1SQM
 
 | | STRUCTURE OF [R563A] LEUKOTRIENE A4 HYDROLASE | | Descriptor: | ACETIC ACID, IMIDAZOLE, LEUKOTRIENE A-4 HYDROLASE, ... | | Authors: | Tholander, F.O.T, Rudberg, P.C, Thunnissen, M.M.G.M, Haeggstrom, J.Z. | | Deposit date: | 2004-03-19 | | Release date: | 2004-08-03 | | Last modified: | 2024-02-14 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Leukotriene A4 hydrolase: identification of a common carboxylate recognition site for the epoxide hydrolase and aminopeptidase substrates
J.Biol.Chem., 279, 2004
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6YDX
 | | Insulin-regulated aminopeptidase complexed with a macrocyclic peptidic inhibitor | | Descriptor: | 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, ... | | Authors: | Mpakali, A, Saridakis, E, Giastas, P, Stratikos, E. | | Deposit date: | 2020-03-21 | | Release date: | 2020-07-22 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Structural Basis of Inhibition of Insulin-Regulated Aminopeptidase by a Macrocyclic Peptidic Inhibitor.
Acs Med.Chem.Lett., 11, 2020
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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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1GW6
 | | STRUCTURE OF LEUKOTRIENE A4 HYDROLASE D375N MUTANT | | Descriptor: | 2-(3-AMINO-2-HYDROXY-4-PHENYL-BUTYRYLAMINO)-4-METHYL-PENTANOIC ACID, ACETATE ION, IMIDAZOLE, ... | | Authors: | Rudberg, P.C, Tholander, F, Thunnissen, M.M.G.M, Samuelsson, B, Haeggstrom, J.Z. | | Deposit date: | 2002-03-07 | | Release date: | 2003-03-06 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.2 Å) | | Cite: | Leukotriene A4 Hydrolase: Selective Abrogation of Leukotriene B4 Formation by Mutation of Aspartic Acid 375
Proc.Natl.Acad.Sci.USA, 99, 2002
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2R59
 | | Leukotriene A4 hydrolase complexed with inhibitor RB3041 | | Descriptor: | ACETIC ACID, Leukotriene A-4 hydrolase, N-{(2S)-3-[(R)-[(1R)-1-amino-2-phenylethyl](hydroxy)phosphoryl]-2-benzylpropanoyl}-L-phenylalanine, ... | | Authors: | Tholander, F, Haeggstrom, J.Z, Thunnissen, M, Muroya, A, Roques, B.P, Fournie-Zaluski, M.C. | | Deposit date: | 2007-09-03 | | Release date: | 2008-08-12 | | Last modified: | 2024-04-03 | | Method: | X-RAY DIFFRACTION (1.89 Å) | | Cite: | Structure-based dissection of the active site chemistry of leukotriene a4 hydrolase: implications for m1 aminopeptidases and inhibitor design.
Chem.Biol., 15, 2008
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1H19
 | | STRUCTURE OF [E271Q]LEUKOTRIENE A4 HYDROLASE | | Descriptor: | ACETIC ACID, IMIDAZOLE, LEUKOTRIENE A-4 HYDROLASE, ... | | Authors: | Rudberg, P.C, Tholander, F, Thunnissen, M.M.G.M, Haeggstrom, J.Z. | | Deposit date: | 2002-07-04 | | Release date: | 2002-08-08 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Leukotriene A4 Hydrolase/Aminopeptidase, Glutamate 271 is a Catalyticresidue with Specific Roles in Two Distinct Enzyme Mechanisms
J.Biol.Chem., 277, 2002
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1HS6
 | | STRUCTURE OF LEUKOTRIENE A4 HYDROLASE COMPLEXED WITH BESTATIN. | | Descriptor: | 2-(3-AMINO-2-HYDROXY-4-PHENYL-BUTYRYLAMINO)-4-METHYL-PENTANOIC ACID, ACETATE ION, IMIDAZOLE, ... | | Authors: | Thunnissen, M.M.G.M, Nordlund, P.N, Haeggstrom, J.Z. | | Deposit date: | 2000-12-24 | | Release date: | 2001-06-24 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Crystal structure of human leukotriene A(4) hydrolase, a bifunctional enzyme in inflammation.
