7Z28
 
 | | High-resolution crystal structure of ERAP1 with bound bestatin analogue inhibitor | | Descriptor: | 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, ... | | Authors: | Giastas, P, Papakyriakou, A, Stratikos, E, Vourloumis, D. | | Deposit date: | 2022-02-26 | | Release date: | 2022-07-27 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | 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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6Q4R
 | | High-resolution crystal structure of ERAP1 with bound phosphinic transition-state analogue inhibitor | | Descriptor: | 1,2-ETHANEDIOL, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Giastas, P, Neu, M, Rowland, P, Stratikos, E. | | Deposit date: | 2018-12-06 | | Release date: | 2019-04-10 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | High-Resolution Crystal Structure of Endoplasmic Reticulum Aminopeptidase 1 with Bound Phosphinic Transition-State Analogue Inhibitor.
Acs Med.Chem.Lett., 10, 2019
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6T6R
 | | Human endoplasmic reticulum aminopeptidase 1 (ERAP1) in complex with (4aR,5S,6R,8S,8aR)-5-(2-(Furan-3-yl)ethyl)-8-hydroxy-5,6,8a-trimethyl-3,4,4a,5,6,7,8,8a-octahydronaphthalene-1-carboxylic acid | | Descriptor: | (4~{a}~{R},5~{S},6~{R},8~{S},8~{a}~{R})-5-[2-(furan-3-yl)ethyl]-5,6,8~{a}-trimethyl-8-oxidanyl-3,4,4~{a},6,7,8-hexahydronaphthalene-1-carboxylic acid, 1,2-ETHANEDIOL, D-MALATE, ... | | Authors: | Rowland, P. | | Deposit date: | 2019-10-18 | | Release date: | 2020-03-18 | | Last modified: | 2020-04-08 | | Method: | X-RAY DIFFRACTION (1.67 Å) | | Cite: | Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
J.Med.Chem., 63, 2020
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6RQX
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6RYF
 | | High-resolution crystal structure of ERAP1 in complex with 15mer phosphinic peptide | | Descriptor: | 1,2-ETHANEDIOL, 2-[3-(2-HYDROXY-1,1-DIHYDROXYMETHYL-ETHYLAMINO)-PROPYLAMINO]-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Giastas, P, Stratikos, E. | | Deposit date: | 2019-06-10 | | Release date: | 2019-12-18 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (1.72 Å) | | Cite: | Mechanism for antigenic peptide selection by endoplasmic reticulum aminopeptidase 1.
Proc.Natl.Acad.Sci.USA, 2019
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3RJO
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2YD0
 | | Crystal structure of the soluble domain of human endoplasmic reticulum aminopeptidase 1 ERAP1 | | Descriptor: | 1,2-ETHANEDIOL, 2-(3-AMINO-2-HYDROXY-4-PHENYL-BUTYRYLAMINO)-4-METHYL-PENTANOIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Vollmar, M, Kochan, G, Krojer, T, Ugochukwu, E, Muniz, J.R.C, Raynor, J, Chaikuad, A, Allerston, C, von Delft, F, Bountra, C, Arrowsmith, C.H, Weigelt, J, Edwards, A, Knapp, S. | | Deposit date: | 2011-03-17 | | Release date: | 2011-04-13 | | Last modified: | 2020-07-29 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystal Structures of the Endoplasmic Reticulum Aminopeptidase-1 (Erap1) Reveal the Molecular Basis for N-Terminal Peptide Trimming.
Proc.Natl.Acad.Sci.USA, 108, 2011
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5J5E
 | | crystal structure of antigen-ERAP1 domain complex | | Descriptor: | Endoplasmic reticulum aminopeptidase 1 | | Authors: | Sui, L, Gandhi, A, Guo, H.-C. | | Deposit date: | 2016-04-02 | | Release date: | 2017-04-12 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal structure of a polypeptide's C-terminus in complex with the regulatory domain of ER aminopeptidase 1.
