 2001
4JAZ
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Crystal structure of the complex between PPARgamma LBD and trans-resveratrol
分子名称: Peroxisome proliferator-activated receptor gamma, RESVERATROL
著者Pochetti, G, Capelli, D, Montanari, R, Calleri, E, Moaddel, R, Temporini, C.
登録日2013-02-19
公開日2014-02-12
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.85 Å)
主引用文献Resveratrol and Its Metabolites Bind to PPARs.
Chembiochem, 15, 2014
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
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
6TSG
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Crystal structure of Peroxisome proliferator-activated receptor gamma (PPARG) in complex with TETRAC
分子名称: 3,3',5,5'-TETRAIODOTHYROACETIC ACID, Peroxisome proliferator-activated receptor gamma
著者Chaikuad, A, Gellrich, L, Arrowsmith, C.H, Edwards, A.M, Bountra, C, Merk, D, Knapp, S, Structural Genomics Consortium (SGC)
登録日2019-12-20
公開日2020-07-22
最終更新日2024-01-24
実験手法X-RAY DIFFRACTION (2.98 Å)
主引用文献l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPAR gamma.
J.Med.Chem., 63, 2020
6T1V
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Structure of PPARg H494Y mutant in complex with GW1929
分子名称: (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
著者Rochel, N.
登録日2019-10-06
公開日2021-04-14
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.21 Å)
主引用文献Structure of a PPARg mutant complex
To Be Published
6T1S
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PPAR mutant
分子名称: (2~{S})-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]-2-[[2-(phenylcarbonyl)phenyl]amino]propanoic acid, Peroxisome proliferator-activated receptor gamma, SULFATE ION
著者Rochel, N.
登録日2019-10-05
公開日2021-04-14
最終更新日2024-01-24
実験手法X-RAY DIFFRACTION (1.65 Å)
主引用文献Structure of PPARg mutant
To Be Published
4L98
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Crystal structure of the complex of F360L PPARgamma mutant with the ligand LT175
分子名称: (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Consalvi, V, Chiaraluce, R, Pasquo, A, Capelli, D, Loiodice, F, Laghezza, A, Lori, C.
登録日2013-06-18
公開日2014-06-25
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.28 Å)
主引用文献Structural basis of the transactivation deficiency of the human PPAR gamma F360L mutant associated with familial partial lipodystrophy.
Acta Crystallogr.,Sect.D, 70, 2014
5TWO
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Peroxisome proliferator-activated receptor gamma ligand binding domain in complex with a novel selectively PPAR gamma-modulating ligand VSP-51
分子名称: N-benzyl-1-[(4-chloro-3-fluorophenyl)methyl]-1H-indole-5-carboxamide, PRO-SER-LEU-LEU-LYS-LYS-LEU-LEU-LEU-ALA-PRO, Peroxisome proliferator-activated receptor gamma
著者Yi, W, Shi, J, Zhao, G, Zhou, X.E, Suino-Powell, K, Melcher, K, Xu, H.E.
登録日2016-11-14
公開日2017-02-08
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (1.927 Å)
主引用文献Identification of a novel selective PPAR gamma ligand with a unique binding mode and improved therapeutic profile in vitro.
Sci Rep, 7, 2017
5TTO
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X-ray crystal structure of PPARgamma in complex with SR1643
分子名称: 4-bromo-N-{3,5-dichloro-4-[(quinolin-3-yl)oxy]phenyl}-2,5-difluorobenzene-1-sulfonamide, Peroxisome proliferator-activated receptor gamma
著者Bruning, J.B, Frkic, R.L, Griffin, P, Kamenecka, T, Abell, A.
登録日2016-11-04
公開日2017-05-24
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.246 Å)
主引用文献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
6ZLY
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Crystal structure of the complex between PPARgamma LBD and the ligand NV1362 (7a)
分子名称: (2~{S})-2-[(4-hexoxyphenyl)carbonylamino]-3-methyl-butanoic acid, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Capelli, D.
登録日2020-07-01
公開日2020-11-25
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.79 Å)
主引用文献A Novel N-Substituted Valine Derivative with Unique Peroxisome Proliferator-Activated Receptor gamma Binding Properties and Biological Activities.
J.Med.Chem., 63, 2020
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
7WOX
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PPARgamma antagonist (MMT-160)- PPARgamma LBD complex
分子名称: N-[[5-(3-phenylprop-2-ynoylamino)-2-propoxy-phenyl]methyl]-4-pyrimidin-2-yl-benzamide, Peroxisome proliferator-activated receptor gamma
著者Yoshizawa, M, Aoyama, T, Itoh, T, Miyachi, H.
登録日2022-01-22
公開日2022-04-13
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (3.2 Å)
主引用文献Arylalkynyl amide-type peroxisome proliferator-activated receptor gamma (PPAR gamma )-selective antagonists covalently bind to the PPAR gamma ligand binding domain with a unique binding mode.
Bioorg.Med.Chem.Lett., 64, 2022
5UGM
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Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with Edaglitazone
分子名称: (5R)-5-({4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}methyl)-1,3-thiazolidine-2,4-dione, Peroxisome proliferator-activated receptor gamma, nonanoic acid
著者Shang, J, Kojetin, D.J.
登録日2017-01-09
公開日2018-01-17
最終更新日2024-03-06
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPAR gamma.
