5J6S
 
 | | Crystal structure of Endoplasmic Reticulum Aminopeptidase 2 (ERAP2) in complex with a hydroxamic derivative ligand | | Descriptor: | (2S)-N~1~-benzyl-2-[(4-fluorophenyl)methyl]-N~3~-hydroxypropanediamide, 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Saridakis, E, Giastas, P, Mpakali, A, Deprez-Poulain, R, Stratikos, E. | | Deposit date: | 2016-04-05 | | Release date: | 2017-03-15 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.8 Å) | | Cite: | Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency.
ACS Med Chem Lett, 8, 2017
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1Z5H
 | | Crystal structures of the Tricorn interacting Factor F3 from Thermoplasma acidophilum | | Descriptor: | SULFATE ION, Tricorn protease interacting factor F3, ZINC ION | | Authors: | Kyrieleis, O.J.P, Goettig, P, Kiefersauer, R, Huber, R, Brandstetter, H. | | Deposit date: | 2005-03-18 | | Release date: | 2005-06-28 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Crystal Structures of the Tricorn Interacting Factor F3 from Thermoplasma acidophilum, a Zinc Aminopeptidase in Three Different Conformations
J.MOL.BIOL., 349, 2005
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7KZE
 | | Substrate-dependent divergence of leukotriene A4 hydrolase aminopeptidase activity | | Descriptor: | 1-benzyl-4-methoxybenzene, Leukotriene A-4 hydrolase, TRIETHYLENE GLYCOL, ... | | Authors: | Lee, K.H, Shim, Y, Paige, M, Noble, S.M. | | Deposit date: | 2020-12-10 | | Release date: | 2022-06-15 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Substrate-dependent modulation of the leukotriene A 4 hydrolase aminopeptidase activity and effect in a murine model of acute lung inflammation.
Sci Rep, 12, 2022
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2DQ6
 | | Crystal Structure of Aminopeptidase N from Escherichia coli | | Descriptor: | Aminopeptidase N, SULFATE ION, ZINC ION | | Authors: | Nakajima, Y, Onohara, Y, Ito, K, Yoshimoto, T. | | Deposit date: | 2006-05-22 | | Release date: | 2006-08-01 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | Aminopeptidase N (proteobacteria alanyl aminopeptidase) from Escherichia coli: Crystal structure and conformational change of the methionine 260 residue involved in substrate recognition
J.Biol.Chem., 281, 2006
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3U9W
 | | Structure of human Leukotriene A4 hydrolase in complex with inhibitor sc57461A | | Descriptor: | ACETATE ION, CHLORIDE ION, GLYCEROL, ... | | Authors: | Niegowski, D, Thunnissen, M, Tholander, F, Rinaldo-Matthis, A, Muroya, A, Haeggstrom, J.Z. | | Deposit date: | 2011-10-20 | | Release date: | 2012-10-24 | | Last modified: | 2024-02-28 | | Method: | X-RAY DIFFRACTION (1.25 Å) | | Cite: | Structure of human Leukotriene A4 hydrolase in complex with inhibitor sc57461A
To be Published
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2HPT
 | | Crystal Structure of E. coli PepN (Aminopeptidase N)in complex with Bestatin | | Descriptor: | 2-(3-AMINO-2-HYDROXY-4-PHENYL-BUTYRYLAMINO)-4-METHYL-PENTANOIC ACID, Aminopeptidase N, GLYCEROL, ... | | Authors: | Addlagatta, A, Matthews, B.W, Gay, L. | | Deposit date: | 2006-07-17 | | Release date: | 2006-08-15 | | Last modified: | 2023-08-30 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structure of aminopeptidase N from Escherichia coli suggests a compartmentalized, gated active site.
Proc.Natl.Acad.Sci.Usa, 103, 2006
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2HPO
 | | Structure of Aminopeptidase N from E. coli Suggests a Compartmentalized, Gated Active Site | | Descriptor: | Aminopeptidase N, GLYCEROL, ZINC ION | | Authors: | Addlagatta, A, Matthews, B.W, Gay, L. | | Deposit date: | 2006-07-17 | | Release date: | 2006-08-15 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Structure of aminopeptidase N from Escherichia coli suggests a compartmentalized, gated active site.
