7E2O
| X-ray Crystal structure of PPARgamma R288H mutant. | Descriptor: | Peroxisome proliferator-activated receptor gamma | Authors: | Egawa, D, Itoh, T. | Deposit date: | 2021-02-06 | Release date: | 2022-01-19 | Last modified: | 2023-11-29 | Method: | X-RAY DIFFRACTION (3.2 Å) | Cite: | Structural Insights into the Loss-of-Function R288H Mutant of Human PPAR gamma. Biol.Pharm.Bull., 44, 2021
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3CS8
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3D6D
| Crystal Structure of the complex between PPARgamma LBD and the LT175(R-enantiomer) | Descriptor: | (2S)-2-(biphenyl-4-yloxy)-3-phenylpropanoic acid, Peroxisome proliferator-activated receptor gamma | Authors: | Pochetti, G, Montanari, R. | Deposit date: | 2008-05-19 | Release date: | 2008-12-30 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Crystal Structure of the Peroxisome Proliferator-Activated Receptor gamma (PPARgamma) Ligand Binding Domain Complexed with a Novel Partial Agonist: A New Region of the Hydrophobic Pocket Could Be Exploited for Drug Design J.Med.Chem., 51, 2008
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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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2OM9
| Ajulemic acid, a synthetic cannabinoid bound to PPAR gamma | Descriptor: | (6AR,10AR)-3-(1,1-DIMETHYLHEPTYL)-1-HYDROXY-6,6-DIMETHYL-6A,7,10,10A-TETRAHYDRO-6H-BENZO[C]CHROMENE-9-CARBOXYLIC ACID, Peroxisome proliferator-activated receptor gamma | Authors: | Ambrosio, A.L.B, Garratt, R.C. | Deposit date: | 2007-01-21 | Release date: | 2007-04-24 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.8 Å) | Cite: | Ajulemic Acid, a Synthetic Nonpsychoactive Cannabinoid Acid, Bound to the Ligand Binding Domain of the Human Peroxisome Proliferator-activated Receptor gamma J.Biol.Chem., 282, 2007
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8HHQ
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2POB
| PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709 | Descriptor: | GLYCEROL, N-[(2S)-2-[(2-BENZOYLPHENYL)AMINO]-3-{4-[2-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)ETHOXY]PHENYL}PROPYL]ACETAMIDE, Peroxisome proliferator-activated receptor gamma | Authors: | Nolte, R.T. | Deposit date: | 2007-04-26 | Release date: | 2008-03-18 | Last modified: | 2024-04-03 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Cocrystal structure guided array synthesis of PPARgamma inverse agonists BIOORG.MED.CHEM.LETT., 17, 2007
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7CXE
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6IZM
| Crystal structure of the PPARgamma-LBD complexed with compound 1l | Descriptor: | 3-[[6-(2,6-dimethylpyridin-3-yl)oxy-1-methyl-benzimidazol-2-yl]methoxy]benzoic acid, Peptide from Peroxisome proliferator-activated receptor gamma coactivator 1-alpha, Peroxisome proliferator-activated receptor gamma | Authors: | Matsui, Y, Hanzawa, H. | Deposit date: | 2018-12-20 | Release date: | 2019-03-27 | Last modified: | 2023-11-22 | Method: | X-RAY DIFFRACTION (1.8 Å) | Cite: | Structure-Activity Relationship Studies of 3- or 4-Pyridine Derivatives of DS-6930. Acs Med.Chem.Lett., 10, 2019
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7CXG
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3GBK
| Crystal Structure of Human PPAR-gamma Ligand Binding Domain Complexed with a Potent and Selective Agonist | Descriptor: | 2-[(1-{3-[4-(biphenyl-4-ylcarbonyl)-2-propylphenoxy]propyl}-1,2,3,4-tetrahydroquinolin-5-yl)oxy]-2-methylpropanoic acid, Peroxisome proliferator-activated receptor gamma | Authors: | Peng, Y.-H, Lin, C.-H, Hsieh, H.-P, Wu, S.-Y. | Deposit date: | 2009-02-19 | Release date: | 2009-12-29 | Last modified: | 2023-11-01 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists J.Med.Chem., 52, 2009
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2Q6S
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2Q5P