Elife, 7, 2018
4L96
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Structure of the complex between the F360L PPARgamma mutant and the ligand LT175 (space group I222)
分子名称: (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Capelli, D, Chiaraluce, R, Consalvi, V, Pasquo, A, Lori, C, Laghezza, A, Loiodice, F.
登録日2013-06-18
公開日2014-06-25
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.38 Å)
主引用文献Structural basis of the transactivation deficiency of the human PPAR gamma F360L mutant associated with familial partial lipodystrophy.
Acta Crystallogr.,Sect.D, 70, 2014
7A7H
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Crystal structure of PPARgamma in complex with compound TK90
分子名称: (2~{R})-2-[[4-[[4-methoxy-2-(trifluoromethyl)phenyl]methylcarbamoyl]phenyl]methyl]butanoic acid, 1,2-ETHANEDIOL, Peroxisome proliferator-activated receptor gamma
著者Ni, X, Kirchner, T, Proschak, E, Chaikuad, A, Knapp, S, Structural Genomics Consortium (SGC)
登録日2020-08-28
公開日2021-08-04
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (2.4 Å)
主引用文献Combined Cardioprotective and Adipocyte Browning Effects Promoted by the Eutomer of Dual sEH/PPAR gamma Modulator.
J.Med.Chem., 64, 2021
2F4B
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Crystal structure of the ligand binding domain of human PPAR-gamma in complex with an agonist
分子名称: (5-{3-[(6-BENZOYL-1-PROPYL-2-NAPHTHYL)OXY]PROPOXY}-1H-INDOL-1-YL)ACETIC ACID, Peroxisome proliferator-activated receptor gamma
著者Lu, I.L, Peng, Y.H, Mahindroo, N, Hsieh, H.P, Wu, S.Y.
登録日2005-11-23
公開日2006-02-14
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.07 Å)
主引用文献Indol-1-yl Acetic Acids as Peroxisome Proliferator-Activated Receptor Agonists: Design, Synthesis, Structural Biology, and Molecular Docking Studies
J.Med.Chem., 49, 2006
7AHJ
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Crystal structure of PPARgamma V290M mutant ligand binding domain in complex with farglitazar
分子名称: 2-(2-BENZOYL-PHENYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, Peroxisome proliferator-activated receptor gamma
著者Schoenmakers, E, Schwabe, B.T.W, Fairall, L, Chatterjee, K, Schwabe, J.W.R.
登録日2020-09-24
公開日2020-10-14
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Crystal structure of PPARgamma V290M mutant ligand binding domain in complex with farglitazar
To Be Published
7AWC
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Crystal structure of Peroxisome proliferator-activated receptor gamma (PPARG)in complex with rosiglitazone
分子名称: 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), GLYCEROL, ...
著者Chaikuad, A, Merk, D, Knapp, S, Structural Genomics Consortium (SGC)
登録日2020-11-06
公開日2020-11-25
最終更新日2024-01-31
実験手法X-RAY DIFFRACTION (1.74 Å)
主引用文献Endogenous vitamin E metabolites mediate allosteric PPAR gamma activation with unprecedented co-regulatory interactions.
Cell Chem Biol, 28, 2021
5AZV
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Crystal structure of hPPARgamma ligand binding domain complexed with 17-oxoDHA
分子名称: (4~{Z},7~{Z},10~{Z},13~{Z},19~{Z})-17-oxidanylidenedocosa-4,7,10,13,19-pentaenoic acid, Peroxisome proliferator-activated receptor gamma
著者Egawa, D, Itoh, T, Yamamoto, K.
登録日2015-10-23
公開日2016-07-06
最終更新日2020-02-26
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献17-OxoDHA Is a PPAR alpha/gamma Dual Covalent Modifier and Agonist
Acs Chem.Biol., 2016
6T9C
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Crystal structure of the complex between PPARgamma LBD and the ligand NV1346 (3a)
分子名称: 4-hexoxy-~{N}-[(2~{S})-3-methyl-1-(oxidanylamino)-1-oxidanylidene-butan-2-yl]benzamide, Peroxisome proliferator-activated receptor gamma
著者Pochetti, G, Montanari, R, Capelli, D.
登録日2019-10-27
公開日2020-02-26
最終更新日2024-01-24
実験手法X-RAY DIFFRACTION (1.95 Å)
主引用文献Insights into PPAR gamma Phosphorylation and Its Inhibition Mechanism.
J.Med.Chem., 63, 2020
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
5DSH
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Human PPARgamma ligand binding dmain complexed with SB1406 in a covalent bonded form
分子名称: N-[3-(benzyloxy)phenyl]-3-nitrobenzamide, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Jang, J.Y.
登録日2015-09-17
公開日2016-09-21
実験手法X-RAY DIFFRACTION (2.95 Å)
主引用文献Human PPARgamma ligand binding dmain complexed with SB1406 in a covalent bonded form
To Be Published
4O8F
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Crystal Structure of the complex between PPARgamma mutant R357A and 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Pochetti, G, Montanari, R, Capelli, D, Chiaraluce, R, Consalvi, V, Lori, C, Loiodice, F, Laghezza, A, Pasquo, A, Cervoni, L, Aschi, M.
登録日2013-12-27
公開日2014-07-23
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.6 Å)
主引用文献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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