8DKV
 
 | | PPARg bound to JTP-426467 and Co-R peptide | | Descriptor: | 2-chloro-N-[4-(5-methyl-1,3-benzoxazol-2-yl)phenyl]-5-nitrobenzamide, 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, Nuclear receptor corepressor 1, ... | | Authors: | Larsen, N.A. | | Deposit date: | 2022-07-06 | | Release date: | 2022-09-07 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.59 Å) | | Cite: | Biochemical and structural basis for the pharmacological inhibition of nuclear hormone receptor PPAR gamma by inverse agonists.
J.Biol.Chem., 298, 2022
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6ONI
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6PDZ
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8DKN
 | | PPARg bound to T0070907 and Co-R peptide | | Descriptor: | 2-chloro-5-nitro-N-(pyridin-4-yl)benzamide, 3-CYCLOHEXYL-1-PROPYLSULFONIC ACID, Nuclear receptor corepressor 1 peptide, ... | | Authors: | Larsen, N.A, Tsai, J. | | Deposit date: | 2022-07-05 | | Release date: | 2022-09-07 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Biochemical and structural basis for the pharmacological inhibition of nuclear hormone receptor PPAR gamma by inverse agonists.
J.Biol.Chem., 298, 2022
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4Y29
 | | Identification of a novel PPARg ligand that regulates metabolism | | Descriptor: | 1,2-dimethoxy-12-methyl[1,3]benzodioxolo[5,6-c]phenanthridin-12-ium, Peptide from Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma | | Authors: | Wang, R, Li, Y. | | Deposit date: | 2015-02-09 | | Release date: | 2015-09-09 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (1.98 Å) | | Cite: | Selective targeting of PPAR gamma by the natural product chelerythrine with a unique binding mode and improved antidiabetic potency.
Sci Rep, 5, 2015
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4FGY
 | | Identification of a unique PPAR ligand with an unexpected binding mode and antibetic activity | | Descriptor: | (4R,6S,8S,12R,14R,16Z,18R,19R,20S,21S)-19,21-dihydroxy-22-{(2S,2'R,5S,5'S)-5'-[(1R)-1-hydroxyethyl]-2,5'-dimethyloctahydro-2,2'-bifuran-5-yl}-4,6,8,12,14,18,20-heptamethyl-9,11-dioxodocos-16-enoic acid, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma | | Authors: | Wang, R, Li, Y. | | Deposit date: | 2012-06-05 | | Release date: | 2013-03-20 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.84 Å) | | Cite: | Identification of the antibiotic ionomycin as an unexpected peroxisome proliferator-activated receptor Gamma (PPAR-gamma) ligand with a unique binding mode and effective glucose-lowering activity in a mouse model of diabetes.
Diabetologia, 56, 2013
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4F9M
 | | Crystal structure of the PPARgamma-LBD complexed with a cercosporamide derivative modulator | | Descriptor: | (9aS)-8-acetyl-N-[(2-ethyl-4-fluoronaphthalen-1-yl)methyl]-1,7-dihydroxy-3-methoxy-9a-methyl-9-oxo-9,9a-dihydrodibenzo[b,d]furan-4-carboxamide, Peroxisome proliferator-activated receptor gamma, peptide from Nuclear receptor coactivator 1 | | Authors: | Matsui, Y, Hanzawa, H. | | Deposit date: | 2012-05-19 | | Release date: | 2012-08-08 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Synthesis and biological evaluation of novel (-)-cercosporamide derivatives as potent selective PPARg modulators
Eur.J.Med.Chem., 54, 2012
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5DVC
 | | Human PPARgamma ligand binding dmain complexed with SB1453 in a covalent bonded form | | Descriptor: | N-[2-({3-[({4-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)methyl]benzyl}oxy)phenyl]-3-nitrobenzamide, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma | | Authors: | Jang, J.Y. | | Deposit date: | 2015-09-21 | | Release date: | 2016-09-21 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Human PPARgamma ligand binding dmain complexed with SB1453 in a covalent bonded form
To Be Published
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5DV3
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5DV6
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5DWL
 | | Human PPARgamma ligand binding dmain in complex with SR1664 | | Descriptor: | 4'-[(2,3-dimethyl-5-{[(1S)-1-(4-nitrophenyl)ethyl]carbamoyl}-1H-indol-1-yl)methyl]biphenyl-2-carboxylic acid, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma | | Authors: | Jang, J.Y. | | Deposit date: | 2015-09-22 | | Release date: | 2016-09-21 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Human PPARgamma ligand binding dmain in complex with SR1664
