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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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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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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6KOY
 | | Crystal structure of two domain M1 Zinc metallopeptidase E323A mutant bound to L-tryptophan amino acid | | Descriptor: | TRYPTOPHAN, ZINC ION, Zinc metalloprotease | | Authors: | Agrawal, R, Kumar, A, Kumar, A, Makde, R.D. | | Deposit date: | 2019-08-13 | | Release date: | 2020-01-22 | | Last modified: | 2023-11-22 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | Structural basis for the unusual substrate specificity of unique two-domain M1 metallopeptidase.
Int.J.Biol.Macromol., 147, 2020
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4NAQ
 | | Crystal structure of porcine aminopeptidase-N complexed with poly-alanine | | 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: | Chen, L, Lin, Y.L, Peng, G, Li, F. | | Deposit date: | 2013-10-22 | | Release date: | 2013-12-04 | | Last modified: | 2020-07-29 | | Method: | X-RAY DIFFRACTION (2.1 Å) | | Cite: | Structural basis for multifunctional roles of mammalian aminopeptidase N.
Proc.Natl.Acad.Sci.USA, 109, 2012
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4F5C
 | | Crystal structure of the spike receptor binding domain of a porcine respiratory coronavirus in complex with the pig aminopeptidase N ectodomain | | 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: | Santiago, C, Reguera, J, Gaurav, M, Ordono, D, Enjuanes, L, Casasnovas, J.M. | | Deposit date: | 2012-05-13 | | Release date: | 2012-08-22 | | Last modified: | 2020-07-29 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Structural bases of coronavirus attachment to host aminopeptidase N and its inhibition by neutralizing antibodies.
Plos Pathog., 8, 2012
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3CHQ
 | | Crystal structure of leukotriene a4 hydrolase in complex with N5-[4-(phenylmethoxy)phenyl]-L-glutamine | | Descriptor: | (2S)-2-amino-5-oxo-5-[(4-phenylmethoxyphenyl)amino]pentanoic acid, IMIDAZOLE, Leukotriene A-4 hydrolase, ... | | Authors: | Thunnissen, M.M.G.M, Adler, M, Whitlow, M. | | Deposit date: | 2008-03-10 | | Release date: | 2008-04-22 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (2.09 Å) | | Cite: | Synthesis of glutamic acid analogs as potent inhibitors of leukotriene A4 hydrolase.
Bioorg.Med.Chem., 16, 2008
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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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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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7U0L
 | | Crystal structure of the CCoV-HuPn-2018 RBD (domain B) in complex with canine 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: | Tortorici, M.A, Veesler, D, Seattle Structural Genomics Center for Infectious Disease (SSGCID) | | Deposit date: | 2022-02-18 | | Release date: | 2022-08-24 | | Last modified: | 2023-10-18 | | Method: | X-RAY DIFFRACTION (3.3 Å) | | Cite: | Structure, receptor recognition, and antigenicity of the human coronavirus CCoV-HuPn-2018 spike glycoprotein.
Cell, 185, 2022
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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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2VJ8
 | | Complex of human leukotriene A4 hydrolase with a hydroxamic acid inhibitor | | Descriptor: | 6-[{(2S)-2-AMINO-3-[4-(BENZYLOXY)PHENYL]PROPYL}(HYDROXY)AMINO]-6-OXOHEXANOIC ACID), ACETATE ION, IMIDAZOLE, ... | | Authors: | Thunnissen, M.M.G.M, Andersson, B, Wong, C.-H, Samuelsson, B, Haeggstrom, J.Z. | | Deposit date: | 2007-12-07 | | Release date: | 2008-01-15 | | Last modified: | 2023-12-13 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Crystal Structures of Leukotriene A4 Hydrolase in Complex with Captopril and Two Competitive Tight-Binding Inhibitors
Faseb J., 16, 2002
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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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7SH0
 | | CRYSTAL STRUCTURE OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 2 (ERAP2) COMPLEX WITH A HIGHLY SELECTIVE AND POTENT SMALL MOLECULE | | Descriptor: | (2S)-N-hydroxy-3-(4-methoxyphenyl)-2-[4-({[5-(pyridin-2-yl)thiophene-2-sulfonyl]amino}methyl)-1H-1,2,3-triazol-1-yl]propanamide, 2-(N-MORPHOLINO)-ETHANESULFONIC ACID, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | Authors: | Li, L, Bouvier, M. | | Deposit date: | 2021-10-07 | | Release date: | 2022-07-20 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (3.2 Å) | | Cite: | Discovery of the First Selective Nanomolar Inhibitors of ERAP2 by Kinetic Target-Guided Synthesis.