Nat.Struct.Biol., 8, 2001
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6OIU
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6O5H
 | | The effect of modifier structure on the activation of leukotriene A4 hydrolase aminopeptidase activity. | | Descriptor: | 4-{4-[(4-methoxyphenyl)methyl]phenyl}-1,3-thiazol-2-amine, Leukotriene A-4 hydrolase, ZINC ION | | Authors: | Noble, S.M, Lee, K.H, Paige, M. | | Deposit date: | 2019-03-03 | | Release date: | 2019-12-04 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.84 Å) | | Cite: | Effect of Modifier Structure on the Activation of Leukotriene A4Hydrolase Aminopeptidase Activity.
J.Med.Chem., 62, 2019
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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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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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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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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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4DPR
 | | Structure of human Leukotriene A4 hydrolase in complex with inhibitor captopril | | Descriptor: | ACETIC ACID, GLYCEROL, L-CAPTOPRIL, ... | | Authors: | Stsiapanava, A, Haeggstrom, J.Z, Rinaldo-Matthis, A. | | Deposit date: | 2012-02-14 | | Release date: | 2013-02-20 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (2.02 Å) | | Cite: | Capturing LTA4hydrolase in action: Insights to the chemistry and dynamics of chemotactic LTB4synthesis.
Proc. Natl. Acad. Sci. U.S.A., 114, 2017
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4E36
 | | Crystal structure of the human Endoplasmic Reticulum Aminopeptidase 2 variant N392K | | 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, Pegias, P, Stratikos, E, Mavridis, I.M. | | Deposit date: | 2012-03-09 | | Release date: | 2012-08-29 | | Last modified: | 2023-09-13 | | Method: | X-RAY DIFFRACTION (3.22 Å) | | Cite: | A common single nucleotide polymorphism in endoplasmic reticulum aminopeptidase 2 induces a specificity switch that leads to altered antigen processing.
J.Immunol., 189, 2012
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7PFS
 | | Crystal structure of ERAP2 aminopeptidase in complex with phosphinic pseudotripeptide ((1R)-1-Amino-3-phenylpropyl){2-([1,1:3,1-terphenyl]-5-ylmethyl)-3-[((2S)-1-amino-1-oxo-3-phenylpropan-2-yl)-amino]-3-oxopropyl}phosphinic acid | | 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, Stratikos, E, Mpakali, A. | | Deposit date: | 2021-08-12 | | Release date: | 2022-01-26 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Inhibitor-Dependent Usage of the S1' Specificity Pocket of ER Aminopeptidase 2.
Acs Med.Chem.Lett., 13, 2022
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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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6U7E
 | | HCoV-229E RBD Class III in complex with human APN | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Aminopeptidase N, ... | | Authors: | Tomlinson, A.C.A, Li, Z, Rini, J.M. | | Deposit date: | 2019-09-02 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (3 Å) | | Cite: | The human coronavirus HCoV-229E S-protein structure and receptor binding.
Elife, 8, 2019
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7LLQ
 | | Substrate-dependent divergence of leukotriene A4 hydrolase aminopeptidase activity | | Descriptor: | 1-benzyl-4-methoxybenzene, 1-{4-oxo-4-[(2S)-pyrrolidin-2-yl]butanoyl}-L-proline, Leukotriene A-4 hydrolase, ... | | Authors: | Lee, K.H, Lee, S.H, Shim, Y.M, Paige, M, Noble, S.M. | | Deposit date: | 2021-02-04 | | Release date: | 2022-06-22 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (2.85 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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6U7G
 | | HCoV-229E RBD Class V in complex with human APN | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Aminopeptidase N, ... | | Authors: | Tomlinson, A, Li, Z, Rini, J.M. | | Deposit date: | 2019-09-02 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | The human coronavirus HCoV-229E S-protein structure and receptor binding.
Elife, 8, 2019
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6U7F
 | | HCoV-229E RBD Class IV in complex with human APN | | Descriptor: | 2-acetamido-2-deoxy-beta-D-glucopyranose, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-2-acetamido-2-deoxy-beta-D-glucopyranose, Aminopeptidase N, ... | | Authors: | Tomlinson, A.C.A, Li, Z, Rini, J.M. | | Deposit date: | 2019-09-02 | | Release date: | 2019-11-13 | | Last modified: | 2023-10-11 | | Method: | X-RAY DIFFRACTION (2.75 Å) | | Cite: | The human coronavirus HCoV-229E S-protein structure and receptor binding.
Elife, 8, 2019
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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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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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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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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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