5VND
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![BU of 5vnd by Molmil](/molmil-images/mine/5vnd) | Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to H3B-6527 | 分子名称: | 1,2-ETHANEDIOL, Fibroblast growth factor receptor 1, N-{2-[(6-{[(2,6-dichloro-3,5-dimethoxyphenyl)carbamoyl](methyl)amino}pyrimidin-4-yl)amino]-5-(4-ethylpiperazin-1-yl)phenyl}propanamide, ... | 著者 | Tsai, J.H.C, Reynolds, D, Fekkes, P, Smith, P, Larsen, N.A. | 登録日 | 2017-04-30 | 公開日 | 2017-05-24 | 最終更新日 | 2023-10-04 | 実験手法 | X-RAY DIFFRACTION (2.2 Å) | 主引用文献 | H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma. Cancer Res., 77, 2017
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5SYB
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![BU of 5syb by Molmil](/molmil-images/mine/5syb) | Crystal structure of human PHF5A | 分子名称: | 1,2-ETHANEDIOL, PHD finger-like domain-containing protein 5A, ZINC ION | 著者 | Tsai, J.H.C, Teng, T, Zhu, P, Fekkes, P, Larsen, N.A. | 登録日 | 2016-08-10 | 公開日 | 2016-09-07 | 最終更新日 | 2024-03-06 | 実験手法 | X-RAY DIFFRACTION (1.82 Å) | 主引用文献 | Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex. Nat Commun, 8, 2017
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5JI0
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![BU of 5ji0 by Molmil](/molmil-images/mine/5ji0) | PPARgamma-RXRalpha(S427F) heterodimer in complex with SRC-1, rosiglitazone, and 9-cis-retanoic acid | 分子名称: | (9cis)-retinoic acid, 2,4-THIAZOLIDIINEDIONE, 5-[[4-[2-(METHYL-2-PYRIDINYLAMINO)ETHOXY]PHENYL]METHYL]-(9CL), ... | 著者 | Bloudoff, K, Larsen, N.A. | 登録日 | 2016-04-21 | 公開日 | 2017-04-26 | 実験手法 | X-RAY DIFFRACTION (1.98 Å) | 主引用文献 | PPARgamma-RXRalpha(S427F) heterodimer in complex with SRC-1, rosiglitazone, and 9-cis-retanoic acid To Be Published
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4PH4
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![BU of 4ph4 by Molmil](/molmil-images/mine/4ph4) | The crystal structure of Human VPS34 in complex with PIK-III | 分子名称: | 4'-(cyclopropylmethyl)-N~2~-(pyridin-4-yl)-4,5'-bipyrimidine-2,2'-diamine, GLYCEROL, Phosphatidylinositol 3-kinase catalytic subunit type 3 | 著者 | Knapp, M.S, Elling, R.A. | 登録日 | 2014-05-04 | 公開日 | 2014-10-29 | 最終更新日 | 2023-12-27 | 実験手法 | X-RAY DIFFRACTION (2.8 Å) | 主引用文献 | Selective VPS34 inhibitor blocks autophagy and uncovers a role for NCOA4 in ferritin degradation and iron homeostasis in vivo. Nat.Cell Biol., 16, 2014
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5EHR
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![BU of 5ehr by Molmil](/molmil-images/mine/5ehr) | |
7JVN
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![BU of 7jvn by Molmil](/molmil-images/mine/7jvn) | |
7JVM
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![BU of 7jvm by Molmil](/molmil-images/mine/7jvm) | |
5EHP
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![BU of 5ehp by Molmil](/molmil-images/mine/5ehp) | Non-receptor Protein Tyrosine Phosphatase SHP2 in Complex with Allosteric Inhibitor SHP836 | 分子名称: | 5-[2,3-bis(chloranyl)phenyl]-2-[(3~{R},5~{S})-3,5-dimethylpiperazin-1-yl]pyrimidin-4-amine, PHOSPHATE ION, Tyrosine-protein phosphatase non-receptor type 11 | 著者 | Stams, T, Fodor, M. | 登録日 | 2015-10-28 | 公開日 | 2016-07-06 | 最終更新日 | 2023-09-27 | 実験手法 | X-RAY DIFFRACTION (1.85 Å) | 主引用文献 | Allosteric Inhibition of SHP2: Identification of a Potent, Selective, and Orally Efficacious Phosphatase Inhibitor. J.Med.Chem., 59, 2016
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6CHZ
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![BU of 6chz by Molmil](/molmil-images/mine/6chz) | Estrogen Receptor Alpha Y537S bound to antagonist H3B-9224. | 分子名称: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, Estrogen receptor | 著者 | Larsen, N.A. | 登録日 | 2018-02-23 | 公開日 | 2018-03-21 | 最終更新日 | 2024-03-13 | 実験手法 | X-RAY DIFFRACTION (1.68 Å) | 主引用文献 | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer. Cancer Discov, 8, 2018
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6CHW
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![BU of 6chw by Molmil](/molmil-images/mine/6chw) | Estrogen Receptor Alpha Y537S covalently bound to antagonist H3B-5942. | 分子名称: | 1,2-ETHANEDIOL, 4-[(2-{4-[(1E)-1-(1H-indazol-5-yl)-2-phenylbut-1-en-1-yl]phenoxy}ethyl)amino]-N,N-dimethylbutanamide, DIMETHYL SULFOXIDE, ... | 著者 | Larsen, N.A. | 登録日 | 2018-02-23 | 公開日 | 2018-03-21 | 最終更新日 | 2020-02-26 | 実験手法 | X-RAY DIFFRACTION (1.89 Å) | 主引用文献 | Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ER alphaWTand ER alphaMUTBreast Cancer. Cancer Discov, 8, 2018
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6EN4
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![BU of 6en4 by Molmil](/molmil-images/mine/6en4) | SF3b core in complex with a splicing modulator | 分子名称: | PHD finger-like domain-containing protein 5A, Splicing factor 3B subunit 1, Splicing factor 3B subunit 3, ... | 著者 | Cretu, C, Pena, V. | 登録日 | 2017-10-04 | 公開日 | 2018-06-20 | 最終更新日 | 2024-01-17 | 実験手法 | X-RAY DIFFRACTION (3.08 Å) | 主引用文献 | Structural Basis of Splicing Modulation by Antitumor Macrolide Compounds. Mol. Cell, 70, 2018
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8DKN
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![BU of 8dkn by Molmil](/molmil-images/mine/8dkn) | 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
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8DKV
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![BU of 8dkv by Molmil](/molmil-images/mine/8dkv) | 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
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8DSZ
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![BU of 8dsz by Molmil](/molmil-images/mine/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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8DSY
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![BU of 8dsy by Molmil](/molmil-images/mine/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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5ZYA
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![BU of 5zya by Molmil](/molmil-images/mine/5zya) | SF3b spliceosomal complex bound to E7107 | 分子名称: | PHD finger-like domain-containing protein 5A, POTASSIUM ION, Splicing factor 3B subunit 1, ... | 著者 | Finci, L.I, Larsen, N.A. | 登録日 | 2018-05-23 | 公開日 | 2018-06-20 | 最終更新日 | 2024-03-27 | 実験手法 | ELECTRON MICROSCOPY (3.95 Å) | 主引用文献 | The cryo-EM structure of the SF3b spliceosome complex bound to a splicing modulator reveals a pre-mRNA substrate competitive mechanism of action Genes Dev., 32, 2018
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