Angew.Chem.Int.Ed.Engl., 61, 2022
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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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3KED
 | | Crystal structure of Aminopeptidase N in complex with 2,4-diaminobutyric acid | | Descriptor: | 2,4-DIAMINOBUTYRIC ACID, Aminopeptidase N, GLYCEROL, ... | | Authors: | Addlagatta, A, Gumpena, R. | | Deposit date: | 2009-10-25 | | Release date: | 2010-11-03 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Discovery of alpha, beta- and alpha, gamma-Diamino Acid Scaffolds for the Inhibition of M1 Family Aminopeptidases
Chemmedchem, 6, 2011
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5FWQ
 | | Apo structure of human Leukotriene A4 hydrolase | | Descriptor: | ACETATE ION, HUMAN LEUKOTRIENE A4 HYDROLASE, IMIDAZOLE, ... | | Authors: | Wittmann, S.K, Kalinowsky, L, Kramer, J, Bloecher, R, Steinhilber, D, Pogoryelov, D, Proschak, E, Heering, J. | | Deposit date: | 2016-02-19 | | Release date: | 2016-10-05 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (2.047 Å) | | Cite: | Thermodynamic properties of leukotriene A4hydrolase inhibitors.
Bioorg.Med.Chem., 24, 2016
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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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4RSY
 | | Crystal structures of the Human leukotriene A4 Hydrolase complex with a potential inhibitor H7 | | Descriptor: | 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide, ACETIC ACID, IMIDAZOLE, ... | | Authors: | Ouyang, P, Lu, W, Cui, K, Huang, J. | | Deposit date: | 2014-11-12 | | Release date: | 2015-12-02 | | Last modified: | 2024-03-20 | | Method: | X-RAY DIFFRACTION (1.93 Å) | | Cite: | Structure of Human Leukotriene A4 Hydrolase in complex with inhibitor H1
To be Published
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4RVB
 | | Crystal Structure Analysis of the Human Leukotriene A4 Hydrolase | | Descriptor: | ACETATE ION, ACETIC ACID, GLYCEROL, ... | | Authors: | Ouyang, P, Lu, W, Cui, K, Huang, J. | | Deposit date: | 2014-11-25 | | Release date: | 2015-12-02 | | Last modified: | 2023-11-08 | | Method: | X-RAY DIFFRACTION (1.93 Å) | | Cite: | Crystal Structure Analysis of the Human Leukotriene A4 Hydrolase
To be Published
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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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4WZ9
 | | APN1 from Anopheles gambiae | | Descriptor: | 2-[N-CYCLOHEXYLAMINO]ETHANE SULFONIC ACID, AGAP004809-PA, ALA-ALA-ALA-LYS-ALA, ... | | Authors: | Atkinson, S.C, Armistead, J.S, Mathias, D.K, Sandeu, M.M, Tao, D, Borhani-Dizaji, N, Morlais, I, Dinglasan, R.R, Borg, N.A. | | Deposit date: | 2014-11-19 | | Release date: | 2015-06-17 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (2.65 Å) | | Cite: | The Anopheles-midgut APN1 structure reveals a new malaria transmission-blocking vaccine epitope.
Nat.Struct.Mol.Biol., 22, 2015
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4X2U
 | | X-ray crystal structure of the orally available aminopeptidase inhibitor, Tosedostat, bound to the M1 Alanyl Aminopeptidase from P. falciparum | | Descriptor: | (2S)-({(2R)-2-[(1S)-1-hydroxy-2-(hydroxyamino)-2-oxoethyl]-4-methylpentanoyl}amino)(phenyl)ethanoic acid, GLYCEROL, M1 family aminopeptidase, ... | | Authors: | Drinkwater, N, McGowan, S. | | Deposit date: | 2014-11-27 | | Release date: | 2015-02-18 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.5 Å) | | Cite: | X-ray crystal structures of an orally available aminopeptidase inhibitor, Tosedostat, bound to anti-malarial drug targets PfA-M1 and PfA-M17.
Proteins, 83, 2015
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2DQM
 | | Crystal Structure of Aminopeptidase N complexed with bestatin | | Descriptor: | 2-(3-AMINO-2-HYDROXY-4-PHENYL-BUTYRYLAMINO)-4-METHYL-PENTANOIC ACID, Aminopeptidase N, SULFATE ION, ... | | Authors: | Onohara, Y, Nakajima, Y, Ito, K, Yoshimoto, T. | | Deposit date: | 2006-05-29 | | Release date: | 2006-08-01 | | Last modified: | 2023-10-25 | | Method: | X-RAY DIFFRACTION (1.6 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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1Z1W
 | | Crystal structures of the tricorn interacting facor F3 from Thermoplasma acidophilum, a zinc aminopeptidase in three different conformations | | 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: | 2005-03-07 | | Release date: | 2005-05-31 | | Last modified: | 2024-03-13 | | Method: | X-RAY DIFFRACTION (2.7 Å) | | Cite: | Crystal Structures of the Tricorn Interacting Factor F3 from Thermoplasma acidophilum, a Zinc Aminopeptidase in Three Different Conformations
J.MOL.BIOL., 394, 2005
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