Mol.Immunol., 80, 2016
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6MGQ
 | | ERAP1 in the open conformation bound to 10mer phosphinic inhibitor DG014 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Endoplasmic reticulum aminopeptidase 1, Phosphinic inhibitor DG014, ... | | Authors: | Stern, L.J, Maben, Z. | | Deposit date: | 2018-09-14 | | Release date: | 2019-12-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.92 Å) | | Cite: | Conformational dynamics linked to domain closure and substrate binding explain the ERAP1 allosteric regulation mechanism.
Nat Commun, 12, 2021
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3MDJ
 | | ER Aminopeptidase, ERAP1, Bound to the Zinc Aminopeptidase Inhibitor, Bestatin | | Descriptor: | 2-(3-AMINO-2-HYDROXY-4-PHENYL-BUTYRYLAMINO)-4-METHYL-PENTANOIC ACID, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Nguyen, T.T, Stern, L.J. | | Deposit date: | 2010-03-30 | | Release date: | 2011-03-30 | | Last modified: | 2023-09-06 | | Method: | X-RAY DIFFRACTION (2.95 Å) | | Cite: | Structural basis for antigenic peptide precursor processing by the endoplasmic reticulum aminopeptidase ERAP1.
Nat.Struct.Mol.Biol., 18, 2011
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7MWC
 | | ERAP1 binds peptide C-terminus of a LPF sequence (AAAAFKARKF) | | Descriptor: | Endoplasmic reticulum aminopeptidase 1,LPF sequence | | Authors: | Guo, H.C, Sui, L. | | Deposit date: | 2021-05-16 | | Release date: | 2021-07-28 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | ERAP1 binds peptide C-termini of different sequences and/or lengths by a common recognition mechanism.
Immunobiology, 226, 2021
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3QNF
 | | Crystal structure of the open state of human endoplasmic reticulum aminopeptidase 1 ERAP1 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Endoplasmic reticulum aminopeptidase 1, ZINC ION, ... | | Authors: | Vollmar, M, Kochan, G, Krojer, T, Harvey, D, Chaikuad, A, Allerston, C, Muniz, J.R.C, Raynor, J, Ugochukwu, E, Berridge, G, Wordsworth, B.P, von Delft, F, Bountra, C, Arrowsmith, C.H, Edwards, A, Kavanagh, K, Oppermann, U, Structural Genomics Consortium (SGC) | | Deposit date: | 2011-02-08 | | Release date: | 2011-02-23 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Crystal structures of the endoplasmic reticulum aminopeptidase-1 (ERAP1) reveal the molecular basis for N-terminal peptide trimming.
Proc.Natl.Acad.Sci.USA, 108, 2011
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7MWB
 | | ERAP1 binds peptide C-terminus of a SPF sequence (FKARKF) | | Descriptor: | Endoplasmic reticulum aminopeptidase 1,SPF Sequence | | Authors: | Guo, H.C, Sui, L. | | Deposit date: | 2021-05-16 | | Release date: | 2021-07-28 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | ERAP1 binds peptide C-termini of different sequences and/or lengths by a common recognition mechanism.
Immunobiology, 226, 2021
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6M8P
 | | Human ERAP1 bound to phosphinic pseudotripeptide inhibitor DG013 | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, Endoplasmic reticulum aminopeptidase 1, Nalpha-[(2S)-2-{[[(1R)-1-amino-3-phenylpropyl](hydroxy)phosphoryl]methyl}-4-methylpentanoyl]-L-tryptophanamide, ... | | Authors: | Maben, Z, Stern, L.J. | | Deposit date: | 2018-08-22 | | Release date: | 2019-12-18 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3.31 Å) | | Cite: | Conformational dynamics linked to domain closure and substrate binding explain the ERAP1 allosteric regulation mechanism.
Nat Commun, 12, 2021
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