5D6E
 
 | | Structure of human methionine aminopeptidase 2 with covalent spiroepoxytriazole inhibitor (-)-31b | | Descriptor: | (4R,7S)-7-hydroxy-1-(4-methoxybenzyl)-7-methyl-4,5,6,7-tetrahydro-1H-benzotriazol-4-yl propan-2-ylcarbamate, COBALT (II) ION, Methionine aminopeptidase 2, ... | | Authors: | Janowski, R, Miller, A.K, Niessing, D. | | Deposit date: | 2015-08-12 | | Release date: | 2016-01-13 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.49 Å) | | Cite: | Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
Acs Chem.Biol., 11, 2016
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5D6F
 | | Structure of human methionine aminopeptidase-2 complexed with spiroepoxytriazole inhibitor (+)-31b | | Descriptor: | (4S,7R)-7-hydroxy-1-(4-methoxybenzyl)-7-methyl-4,5,6,7-tetrahydro-1H-benzotriazol-4-yl propan-2-ylcarbamate, 1,2-ETHANEDIOL, COBALT (II) ION, ... | | Authors: | Janowski, R, Miller, A.K, Niessing, D. | | Deposit date: | 2015-08-12 | | Release date: | 2016-01-13 | | Last modified: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.55 Å) | | Cite: | Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
Acs Chem.Biol., 11, 2016
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1QZY
 | | Human Methionine Aminopeptidase in complex with bengamide inhibitor LAF153 and cobalt | | Descriptor: | (E)-(2R,3R,4S,5R)-3,4,5-TRIHYDROXY-2-METHOXY-8,8-DIMETHYL-NON-6-ENOIC ACID ((3S,6R)-6-HYDROXY-2-OXO-AZEPAN-3-YL)-AMIDE, COBALT (II) ION, Methionine aminopeptidase 2, ... | | Authors: | Eck, M.J, Song, H.K, Morollo, A. | | Deposit date: | 2003-09-18 | | Release date: | 2003-11-25 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Proteomics-based target identification: bengamides as a new class of methionine aminopeptidase inhibitors.
J.Biol.Chem., 278, 2003
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5JFR
 | | Potent, Reversible MetAP2 Inhibitors via Fragment Based Drug Discovery | | Descriptor: | 1,2-ETHANEDIOL, 7-fluoro-4-(5-methyl-3H-imidazo[4,5-b]pyridin-6-yl)-2,4-dihydropyrazolo[4,3-b]indole, DIMETHYL SULFOXIDE, ... | | Authors: | Dougan, D.R, Lawson, J.D. | | Deposit date: | 2016-04-19 | | Release date: | 2016-05-25 | | Last modified: | 2016-06-15 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 2.
Bioorg.Med.Chem.Lett., 26, 2016
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1B6A
 | | HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470 | | Descriptor: | (1R,2S,3S,4R)-4-hydroxy-2-methoxy-4-methyl-3-[(2R,3R)-2-methyl-3-(3-methylbut-2-en-1-yl)oxiran-2-yl]cyclohexyl (chloroacetyl)carbamate, COBALT (II) ION, METHIONINE AMINOPEPTIDASE | | Authors: | Liu, S, Clardy, J.C. | | Deposit date: | 1999-01-13 | | Release date: | 2000-01-13 | | Last modified: | 2023-08-02 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | Structure of human methionine aminopeptidase-2 complexed with fumagillin.
