8CPJ
 
 | | Crystal structure of PPAR gamma (PPARG) in an inactive form | | 分子名称: | 1,2-ETHANEDIOL, Peroxisome proliferator-activated receptor gamma | | 著者 | Chaikuad, A, Merk, D, Knapp, S, Structural Genomics Consortium (SGC) | | 登録日 | 2023-03-02 | | 公開日 | 2023-07-12 | | 最終更新日 | 2024-06-19 | | 実験手法 | X-RAY DIFFRACTION (2.4 Å) | | 主引用文献 | Targeting the Alternative Vitamin E Metabolite Binding Site Enables Noncanonical PPAR gamma Modulation.
J.Am.Chem.Soc., 145, 2023
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6AN1
 | | Crystal structure of the complex between PPARgamma LBD and the ligand AM-879 | | 分子名称: | 4-({2-[(1,3-dioxo-1,3-dihydro-2H-inden-2-ylidene)methyl]phenoxy}methyl)benzoic acid, Peroxisome proliferator-activated receptor gamma | | 著者 | Veras, H, Figueira, A.C, le Maire, A. | | 登録日 | 2017-08-11 | | 公開日 | 2018-02-14 | | 最終更新日 | 2024-03-13 | | 実験手法 | X-RAY DIFFRACTION (2.687 Å) | | 主引用文献 | Screening for PPAR Non-Agonist Ligands Followed by Characterization of a Hit, AM-879, with Additional No-Adipogenic and cdk5-Mediated Phosphorylation Inhibition Properties.
Front Endocrinol (Lausanne), 9, 2018
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6AVI
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6AUG
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8DSY
 | | PPARg bound to inverse agonist H3B-343 | | 分子名称: | Peroxisome proliferator-activated receptor gamma, {5-[(5-{[(4-tert-butylphenyl)methyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]-2-chlorophenoxy}acetic acid | | 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 (2.95 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
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8FHF
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8DK4
 | | 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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6C5Q
 | | PPARg LBD bound to SR10171 | | 分子名称: | 2-{3-[(5-{[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]phenoxy}-2-methylpropanoic acid, Peroxisome proliferator-activated receptor gamma | | 著者 | Bruning, J.B, Frkic, R.L. | | 登録日 | 2018-01-16 | | 公開日 | 2018-08-01 | | 最終更新日 | 2023-11-15 | | 実験手法 | X-RAY DIFFRACTION (2.404 Å) | | 主引用文献 | PPAR gamma in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix.
iScience, 5, 2018
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6C5T
 | | PPARg LBD bound to SR11023 | | 分子名称: | 2-{4-[(5-{[(1R)-1-(3-cyclopropylphenyl)ethyl]carbamoyl}-2,3-dimethyl-1H-indol-1-yl)methyl]phenyl}-2-methylpropanoic acid, Peroxisome proliferator-activated receptor gamma | | 著者 | Bruning, J.B, Frkic, R.L, Griffin, P.R. | | 登録日 | 2018-01-16 | | 公開日 | 2018-08-01 | | 最終更新日 | 2024-10-16 | | 実験手法 | X-RAY DIFFRACTION (2.75 Å) | | 主引用文献 | PPAR gamma in Complex with an Antagonist and Inverse Agonist: a Tumble and Trap Mechanism of the Activation Helix.
iScience, 5, 2018
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8DSZ
 | | 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
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6D3E
 | | PPARg LBD in Complex with SR1988 | | 分子名称: | 1-[(2,4-difluorophenyl)methyl]-2,3-dimethyl-N-[(1R)-1-phenylpropyl]-1H-indole-5-carboxamide, Peroxisome proliferator-activated receptor gamma | | 著者 | Frkic, R.L, Bruning, J.B. | | 登録日 | 2018-04-15 | | 公開日 | 2019-02-27 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.395 Å) | | 主引用文献 | Structural and Dynamic Elucidation of a Non-acid PPARgammaPartial Agonist: SR1988.
Nucl Receptor Res, 5, 2018
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6C1I
 | | Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with T0070907 | | 分子名称: | 2-chloro-5-nitro-N-(pyridin-4-yl)benzamide, Peroxisome proliferator-activated receptor gamma, nonanoic acid | | 著者 | Shang, J, Fuhrmann, J, Brust, R, Kojetin, D.J. | | 登録日 | 2018-01-04 | | 公開日 | 2018-12-12 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (2.26 Å) | | 主引用文献 | A structural mechanism for directing corepressor-selective inverse agonism of PPAR gamma.