| Crystal Structure of PPARgamma bound to partial agonist MRL24 | Descriptor: | (2S)-2-(3-{[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: | 2007-06-01 | Release date: | 2007-10-23 | Last modified: | 2023-08-30 | Method: | X-RAY DIFFRACTION (2.3 Å) | Cite: | Partial Agonists Activate PPARgamma Using a Helix 12 Independent Mechanism Structure, 15, 2007
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2Q8S
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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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2Q6R
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2Q5S
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2Q61
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3VJI
| Human PPAR gamma ligand binding domain in complex with JKPL53 | Descriptor: | (2S)-2-{4-butoxy-3-[({4-[(3S,5S,7S)-tricyclo[3.3.1.1~3,7~]dec-1-yl]benzoyl}amino)methyl]benzyl}butanoic 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 (2.61 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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3VSP
| Human PPAR gamma ligand binding domain in complex with a gamma selective agonist mekt28 | Descriptor: | (2R)-2-benzyl-3-[3-({[4-(piperidin-1-yl)benzoyl]amino}methyl)-4-propoxyphenyl]propanoic acid, Peroxisome proliferator-activated receptor gamma | Authors: | Oyama, T, Waku, T, Ohashi, M, Morikawa, K, Miyachi, H. | Deposit date: | 2012-04-30 | Release date: | 2013-05-01 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2.4 Å) | Cite: | Human PPAR gamma ligand binding domain in complex with a gamma selective agonist mekt28 To be Published
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3VSO
| Human PPAR gamma ligand binding domain in complex with a gamma selective agonist mekt21 | Descriptor: | (2R)-2-benzyl-3-[4-propoxy-3-({[4-(pyrimidin-2-yl)benzoyl]amino}methyl)phenyl]propanoic acid, Peroxisome proliferator-activated receptor gamma | Authors: | Oyama, T, Waku, T, Ohashi, M, Morikawa, K, Miyachi, H. | Deposit date: | 2012-04-30 | Release date: | 2013-05-01 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (2 Å) | Cite: | Design and synthesis of a series of alpha-benzyl phenylpropanoic acid-type peroxisome proliferator-activated receptor (PPAR) gamma partial agonists with improved aqueous solubility Bioorg.Med.Chem., 21, 2013
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6AVI
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6AUG
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3V9V
| Crystal structure of the PPARgamma-LBD complexed with a cercosporamide derivative modulator | Descriptor: | Peptide from Peroxisome proliferator-activated receptor gamma coactivator 1-alpha, Peroxisome proliferator-activated receptor gamma, methyl 3-{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}propanoate | Authors: | Matsui, Y, Hanzawa, H. | Deposit date: | 2011-12-28 | Release date: | 2012-02-01 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.6 Å) | Cite: | Substituents at the naphthalene C3 position of (-)-Cercosporamide derivatives significantly affect the maximal efficacy as PPAR(gamma) partial agonists Bioorg.Med.Chem.Lett., 22, 2011
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3V9T
| Crystal structure of the PPARgamma-LBD complexed with a cercosporamide derivative modulator | Descriptor: | (9aS)-8-acetyl-N-[(3-ethoxynaphthalen-1-yl)methyl]-1,7-dihydroxy-3-methoxy-9a-methyl-9-oxo-9,9a-dihydrodibenzo[b,d]furan-4-carboxamide, Peptide from Peroxisome proliferator-activated receptor gamma coactivator 1-alpha, Peroxisome proliferator-activated receptor gamma | Authors: | Matsui, Y, Hanzawa, H. | Deposit date: | 2011-12-28 | Release date: | 2012-02-01 | Last modified: | 2023-11-08 | Method: | X-RAY DIFFRACTION (1.65 Å) | Cite: | 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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