Science, 282, 1998
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6QEJ
 | | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR Thiophene-2-sulfonic acid (4-fluoro-benzyl)-(4H-[1,2,4]triazol-3-ylmethyl)-amide | | Descriptor: | 1,2-ETHANEDIOL, MANGANESE (II) ION, Methionine aminopeptidase 2, ... | | Authors: | Musil, D, Heinrich, T, Lehmann, M. | | Deposit date: | 2019-01-07 | | Release date: | 2019-05-01 | | Last modified: | 2019-06-05 | | Method: | X-RAY DIFFRACTION (1.62 Å) | | Cite: | Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
J.Med.Chem., 62, 2019
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1YW9
 | | h-MetAP2 complexed with A849519 | | Descriptor: | 2-[({2-[(1Z)-3-(DIMETHYLAMINO)PROP-1-ENYL]-4-FLUOROPHENYL}SULFONYL)AMINO]-5,6,7,8-TETRAHYDRONAPHTHALENE-1-CARBOXYLIC ACID, MANGANESE (II) ION, Methionine aminopeptidase 2 | | Authors: | Park, C.H. | | Deposit date: | 2005-02-17 | | Release date: | 2006-02-21 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.64 Å) | | Cite: | Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
J.Med.Chem., 49, 2006
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5LYW
 | | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR 6-((R)-2-o-Tolyloxymethyl-pyrrolidin-1-yl)-9H-purine | | Descriptor: | 6-[(2~{R})-2-[(2-methylphenoxy)methyl]pyrrolidin-1-yl]-7~{H}-purine, MANGANESE (II) ION, Methionine aminopeptidase 2 | | Authors: | Musil, D, Heinrich, T, Knoechel, T, Lehmann, M. | | Deposit date: | 2016-09-28 | | Release date: | 2017-08-16 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.69 Å) | | Cite: | Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates.
Bioorg. Med. Chem. Lett., 27, 2017
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8OXG
 | | Crystal structure of human methionine aminopeptidase-2 complexed with (3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-buten-1-yl)-2-oxiranyl]-1-oxaspiro[2.5]oct-6-yl N-(trans-4-aminocyclohexyl)carbamate | | Descriptor: | MANGANESE (II) ION, Methionine aminopeptidase 2, [(1~{R},2~{S},3~{S},4~{R})-2-methoxy-4-methyl-3-[(2~{R},3~{S})-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-4-oxidanyl-cyclohexyl] ~{N}-(4-azanylcyclohexyl)carbamate | | Authors: | Moss, S, Cornelius, P. | | Deposit date: | 2023-05-02 | | Release date: | 2024-04-10 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (1.731 Å) | | Cite: | Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity.
Mol.Cancer Ther., 23, 2024
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5CLS
 | | Structure of human methionine aminopeptidase-2 complexed with spiroepoxytriazole inhibitor (+)-31a | | Descriptor: | (4R,7R)-7-hydroxy-1-(4-methoxybenzyl)-7-methyl-4,5,6,7-tetrahydro-1H-benzotriazol-4-yl propan-2-ylcarbamate, CHLORIDE ION, CITRIC ACID, ... | | Authors: | Janowski, R, Miller, A.K, Niessing, D. | | Deposit date: | 2015-07-16 | | Release date: | 2016-01-13 | | Last modified: | 2019-11-20 | | Method: | X-RAY DIFFRACTION (1.75 Å) | | Cite: | Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.
Acs Chem.Biol., 11, 2016
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6QEF
 | | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR (S)-3-Hydroxy-2-oxo-1-phenyl-pyrrolidine-3-carboxylic acid 3-chloro-5-fluoro-benzylamide | | Descriptor: | (3~{S})-~{N}-[(3-chloranyl-5-fluoranyl-phenyl)methyl]-3-oxidanyl-2-oxidanylidene-1-phenyl-pyrrolidine-3-carboxamide, 1,2-ETHANEDIOL, GLYCEROL, ... | | Authors: | Musil, D, Heinrich, T, Lehmann, M. | | Deposit date: | 2019-01-07 | | Release date: | 2019-05-01 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (1.79 Å) | | Cite: | Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
J.Med.Chem., 62, 2019
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6QEI
 | | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX WITH AN INHIBITOR 5,6-Difluoro-3-(2-isopropoxy-4-piperazin-1-yl-phenyl)-1H-indole-2-carboxylic acid amide | | Descriptor: | 1,2-ETHANEDIOL, 5,6-bis(fluoranyl)-3-(4-piperazin-1-yl-2-propan-2-yloxy-phenyl)-1~{H}-indole-2-carboxamide, DIMETHYL SULFOXIDE, ... | | Authors: | Musil, D, Heinrich, T, Lehmann, M. | | Deposit date: | 2019-01-07 | | Release date: | 2019-05-01 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
J.Med.Chem., 62, 2019
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6QED
 | | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR (S)-3-Hydroxy-2-oxo-1-(2-oxo-1,2,3,4-tetrahydro-quinolin-6-yl)-pyrrolidine-3-carboxylic acid 3-chloro-5-fluoro-benzylamide | | Descriptor: | (3~{S})-~{N}-[(3-chloranyl-5-fluoranyl-phenyl)methyl]-3-oxidanyl-2-oxidanylidene-1-(2-oxidanylidene-3,4-dihydro-1~{H}-quinolin-6-yl)pyrrolidine-3-carboxamide, 1,2-ETHANEDIOL, DIMETHYL SULFOXIDE, ... | | Authors: | Musil, D, Heinrich, T, Lehmann, M. | | Deposit date: | 2019-01-07 | | Release date: | 2019-05-01 | | Last modified: | 2024-05-15 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Discovery and Structure-Based Optimization of Next-Generation Reversible Methionine Aminopeptidase-2 (MetAP-2) Inhibitors.