Proc.Natl.Acad.Sci.Usa, 103, 2006
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7NUP
 | | Endoplasmic reticulum aminopeptidase 2 complexed with a mixed hydroxamic and sulfonyl ligand | | Descriptor: | (3~{S})-4-(4-hydroxyphenyl)-~{N}-oxidanyl-3-[5-[[(5-phenylthiophen-2-yl)sulfonylamino]methyl]-1,2,3-triazol-1-yl]butanamide, 1,2-ETHANEDIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Mpakali, A, Giastas, P, Stratikos, E. | | Deposit date: | 2021-03-12 | | Release date: | 2022-06-22 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Endoplasmic reticulum aminopeptidase 2 complexed with a mixed hydroxamic and sulfonyl ligand
To Be Published
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7NSK
 | | Endoplasmic reticulum aminopeptidase 2 complexed with a hydroxamic ligand | | Descriptor: | (2~{S})-3-(4-hydroxyphenyl)-~{N}-oxidanyl-2-[4-[[(5-pyridin-2-ylthiophen-2-yl)sulfonylamino]methyl]-1,2,3-triazol-1-yl]propanamide, 1,2-ETHANEDIOL, 1-ETHOXY-2-(2-ETHOXYETHOXY)ETHANE, ... | | Authors: | Mpakali, A, Giastas, P, Stratikos, E. | | Deposit date: | 2021-03-08 | | Release date: | 2022-06-22 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3.1 Å) | | Cite: | Endoplasmic reticulum aminopeptidase 2 in complex with a phosphinic ligand
To Be Published
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7P7P
 | | Crystal structure of ERAP2 aminopeptidase in complex with phosphinic pseudotripeptide((1R)-1-Amino-3-phenylpropyl){(2S)-3-[((2S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino]-2-{[3-(2-hydroxyphenyl)-isoxazol-5-yl]methyl}-3-oxopropyl}phosphinic acid | | Descriptor: | 1,2-ETHANEDIOL, 1,3-PROPANDIOL, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, ... | | Authors: | Giastas, P, Stratikos, E, Mpakali, A. | | Deposit date: | 2021-07-20 | | Release date: | 2022-01-26 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | Inhibitor-Dependent Usage of the S1' Specificity Pocket of ER Aminopeptidase 2.
Acs Med.Chem.Lett., 13, 2022
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3SE6
 | | Crystal structure of the human Endoplasmic Reticulum Aminopeptidase 2 | | Descriptor: | 2-(N-MORPHOLINO)-ETHANESULFONIC 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: | Birtley, J.R, Saridakis, E, Stratikos, E, Mavridis, I.M. | | Deposit date: | 2011-06-10 | | Release date: | 2011-12-21 | | Last modified: | 2020-07-29 | | Method: | X-RAY DIFFRACTION (3.08 Å) | | Cite: | The crystal structure of human endoplasmic reticulum aminopeptidase 2 reveals the atomic basis for distinct roles in antigen processing.
Biochemistry, 51, 2012
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3T8V
 | | A bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases | | Descriptor: | M1 family aminopeptidase, MAGNESIUM ION, N-[(2-{2-[(N-{(2S,3R)-3-amino-4-[4-(benzyloxy)phenyl]-2-hydroxybutanoyl}-L-alanyl)amino]ethoxy}ethoxy)acetyl]-4-benzoyl-L-phenylalanyl-N~6~-hex-5-ynoyllysinamide, ... | | Authors: | McGowan, S, Klemba, M, Greebaum, D.C. | | Deposit date: | 2011-08-01 | | Release date: | 2011-09-28 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Bestatin-based chemical biology strategy reveals distinct roles for malaria M1- and M17-family aminopeptidases
Proc.Natl.Acad.Sci.USA, 108, 2011
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8AVA
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8AWH
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7ZYF
 | | Insulin regulated aminopeptidase (IRAP) in complex with a nanomolar alpha hydroxy beta amino acid based inhibitor. | | Descriptor: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | Authors: | Mpakali, A, Stratikos, E, Giastas, P, Papakyriakou, A. | | Deposit date: | 2022-05-24 | | Release date: | 2022-07-20 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.81 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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2GTQ
 | | Crystal structure of aminopeptidase N from human pathogen Neisseria meningitidis | | Descriptor: | SULFATE ION, ZINC ION, aminopeptidase N | | Authors: | Nocek, B, Mulligan, R, Bargassa, M, Joachimiak, A, Midwest Center for Structural Genomics (MCSG) | | Deposit date: | 2006-04-28 | | Release date: | 2006-05-30 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (2.05 Å) | | Cite: | Crystal structure of aminopeptidase N from human pathogen Neisseria meningitidis.
