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PDB: 316 件

8FKE
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Crystal structure of PPARgamma ligand-binding domain in complex with N-CoR peptide and inverse agonist SR32904
分子名称: 1,2-ETHANEDIOL, 2-chloro-N-(2-methylpyridin-4-yl)-5-nitrobenzamide, Nuclear receptor corepressor 1, ...
著者MacTavish, B.S, Kojetin, D.J.
登録日2022-12-21
公開日2024-04-17
実験手法X-RAY DIFFRACTION (2.02 Å)
主引用文献Crystal structure of PPARgamma ligand-binding domain in complex with N-CoR peptide and SR32904
To Be Published
8DKN
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PPARg bound to T0070907 and Co-R peptide
分子名称: 2-chloro-5-nitro-N-(pyridin-4-yl)benzamide, 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, Nuclear receptor corepressor 1 peptide, ...
著者Larsen, N.A, Tsai, J.
登録日2022-07-05
公開日2022-09-07
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (1.95 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
8DKV
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PPARg bound to JTP-426467 and Co-R peptide
分子名称: 2-chloro-N-[4-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-5-nitrobenzamide, 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, Nuclear receptor corepressor 1, ...
著者Larsen, N.A.
登録日2022-07-06
公開日2022-09-07
最終更新日2023-10-25
実験手法X-RAY DIFFRACTION (1.59 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
6KTN
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Human PPARgamma ligand-binding domain R288A mutant in complex with imatinib
分子名称: 16-mer peptide from Nuclear receptor coactivator 1, 4-(4-METHYL-PIPERAZIN-1-YLMETHYL)-N-[4-METHYL-3-(4-PYRIDIN-3-YL-PYRIMIDIN-2-YLAMINO)-PHENYL]-BENZAMIDE, Peroxisome proliferator-activated receptor gamma
著者Jang, J.Y, Han, B.W.
登録日2019-08-28
公開日2020-02-05
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2.752 Å)
主引用文献Structural Basis for the Regulation of PPAR gamma Activity by Imatinib.
Molecules, 24, 2019
6KTM
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BU of 6ktm by Molmil
The ligand-free structure of human PPARgamma ligand-binding domain R288A mutant 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2019-08-28
公開日2020-02-05
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2.7 Å)
主引用文献Structural Basis for the Regulation of PPAR gamma Activity by Imatinib.
Molecules, 24, 2019
5YCN
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Human PPARgamma ligand binding domain complexed with Lobeglitazone
分子名称: (5S)-5-[[4-[2-[[6-(4-methoxyphenoxy)pyrimidin-4-yl]-methyl-amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Jang, J.Y, Han, B.W.
登録日2017-09-07
公開日2018-09-12
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2.15 Å)
主引用文献Structural Basis for the Enhanced Anti-Diabetic Efficacy of Lobeglitazone on PPAR gamma.
Sci Rep, 8, 2018
5YCP
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Human PPARgamma ligand binding domain complexed with Rosiglitazone
分子名称: 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), Nuclear receptor coactivator 1, ...
著者Jang, J.Y, Han, B.W.
登録日2017-09-07
公開日2018-09-12
最終更新日2023-11-22
実験手法X-RAY DIFFRACTION (2 Å)
主引用文献Structural Basis for the Enhanced Anti-Diabetic Efficacy of Lobeglitazone on PPAR gamma.
Sci Rep, 8, 2018
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
3T03
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Crystal structure of PPAR gamma ligand binding domain in complex with a novel partial agonist GQ-16
分子名称: (5Z)-5-(5-bromo-2-methoxybenzylidene)-3-(4-methylbenzyl)-1,3-thiazolidine-2,4-dione, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Rajagopalan, S, Webb, P, Baxter, J.D, Brennan, R.G, Phillips, K.J.
登録日2011-07-19
公開日2012-05-23
最終更新日2023-09-13
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献GQ-16, a novel peroxisome proliferator-activated receptor (PPAR gamma) ligand, promotes insulin sensitization without weight gain.
