5MJ6
 
 | | Ligand-induced conformational change of Insulin-regulated aminopeptidase: insights on catalytic mechanism and active site plasticity. | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, BROMIDE ION, ... | | 著者 | Mpakali, A, Stratikos, E, Saridakis, E, Giastas, P. | | 登録日 | 2016-11-30 | | 公開日 | 2017-04-05 | | 最終更新日 | 2024-01-17 | | 実験手法 | X-RAY DIFFRACTION (2.53 Å) | | 主引用文献 | Ligand-Induced Conformational Change of Insulin-Regulated Aminopeptidase: Insights on Catalytic Mechanism and Active Site Plasticity.
J. Med. Chem., 60, 2017
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8CGP
 | | Insulin regulated aminopeptidase (IRAP) in complex with an allosteric aryl sulfonamide inhibitor | | 分子名称: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Mpakali, A, Stratikos, E, Giastas, P. | | 登録日 | 2023-02-06 | | 公開日 | 2024-01-31 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.62 Å) | | 主引用文献 | Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase.
J.Mol.Biol., 436, 2024
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7ZYF
 | | Insulin regulated aminopeptidase (IRAP) in complex with a nanomolar alpha hydroxy beta amino acid based inhibitor. | | 分子名称: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Mpakali, A, Stratikos, E, Giastas, P, Papakyriakou, A. | | 登録日 | 2022-05-24 | | 公開日 | 2022-07-20 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | Discovery of Selective Nanomolar Inhibitors for Insulin-Regulated Aminopeptidase Based on alpha-Hydroxy-beta-amino Acid Derivatives of Bestatin.
J.Med.Chem., 65, 2022
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4PJ6
 | | Crystal Structure of Human Insulin Regulated Aminopeptidase with Lysine in Active Site | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, LYSINE, ... | | 著者 | Hermans, S.J, Ascher, D.B, Hancock, N.C, Holien, J.K, Michell, B, Morton, C.J, Parker, M.W. | | 登録日 | 2014-05-12 | | 公開日 | 2014-12-03 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.96 Å) | | 主引用文献 | Crystal structure of human insulin-regulated aminopeptidase with specificity for cyclic peptides.
Protein Sci., 24, 2015
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4P8Q
 | | Crystal Structure of Human Insulin Regulated Aminopeptidase with Alanine in Active Site | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Leucyl-cystinyl aminopeptidase, ... | | 著者 | Hermans, S.J, Ascher, D.B, Hancock, N.C, Holien, J.K, Michell, B, Morton, C.J, Parker, M.W. | | 登録日 | 2014-03-31 | | 公開日 | 2014-12-03 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (3.02 Å) | | 主引用文献 | Crystal structure of human insulin-regulated aminopeptidase with specificity for cyclic peptides.
Protein Sci., 24, 2015
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8CGW
 | | Insulin-regulated aminopeptidase (IRAP) in complex with an allosteric benzopyran-based inhibitor | | 分子名称: | 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Mpakali, A, Stratikos, E, Giastas, P. | | 登録日 | 2023-02-06 | | 公開日 | 2024-01-31 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (3.03 Å) | | 主引用文献 | Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase.
J.Mol.Biol., 436, 2024
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6YDX
 | | Insulin-regulated aminopeptidase complexed with a macrocyclic peptidic inhibitor | | 分子名称: | 1,2-ETHANEDIOL, 2-[2-[[[(4~{R},8~{S},11~{S})-11-azanyl-8-[(4-hydroxyphenyl)methyl]-6,10-bis(oxidanylidene)-1,2-dithia-5,9-diazacyclotridec-4-yl]carbonylamino]methyl]phenyl]ethanoic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Mpakali, A, Saridakis, E, Giastas, P, Stratikos, E. | | 登録日 | 2020-03-21 | | 公開日 | 2020-07-22 | | 最終更新日 | 2024-01-24 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor.
Acs Med.Chem.Lett., 11, 2020
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5JHQ
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4Z7I
 | | Crystal structure of insulin regulated aminopeptidase in complex with ligand | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, DG025 transition-state analogue enzyme inhibitor, ... | | 著者 | Mpakali, A, Saridakis, E, Harlos, K, Zhao, Y, Stratikos, E. | | 登録日 | 2015-04-07 | | 公開日 | 2015-08-26 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.31 Å) | | 主引用文献 | Crystal Structure of Insulin-Regulated Aminopeptidase with Bound Substrate Analogue Provides Insight on Antigenic Epitope Precursor Recognition and Processing.
J Immunol., 195, 2015
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5C97
 | | Insulin regulated aminopeptidase | | 分子名称: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Leucyl-cystinyl aminopeptidase, ... | | 著者 | Mpakali, A, Saridakis, E, Harlos, K, Zhao, Y, Stratikos, E. | | 登録日 | 2015-06-26 | | 公開日 | 2015-08-26 | | 最終更新日 | 2024-01-10 | | 実験手法 | X-RAY DIFFRACTION (3.37 Å) | | 主引用文献 | Crystal Structure of Insulin-Regulated Aminopeptidase with Bound Substrate Analogue Provides Insight on Antigenic Epitope Precursor Recognition and Processing.
J Immunol., 195, 2015
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8P0I
 | | Crystal structure of the open conformation of insulin-regulated aminopeptidase in complex with a small-MW inhibitor | | 分子名称: | 2-[2-(3,5-dimethylpyrazol-1-yl)-6-(4-methoxyphenyl)pyrimidin-4-yl]oxy-N-methyl-N-[(2-methylpyridin-3-yl)methyl]ethanamide, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Mpakali, A, Giastas, P, Stratikos, E. | | 登録日 | 2023-05-10 | | 公開日 | 2024-09-04 | | 実験手法 | X-RAY DIFFRACTION (3.5 Å) | | 主引用文献 | Stabilization of the open conformation omicron f insulin-regulated aminopeptidase by a novel substrate-selective small-molecule inhibitor.
Protein Sci., 33, 2024
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