Nat Commun, 9, 2018
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6D8X
 | | PPAR gamma LBD complexed with the 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, CITRATE ANION, GLYCEROL, ... | | 著者 | Mou, T.C, Chrisman, I.M, Hughes, T.S, Sprang, S.R. | | 登録日 | 2018-04-27 | | 公開日 | 2019-05-01 | | 最終更新日 | 2023-10-04 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | PPAR gamma LBD complexed with the agonist GW1929
To Be Published
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2VV1
 | | hPPARgamma Ligand binding domain in complex with 4-HDHA | | 分子名称: | (4S,5E,7Z,10Z,13Z,16Z,19Z)-4-hydroxydocosa-5,7,10,13,16,19-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 (2.2 Å) | | 主引用文献 | Structural Basis for the Activation of Pparg by Oxidised Fatty Acids
Nat.Struct.Mol.Biol., 15, 2008
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5Y2T
 | | Structure of PPARgamma ligand binding domain - lobeglitazone complex | | 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, Peroxisome proliferator-activated receptor gamma | | 著者 | Im, Y.J, Lee, M. | | 登録日 | 2017-07-27 | | 公開日 | 2017-12-20 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.7 Å) | | 主引用文献 | Structures of PPAR gamma complexed with lobeglitazone and pioglitazone reveal key determinants for the recognition of antidiabetic drugs
Sci Rep, 7, 2017
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6L89
 | | Human PPARgamma ligand binding domain complexed with Butyrolactone 1 | | 分子名称: | Peroxisome proliferator-activated receptor gamma, methyl (2R)-3-(4-hydroxyphenyl)-2-[[3-(3-methylbut-2-enyl)-4-oxidanyl-phenyl]methyl]-4-oxidanyl-5-oxidanylidene-furan-2-carboxylate | | 著者 | Jang, D.M, Han, B.W. | | 登録日 | 2019-11-05 | | 公開日 | 2020-09-16 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.1 Å) | | 主引用文献 | Cyclin-Dependent Kinase 5 Inhibitor Butyrolactone I Elicits a Partial Agonist Activity of Peroxisome Proliferator-Activated Receptor gamma.
Biomolecules, 10, 2020
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3R8A
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6L8B
 | | The ligand-free structure of human PPARgamma LBD | | 分子名称: | Peroxisome proliferator-activated receptor gamma | | 著者 | Jang, D.M, Han, B.W. | | 登録日 | 2019-11-05 | | 公開日 | 2020-09-16 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (2.102 Å) | | 主引用文献 | Cyclin-Dependent Kinase 5 Inhibitor Butyrolactone I Elicits a Partial Agonist Activity of Peroxisome Proliferator-Activated Receptor gamma.
Biomolecules, 10, 2020
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5Y2O
 | | Structure of PPARgamma ligand binding domain-pioglitazone complex | | 分子名称: | (5S)-5-[[4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione, Peroxisome proliferator-activated receptor gamma | | 著者 | Im, Y.J, Lee, M. | | 登録日 | 2017-07-26 | | 公開日 | 2017-12-20 | | 最終更新日 | 2023-11-22 | | 実験手法 | X-RAY DIFFRACTION (1.801 Å) | | 主引用文献 | Structures of PPAR gamma complexed with lobeglitazone and pioglitazone reveal key determinants for the recognition of antidiabetic drugs
Sci Rep, 7, 2017
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3R5N
 | | Crystal structure of PPARgammaLBD complexed with the agonist magnolol | | 分子名称: | 5,5'-di(prop-2-en-1-yl)biphenyl-2,2'-diol, Peroxisome proliferator-activated receptor gamma | | 著者 | Zhang, H, Chen, L, Chen, J, Hu, L, Jiang, H, Shen, X. | | 登録日 | 2011-03-18 | | 公開日 | 2012-02-08 | | 最終更新日 | 2023-09-13 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Molecular determinants of magnolol targeting both RXR(alpha) and PPAR(gamma).
Plos One, 6, 2011
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2VV0
 | | 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
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5WQX
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6MD1
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6MCZ
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3SZ1
 | | Human PPAR gamma ligand binding domain in complex with luteolin and myristic acid | | 分子名称: | 2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-4H-chromen-4-one, MYRISTIC ACID, Peroxisome proliferator-activated receptor gamma, ... | | 著者 | Puhl, A.C, Bernardes, A, Polikarpov, I. | | 登録日 | 2011-07-18 | | 公開日 | 2012-03-21 | | 最終更新日 | 2024-02-28 | | 実験手法 | X-RAY DIFFRACTION (2.3 Å) | | 主引用文献 | Mode of peroxisome proliferator-activated receptor gamma activation by luteolin.
Mol.Pharmacol., 81, 2012
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