J.Biol.Chem., 287, 2012
3QT0
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Revealing a steroid receptor ligand as a unique PPARgamma agonist
分子名称: 11-(4-DIMETHYLAMINO-PHENYL)-17-HYDROXY-13-METHYL-17-PROP-1-YNYL-1,2,6,7,8,11,12,13,14,15,16,17-DODEC AHYDRO-CYCLOPENTA[A]PHENANTHREN-3-ONE, Nuclear receptor coactivator 1 peptide, Peroxisome proliferator-activated receptor gamma
著者Rong, H.
登録日2011-02-22
公開日2012-02-29
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.496 Å)
主引用文献Revealing a steroid receptor ligand as a unique PPAR gamma agonist.
Cell Res., 22, 2012
3FEJ
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Design and biological evaluation of novel, balanced dual PPARa/g agonists
分子名称: (2S)-3-(4-{[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methoxy}-2-methylphenyl)-2-ethoxypropanoic acid, Peroxisome proliferator-activated receptor gamma, peptide motif 3 of Nuclear receptor coactivator 1
著者Benz, J, Grether, U, Gsell, B, Binggeli, A, Hilpert, H, Kuhn, B, Maerki, H.P, Mohr, P, Ruf, A, Stihle, M.
登録日2008-11-30
公開日2009-10-20
最終更新日2023-12-27
実験手法X-RAY DIFFRACTION (2.01 Å)
主引用文献Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists
Chemmedchem, 4, 2009
3E00
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BU of 3e00 by Molmil
Intact PPAR gamma - RXR alpha Nuclear Receptor Complex on DNA bound with GW9662, 9-cis Retinoic Acid and NCOA2 Peptide
分子名称: (9cis)-retinoic acid, 2-chloro-5-nitro-N-phenylbenzamide, DNA (5'-D(*DCP*DAP*DAP*DAP*DCP*DTP*DAP*DGP*DGP*DTP*DCP*DAP*DAP*DAP*DGP*DGP*DTP*DCP*DAP*DG)-3'), ...
著者Chandra, V, Huang, P, Hamuro, Y, Raghuram, S, Wang, Y, Burris, T.P, Rastinejad, F.
登録日2008-07-30
公開日2008-10-28
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA.
Nature, 456, 2008
3DZY
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BU of 3dzy by Molmil
Intact PPAR gamma - RXR alpha Nuclear Receptor Complex on DNA bound with Rosiglitazone, 9-cis Retinoic Acid and NCOA2 Peptide
分子名称: (9cis)-retinoic acid, 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), ...
著者Chandra, V, Huang, P, Hamuro, Y, Raghuram, S, Wang, Y, Burris, T.P, Rastinejad, F.
登録日2008-07-30
公開日2008-10-28
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (3.1 Å)
主引用文献Structure of the intact PPAR-gamma-RXR- nuclear receptor complex on DNA.
Nature, 456, 2008
3G9E
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Aleglitaar. a new. potent, and balanced dual ppara/g agonist for the treatment of type II diabetes
分子名称: (2S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}propanoic acid, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Ruf, A, Benz, J, Bernardeau, A, Binggeli, A, Blum, D, Boehringer, M, Grether, U, Hilpert, H, Kuhn, B, Maerki, H.P, Meyer, M, Puenterner, K, Raab, S, Schlatter, D, Gsell, B, Stihle, M, Mohr, P.