J.Med.Chem., 62, 2019
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1BN5
 | | HUMAN METHIONINE AMINOPEPTIDASE 2 | | Descriptor: | COBALT (II) ION, METHIONINE AMINOPEPTIDASE, TERTIARY-BUTYL ALCOHOL | | Authors: | Liu, S, Widom, J, Kemp, C.W, Crews, C.M, Clardy, J.C. | | Deposit date: | 1998-07-31 | | Release date: | 1999-07-31 | | Last modified: | 2023-08-09 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structure of human methionine aminopeptidase-2 complexed with fumagillin.
Science, 282, 1998
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1BOA
 | | HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN | | Descriptor: | COBALT (II) ION, FUMAGILLIN, METHIONINE AMINOPEPTIDASE | | Authors: | Liu, S, Widom, J, Kemp, C.W, Crews, C.M, Clardy, J.C. | | Deposit date: | 1998-08-01 | | Release date: | 1999-08-01 | | Last modified: | 2023-08-09 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structure of human methionine aminopeptidase-2 complexed with fumagillin.
Science, 282, 1998
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1B59
 | | COMPLEX OF HUMAN METHIONINE AMINOPEPTIDASE-2 COMPLEXED WITH OVALICIN | | Descriptor: | 3,4-DIHYDROXY-2-METHOXY-4-METHYL-3-[2-METHYL-3-(3-METHYL-BUT-2-ENYL) -OXIRANYL]-CYCLOHEXANONE, COBALT (II) ION, PROTEIN (METHIONINE AMINOPEPTIDASE) | | Authors: | Liu, S, Clardy, J.C. | | Deposit date: | 1999-01-13 | | Release date: | 2000-01-14 | | Last modified: | 2023-08-09 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Structure of human methionine aminopeptidase-2 complexed with fumagillin.
Science, 282, 1998
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5JHU
 | | Potent, Reversible MetAP2 Inhibitors via FBDD | | Descriptor: | DIMETHYL SULFOXIDE, GLYCEROL, MANGANESE (II) ION, ... | | Authors: | Dougan, D.R. | | Deposit date: | 2016-04-21 | | Release date: | 2016-05-25 | | Last modified: | 2017-11-22 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Discovery of potent, reversible MetAP2 inhibitors via fragment based drug discovery and structure based drug design-Part 1.
