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PDB: 305 件

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
2ATH
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Crystal structure of the ligand binding domain of human PPAR-gamma im complex with an agonist
分子名称: 2-{5-[3-(7-PROPYL-3-TRIFLUOROMETHYLBENZO[D]ISOXAZOL-6-YLOXY)PROPOXY]INDOL-1-YL}ETHANOIC ACID, Peroxisome proliferator activated receptor gamma
著者Mahindroo, N, Huang, C.-F, Wu, S.-Y, Hsieh, H.-P.
登録日2005-08-25
公開日2006-08-25
最終更新日2024-03-13
実験手法X-RAY DIFFRACTION (2.28 Å)
主引用文献Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities
J.Med.Chem., 48, 2005
8HUM
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X-ray structure of human PPAR gamma ligand binding domain-lanifibranor-SRC1 coactivator peptide co-crystals obtained by co-crystallization
分子名称: 15-meric peptide from Nuclear receptor coactivator 1, 4-[1-(1,3-benzothiazol-6-ylsulfonyl)-5-chloro-indol-2-yl]butanoic acid, Isoform 1 of Peroxisome proliferator-activated receptor gamma
著者Kamata, S, Honda, A, Machida, Y, Uchii, K, Shiiyama, Y, Masuda, R, Oyama, T, Ishii, I.
登録日2022-12-24
公開日2023-08-09
最終更新日2023-09-06
実験手法X-RAY DIFFRACTION (2.29 Å)
主引用文献Functional and Structural Insights into the Human PPAR alpha / delta / gamma Targeting Preferences of Anti-NASH Investigational Drugs, Lanifibranor, Seladelpar, and Elafibranor.
Antioxidants, 12, 2023
6AVI
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Crystal Structure of Human PPARgamma Ligand Binding Domain in Complex with GW9662 and Nonanoic acid
分子名称: 2-chloro-5-nitro-N-phenylbenzamide, Peroxisome proliferator-activated receptor gamma, nonanoic acid
著者Shang, J, Kojetin, D.J.
登録日2017-09-02
公開日2018-09-12
最終更新日2023-10-04
実験手法X-RAY DIFFRACTION (2.29 Å)
主引用文献Cooperative cobinding of synthetic and natural ligands to the nuclear receptor PPAR gamma.
Elife, 7, 2018
5WQX
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Covalent bond formation of synthetic ligand with hPPARg-LBD
分子名称: 2-[E-(E-2-oxidanylidenehexadec-5-enylidene)amino]ethanoic acid, Peroxisome proliferator-activated receptor gamma
著者Kojima, H, Itoh, T, Yamamoto, K.
登録日2016-11-29
公開日2017-11-22
最終更新日2017-12-13
実験手法X-RAY DIFFRACTION (2.29 Å)
主引用文献On-site reaction for PPAR gamma modification using a specific bifunctional ligand
Bioorg. Med. Chem., 25, 2017
7LOT
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Human PPAR Gamma LBD in Complex with Tetrazole Compound N-{3-[(4-methylbenzyl)oxy]benzyl}-2H-tetrazol-5-amine.
分子名称: Peroxisome proliferator-activated receptor gamma, ~{N}-[[3-[(4-methylphenyl)methoxy]phenyl]methyl]-1~{H}-1,2,3,4-tetrazol-5-amine
著者de Paula, K, Nascimento, A.S.
登録日2021-02-10
公開日2021-02-24
最終更新日2023-10-18
実験手法X-RAY DIFFRACTION (2.29 Å)
主引用文献Tetrazoles as PPAR gamma ligands: A structural and computational investigation.
J.Mol.Graph.Model., 106, 2021
6ONJ
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Crystal structure of PPARgamma ligand binding domain in complex with TRAP220 peptide and agonist rosiglitazone
分子名称: 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), Mediator of RNA polymerase II transcription subunit 1, ...
著者Shang, J, Kojetin, D.J.
登録日2019-04-22
公開日2020-03-04
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献A molecular switch regulating transcriptional repression and activation of PPAR gamma.
Nat Commun, 11, 2020
2G0H
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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: N-[1-(4-FLUOROPHENYL)-3-(2-THIENYL)-1H-PYRAZOL-5-YL]-3,5-BIS(TRIFLUOROMETHYL)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 (2.3 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
1K74
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The 2.3 Angstrom resolution crystal structure of the heterodimer of the human PPARgamma and RXRalpha ligand binding domains respectively bound with GW409544 and 9-cis retinoic acid and co-activator peptides.
分子名称: (9cis)-retinoic acid, 2-(1-METHYL-3-OXO-3-PHENYL-PROPYLAMINO)-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-PHENYL}-PROPIONIC ACID, Peroxisome proliferator activated receptor gamma, ...
著者Xu, H.E, Lambert, M.H, Montana, V.G, Moore, L.B, Collins, J.L, Oplinger, J.A, Kliewer, S.A, Gampe Jr, R.T, McKee, D.D, Moore, J.T, Willson, T.M.
登録日2001-10-18
公開日2001-12-05
最終更新日2024-02-07
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Proc.Natl.Acad.Sci.USA, 98, 2001
3CS8
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Structural and Biochemical Basis for the Binding Selectivity of PPARg to PGC-1a
分子名称: 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), PGC-1alfa peptide, ...
著者Li, Y, Martynowski, D.
登録日2008-04-09
公開日2008-06-03
最終更新日2024-02-21
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Structural and biochemical basis for the binding selectivity of peroxisome proliferator-activated receptor gamma to PGC-1alpha.