登録日2009-02-13
公開日2009-06-02
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
Bioorg.Med.Chem.Lett., 19, 2009
7CXK
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BU of 7cxk by Molmil
The ligand-free structure of human PPARgamma LBD R288H mutant in the presence of the SRC-1 coactivator peptide
分子名称: 16-mer peptide from Nuclear receptor coactivator 1, MALONATE ION, 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 (2.2 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
7CXH
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The ligand-free structure of human PPARgamma LBD Q286E mutant 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, 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 (2.3 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
7CXL
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The ligand-free structure of human PPARgamma LBD S289C mutant in the presence of the SRC-1 coactivator peptide
分子名称: 16-mer peptide from Nuclear receptor coactivator 1, MALONIC ACID, 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 (2.7 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
7CXI
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BU of 7cxi by Molmil
The ligand-free structure of human PPARgamma LBD F287Y mutant in the presence of the SRC-1 coactivator peptide
分子名称: 16-mer peptide from Nuclear receptor coactivator 1, MALONATE ION, 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 (2.3 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
7CXF
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BU of 7cxf by Molmil
The ligand-free structure of human PPARgamma LBD C285Y mutant in the presence of the SRC-1 coactivator peptide
分子名称: 16-mer peptide from Nuclear receptor coactivator 1, MALONIC ACID, 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 (2.35 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
7CXJ
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The ligand-free structure of human PPARgamma LBD R288C mutant 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, 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 (2.65 Å)
主引用文献The ligand-free structure of human PPARgamma LBD
To Be Published
3FUR
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BU of 3fur by Molmil
Crystal Structure of PPARg in complex with INT131
分子名称: 2,4-dichloro-N-[3,5-dichloro-4-(quinolin-3-yloxy)phenyl]benzenesulfonamide, CHLORIDE ION, Nuclear receptor coactivator 1, ...
著者Wang, Z, Liu, J, Walker, N.
登録日2009-01-14
公開日2009-06-09
最終更新日2024-03-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献INT131: a selective modulator of PPAR gamma.
J.Mol.Biol., 386, 2009
2PRG
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LIGAND-BINDING DOMAIN OF THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA
分子名称: 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), NUCLEAR RECEPTOR COACTIVATOR SRC-1, ...
著者Nolte, R.T, Wisely, G.B, Milburn, M.V.
登録日1998-08-14
公開日1999-07-19
最終更新日2024-05-22
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma.
Nature, 395, 1998
3ET3
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Structure of PPARgamma with 3-[5-Methoxy-1-(4-methoxy-benzenesulfonyl)-1H-indol-3-yl]-propionic acid
分子名称: 3-{5-methoxy-1-[(4-methoxyphenyl)sulfonyl]-1H-indol-3-yl}propanoic acid, Peroxisome proliferator-activated receptor gamma, Steroid receptor coactivator 1
著者Zhang, K.Y.J, Wang, W.
登録日2008-10-06
公開日2009-02-17
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (1.95 Å)
主引用文献Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent
Proc.Natl.Acad.Sci.USA, 106, 2009
3H0A
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Crystal Structure of Peroxisome Proliferator-Activated Receptor Gamma (PPARg) and Retinoic Acid Receptor Alpha (RXRa) in Complex with 9-cis Retinoic Acid, Co-activator Peptide, and a Partial Agonist
分子名称: 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl]benzoic acid, Nuclear receptor coactivator 1, Co-activator Peptide, ...
著者Wang, Z, Sudom, A, Walker, N.P.
登録日2009-04-08
公開日2009-06-09
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Bioorg.Med.Chem.Lett., 19, 2009
3V9Y
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Crystal structure of the PPARgamma-LBD complexed with a cercosporamide derivative modulator
分子名称: 4-{4-[({[(9aS)-8-acetyl-1,7-dihydroxy-3-methoxy-9a-methyl-9-oxo-9,9a-dihydrodibenzo[b,d]furan-4-yl]carbonyl}amino)methyl]naphthalen-2-yl}butanoic acid, Peptide from Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma
著者Matsui, Y, Hanzawa, H.
登録日2011-12-28
公開日2012-02-01
最終更新日2023-11-08
実験手法X-RAY DIFFRACTION (2.1 Å)
主引用文献Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPAR(gamma) partial agonists
Bioorg.Med.Chem.Lett., 22, 2012

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