Bioorg.Med.Chem.Lett., 26, 2016
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1YW7
 | | h-MetAP2 complexed with A444148 | | Descriptor: | 5-METHYL-2-[(PHENYLSULFONYL)AMINO]BENZOIC ACID, MANGANESE (II) ION, Methionine aminopeptidase 2 | | Authors: | Park, C.H. | | Deposit date: | 2005-02-17 | | Release date: | 2006-02-21 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
J.Med.Chem., 49, 2006
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7A16
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2ADU
 | | Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor | | Descriptor: | 4-(3-METHYLPHENYL)-1H-1,2,3-TRIAZOLE, COBALT (II) ION, Methionine aminopeptidase 2 | | Authors: | Kallander, L.S, Lu, Q, Chen, W, Tomaszek, T, Yang, G, Tew, D, Meek, T.D, Hofmann, G.A, Schulz-Pritchard, C.K, Smith, W.W, Janson, C.A, Ryan, M.D, Zhang, G.F, Johanson, K.O, Kirkpatrick, R.B, Ho, T.F, Fisher, P.W, Mattern, M.R, Johnson, R.K, Hansbury, M.J, Winkler, J.D, Ward, K.W, Veber, D.F, Thompson, S.K. | | Deposit date: | 2005-07-20 | | Release date: | 2005-09-13 | | Last modified: | 2023-08-23 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | 4-Aryl-1,2,3-triazole: A Novel Template for a Reversible Methionine Aminopeptidase 2 Inhibitor, Optimized To Inhibit Angiogenesis in Vivo
J.Med.Chem., 48, 2005
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1R58
 | | Crystal Structure of MetAP2 complexed with A357300 | | Descriptor: | MANGANESE (II) ION, Methionine aminopeptidase 2, N'-((2S,3R)-3-AMINO-2-HYDROXY-5-(ISOPROPYLSULFANYL)PENTANOYL)-N-3-CHLOROBENZOYL HYDRAZIDE | | Authors: | Sheppard, G.S, Wang, J, Kawai, M, BaMaung, N.Y, Craig, R.A, Ericken, S.A, Lynch, L, Patel, J, Yang, F, Searle, X.B, Lou, P, Park, C, Kim, K.H, Henkin, J, Lesniewski, R. | | Deposit date: | 2003-10-09 | | Release date: | 2004-10-12 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | 3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
Bioorg.Med.Chem.Lett., 14, 2004
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1KQ9
 | | Human methionine aminopeptidase type II in complex with L-methionine | | Descriptor: | METHIONINE, Methionine aminopeptidase 2, TERTIARY-BUTYL ALCOHOL, ... | | Authors: | Nonato, M.C, Widom, J, Clardy, J. | | Deposit date: | 2002-01-04 | | Release date: | 2003-12-09 | | Last modified: | 2023-08-16 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Human methionine aminopeptidase type 2 in complex with L- and D-methionine
Bioorg.Med.Chem.Lett., 16, 2006
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5LYX
 | | CRYSTAL STRUCTURE OF HUMAN METHIONINE AMINOPEPTIDASE-2 IN COMPLEX; WITH AN INHIBITOR 5-((R)-1-[1,2,4]Triazolo[1,5-a]pyrimidin-7-yl-pyrrolidin-2-ylmethoxy)-isoquinoline | | Descriptor: | 5-[[(2~{R})-1-([1,2,4]triazolo[1,5-a]pyrimidin-7-yl)pyrrolidin-2-yl]methoxy]isoquinoline, MANGANESE (II) ION, Methionine aminopeptidase 2 | | Authors: | Musil, D, Heinrich, T, Lehmann, M. | | Deposit date: | 2016-09-29 | | Release date: | 2017-08-16 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Novel reversible methionine aminopeptidase-2 (MetAP-2) inhibitors based on purine and related bicyclic templates.
Bioorg. Med. Chem. Lett., 27, 2017
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2OAZ
 | | Human Methionine Aminopeptidase-2 Complexed with SB-587094 | | Descriptor: | COBALT (II) ION, N-(2-ISOPROPYLPHENYL)-3-[(2-THIENYLMETHYL)THIO]-1H-1,2,4-TRIAZOL-5-AMINE, human Methionine Amino Peptidase 2 | | Authors: | Marino Jr, J.P, Fisher, P.W, Hofmann, G.A, Kirkpatrick, R, Janson, C.A, Johnson, R.K, Ma, C, Mattern, M, Meek, T.D, Ryan, D, Schulz, C, Smith, W.W, Tew, D.G, Tomazek Jr, T.A, Veber, D.F, Xiong, W.C, Yamamoto, Y, Yamashita, K, Yang, G, Thompson, S.K. | | Deposit date: | 2006-12-18 | | Release date: | 2007-06-19 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.
J.Med.Chem., 50, 2007
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2GA2
 | | h-MetAP2 complexed with A193400 | | Descriptor: | 5-BROMO-2-{[(4-CHLOROPHENYL)SULFONYL]AMINO}BENZOIC ACID, MANGANESE (II) ION, Methionine aminopeptidase 2 | | Authors: | Park, C. | | Deposit date: | 2006-03-07 | | Release date: | 2007-03-13 | | Last modified: | 2011-07-13 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Bioorg.Med.Chem.Lett., 16, 2006
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