To Be Published
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5DV8
 | | Human PPARgamma ligand binding dmain complexed with SB1451 in a covalent bonded form | | Descriptor: | N-[2-({2-[({4-[(4-methylpiperazin-1-yl)methyl]benzoyl}amino)methyl]benzyl}oxy)phenyl]-3-nitrobenzamide, Nuclear receptor coactivator 1, Peroxisome proliferator-activated receptor gamma | | Authors: | Jang, J.Y. | | Deposit date: | 2015-09-21 | | Release date: | 2016-09-21 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | Human PPARgamma ligand binding dmain complexed with SB1451 in a covalent bonded form
To Be Published
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4HEE
 | | Crystal structure of PPARgamma in complex with compound 13 | | Descriptor: | 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 | | Authors: | Han, S. | | Deposit date: | 2012-10-03 | | Release date: | 2013-08-21 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | 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
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3H0A
 | | 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 | | Descriptor: | 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, ... | | Authors: | Wang, Z, Sudom, A, Walker, N.P. | | Deposit date: | 2009-04-08 | | Release date: | 2009-06-09 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Identification of a PPARdelta agonist with partial agonistic activity on PPARgamma.
Bioorg.Med.Chem.Lett., 19, 2009
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3FUR
 | | Crystal Structure of PPARg in complex with INT131 | | Descriptor: | 2,4-dichloro-N-[3,5-dichloro-4-(quinolin-3-yloxy)phenyl]benzenesulfonamide, CHLORIDE ION, Nuclear receptor coactivator 1, ... | | Authors: | Wang, Z, Liu, J, Walker, N. | | Deposit date: | 2009-01-14 | | Release date: | 2009-06-09 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | INT131: a selective modulator of PPAR gamma.
J.Mol.Biol., 386, 2009
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5YCN
 | | Human PPARgamma ligand binding domain complexed with Lobeglitazone | | Descriptor: | (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 | | Authors: | Jang, J.Y, Han, B.W. | | Deposit date: | 2017-09-07 | | Release date: | 2018-09-12 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.15 Å) | | Cite: | Structural Basis for the Enhanced Anti-Diabetic Efficacy of Lobeglitazone on PPAR gamma.
Sci Rep, 8, 2018
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5YCP
 | | Human PPARgamma ligand binding domain complexed with Rosiglitazone | | Descriptor: | 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), Nuclear receptor coactivator 1, ... | | Authors: | Jang, J.Y, Han, B.W. | | Deposit date: | 2017-09-07 | | Release date: | 2018-09-12 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | Structural Basis for the Enhanced Anti-Diabetic Efficacy of Lobeglitazone on PPAR gamma.
Sci Rep, 8, 2018
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3G9E
 | | Aleglitaar. a new. potent, and balanced dual ppara/g agonist for the treatment of type II diabetes | | Descriptor: | (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 | | Authors: | 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. | | Deposit date: | 2009-02-13 | | Release date: | 2009-06-02 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
Bioorg.Med.Chem.Lett., 19, 2009
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3FEJ
 | | Design and biological evaluation of novel, balanced dual PPARa/g agonists | | Descriptor: | (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 | | Authors: | Benz, J, Grether, U, Gsell, B, Binggeli, A, Hilpert, H, Kuhn, B, Maerki, H.P, Mohr, P, Ruf, A, Stihle, M. | | Deposit date: | 2008-11-30 | | Release date: | 2009-10-20 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.01 Å) | | Cite: | Design and biological evaluation of novel, balanced dual PPARalpha/gamma agonists
Chemmedchem, 4, 2009
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8FHE
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8FHG
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8FKE
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8FKD
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8FKF
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8FKC
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