J.Biol.Chem., 283, 2008
4R2U
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Crystal Structure of PPARgamma in complex with SR1664
分子名称: 4'-[(2,3-dimethyl-5-{[(1S)-1-(4-nitrophenyl)ethyl]carbamoyl}-1H-indol-1-yl)methyl]biphenyl-2-carboxylic acid, Peroxisome proliferator-activated receptor gamma
著者Marciano, D.P, Kamenecka, T, Griffin, P.R, Bruning, J.B.
登録日2014-08-13
公開日2015-07-01
最終更新日2023-09-20
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Pharmacological repression of PPAR gamma promotes osteogenesis.
Nat Commun, 6, 2015
7EFQ
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Crystal structure of hPPARgamma ligand binding domain complexed with rosiglitazone-based fluorescence probe
分子名称: (5S)-5-[[4-[2-[[7-(diethylamino)-2-oxidanylidene-chromen-4-yl]-methyl-amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione, Peroxisome proliferator-activated receptor gamma
著者Yoshikawa, C, Ishida, H, Ohashi, N, Itoh, T.
登録日2021-03-23
公開日2021-05-12
最終更新日2023-11-29
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Synthesis of a Coumarin-Based PPAR gamma Fluorescence Probe for Competitive Binding Assay.
Int J Mol Sci, 22, 2021
8AQM
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Crystal structure of PPARG and NCOR2 with an inverse agonist (compound 6a)
分子名称: 2-chloranyl-~{N}-[2-(3-methylphenyl)-1,3-benzoxazol-5-yl]-5-nitro-benzamide, Nuclear receptor corepressor 2, Peroxisome proliferator-activated receptor gamma
著者Friberg, A, Orsi, D.L, Pook, E, Braeuer, N, Lemke, C.T, Stellfeld, T, Puetter, V, Goldstein, J.
登録日2022-08-12
公開日2022-11-09
最終更新日2024-05-01
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Discovery and Structure-Based Design of Potent Covalent PPAR gamma Inverse-Agonists BAY-4931 and BAY-0069 .
J.Med.Chem., 65, 2022
5DVC
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Human PPARgamma ligand binding dmain complexed with SB1453 in a covalent bonded form
分子名称: 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
著者Jang, J.Y.
登録日2015-09-21
公開日2016-09-21
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Human PPARgamma ligand binding dmain complexed with SB1453 in a covalent bonded form
To Be Published
2POB
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PPARgamma Ligand binding domain complexed with a farglitazar analogue gw4709
分子名称: 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
著者Nolte, R.T.
登録日2007-04-26
公開日2008-03-18
最終更新日2024-04-03
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Cocrystal structure guided array synthesis of PPARgamma inverse agonists
BIOORG.MED.CHEM.LETT., 17, 2007
6VZN
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Crystal structure of human PPARgamma ligand binding domain Y473E mutant
分子名称: Peroxisome proliferator-activated receptor gamma
著者Shang, J, Kojetin, D.J.
登録日2020-02-28
公開日2021-03-03
最終更新日2023-10-11
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Structural mechanism underlying ligand binding and activation of PPAR gamma.
Structure, 29, 2021
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
4OJ4
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Crystal structure of V290M PPARgamma mutant in complex with diclofenac
分子名称: 2-[2,6-DICHLOROPHENYL)AMINO]BENZENEACETIC ACID, CALCIUM ION, Peroxisome proliferator-activated receptor gamma
著者Puhl, A.C, Webb, P, Polikarpov, I.
登録日2014-01-20
公開日2015-02-04
最終更新日2024-02-28
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Crystal structure of a PPAR ligand-resistance syndrome mutant
To be Published
3GBK
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Crystal Structure of Human PPAR-gamma Ligand Binding Domain Complexed with a Potent and Selective Agonist
分子名称: 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
著者Peng, Y.-H, Lin, C.-H, Hsieh, H.-P, Wu, S.-Y.
登録日2009-02-19
公開日2009-12-29
最終更新日2023-11-01
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists
J.Med.Chem., 52, 2009
3FUR
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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
6FZP
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PPAR gamma complex.
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, Beji, S.
登録日2018-03-15
公開日2019-02-13
最終更新日2024-01-17
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Recurrent activating mutations of PPAR gamma associated with luminal bladder tumors.
Nat Commun, 10, 2019
7CXI
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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
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
2Q8S
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X-ray Crystal structure of the nuclear hormone receptor PPAR-gamma in a complex with a PPAR gamma/alpha dual agonist
分子名称: (2S)-3-{4-[3-(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)PROPYL]PHENYL}-2-(1H-PYRROL-1-YL)PROPANOIC ACID, Peroxisome proliferator-activated receptor gamma
著者Ohren, J.F.
登録日2007-06-11
公開日2008-10-14
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Bioorg.Med.Chem., 16, 2008
2Q5P
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Crystal Structure of PPARgamma bound to partial agonist MRL24
分子名称: (2S)-2-(3-{[1-(4-METHOXYBENZOYL)-2-METHYL-5-(TRIFLUOROMETHOXY)-1H-INDOL-3-YL]METHYL}PHENOXY)PROPANOIC ACID, Peroxisome Proliferator-Activated Receptor gamma
著者Bruning, J.B, Nettles, K.W.
登録日2007-06-01
公開日2007-10-23
最終更新日2023-08-30
実験手法X-RAY DIFFRACTION (2.3 Å)
主引用文献Partial Agonists Activate PPARgamma Using a Helix 12 Independent Mechanism
Structure, 15, 2007

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