Proteins, 70, 2007
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5K1V
 | | Crystal structure of Endoplasmic Reticulum aminopeptidase 2 (ERAP2) in complex with a diaminobenzoic acid derivative ligand. | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Endoplasmic reticulum aminopeptidase 2, ... | | Authors: | Saridakis, E, Papakyriakou, A, Giastas, P, Mpakali, A, Mavridis, I.M, Stratikos, E. | | Deposit date: | 2016-05-18 | | Release date: | 2017-03-29 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.897 Å) | | Cite: | Crystal Structures of ERAP2 Complexed with Inhibitors Reveal Pharmacophore Requirements for Optimizing Inhibitor Potency.
ACS Med Chem Lett, 8, 2017
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7AUZ
 | | LTA4 hydrolase in complex with compound LYS006 | | Descriptor: | (3~{S})-3-azanyl-4-[5-[4-(5-chloranyl-3-fluoranyl-pyridin-2-yl)oxyphenyl]-1,2,3,4-tetrazol-2-yl]butanoic acid, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2020-11-03 | | Release date: | 2021-02-17 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A 4 Hydrolase.
J.Med.Chem., 64, 2021
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7AV1
 | | LTA4 hydrolase in complex with fragment2 | | Descriptor: | 2-[5-(4-methoxyphenyl)-1,2,3,4-tetrazol-2-yl]ethanamine, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2020-11-03 | | Release date: | 2021-02-17 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.79 Å) | | Cite: | Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A 4 Hydrolase.
J.Med.Chem., 64, 2021
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7AV0
 | | LTA4 hydrolase in complex with compound R(13) | | Descriptor: | (3~{R})-3-azanyl-4-[5-[4-(4-chloranylphenoxy)phenyl]-1,2,3,4-tetrazol-2-yl]butanoic acid, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2020-11-03 | | Release date: | 2021-02-17 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A 4 Hydrolase.
J.Med.Chem., 64, 2021
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7AV2
 | | LTA4 hydrolase in complex with fragment1 | | Descriptor: | (4-phenoxyphenyl)methanol, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2020-11-03 | | Release date: | 2021-02-17 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Discovery of LYS006, a Potent and Highly Selective Inhibitor of Leukotriene A 4 Hydrolase.
J.Med.Chem., 64, 2021
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5C97
 | | Insulin regulated aminopeptidase | | Descriptor: | 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, ... | | Authors: | Mpakali, A, Saridakis, E, Harlos, K, Zhao, Y, Stratikos, E. | | Deposit date: | 2015-06-26 | | Release date: | 2015-08-26 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.37 Å) | | Cite: | 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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5DLL
 | | Aminopeptidase N (pepN) from Francisella tularensis subsp. tularensis SCHU S4 | | Descriptor: | Aminopeptidase N, CHLORIDE ION, PHOSPHATE ION, ... | | Authors: | Borek, D, Raczynska, J, Dubrovska, I, Grimshaw, S, Minasov, G, Shuvalova, L, Kwon, K, Anderson, W.F, Otwinowski, Z, Center for Structural Genomics of Infectious Diseases (CSGID) | | Deposit date: | 2015-09-07 | | Release date: | 2015-09-16 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.51 Å) | | Cite: | Aminopeptidase N (pepN) from Francisella tularensis subsp. tularensis SCHU S4
To Be Published
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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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5CU5
 | | Crystal structure of ERAP2 without catalytic Zn(II) atom | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Endoplasmic reticulum aminopeptidase 2, ... | | Authors: | Saridakis, E, Mathioudakis, N, Giastas, P, Mavridis, I.M, Stratikos, E. | | Deposit date: | 2015-07-24 | | Release date: | 2015-09-23 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (3.02 Å) | | Cite: | Structural Basis for Antigenic Peptide Recognition and Processing by Endoplasmic Reticulum (ER) Aminopeptidase 2.
J.Biol.Chem., 290, 2015
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