7V9P
 
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7V9N
 | | Crystal structure of the lanthipeptide zinc-metallopeptidase EryP from saccharopolyspora erythraea in closed state | | 分子名称: | ACETATE ION, Alanine aminopeptidase, CALCIUM ION, ... | | 著者 | Zhao, C, Zhao, N.L, Bao, R. | | 登録日 | 2021-08-26 | | 公開日 | 2022-05-11 | | 最終更新日 | 2022-07-06 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Conformational remodeling enhances activity of lanthipeptide zinc-metallopeptidases.
Nat.Chem.Biol., 18, 2022
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7KZE
 | | Substrate-dependent divergence of leukotriene A4 hydrolase aminopeptidase activity | | 分子名称: | 1-benzyl-4-methoxybenzene, Leukotriene A-4 hydrolase, TRIETHYLENE GLYCOL, ... | | 著者 | Lee, K.H, Shim, Y, Paige, M, Noble, S.M. | | 登録日 | 2020-12-10 | | 公開日 | 2022-06-15 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.9 Å) | | 主引用文献 | 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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7LLQ
 | | Substrate-dependent divergence of leukotriene A4 hydrolase aminopeptidase activity | | 分子名称: | 1-benzyl-4-methoxybenzene, 1-{4-oxo-4-[(2S)-pyrrolidin-2-yl]butanoyl}-L-proline, Leukotriene A-4 hydrolase, ... | | 著者 | Lee, K.H, Lee, S.H, Shim, Y.M, Paige, M, Noble, S.M. | | 登録日 | 2021-02-04 | | 公開日 | 2022-06-22 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (2.85 Å) | | 主引用文献 | 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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7NSK
 | | Endoplasmic reticulum aminopeptidase 2 complexed with a hydroxamic ligand | | 分子名称: | (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, ... | | 著者 | Mpakali, A, Giastas, P, Stratikos, E. | | 登録日 | 2021-03-08 | | 公開日 | 2022-06-22 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Endoplasmic reticulum aminopeptidase 2 in complex with a phosphinic ligand
To Be Published
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7NUP
 | | Endoplasmic reticulum aminopeptidase 2 complexed with a mixed hydroxamic and sulfonyl ligand | | 分子名称: | (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, ... | | 著者 | Mpakali, A, Giastas, P, Stratikos, E. | | 登録日 | 2021-03-12 | | 公開日 | 2022-06-22 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (3.1 Å) | | 主引用文献 | Endoplasmic reticulum aminopeptidase 2 complexed with a mixed hydroxamic and sulfonyl ligand
To Be Published
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7ZYF
 | | Insulin regulated aminopeptidase (IRAP) in complex with a nanomolar alpha hydroxy beta amino acid based inhibitor. | | 分子名称: | 1,2-ETHANEDIOL, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... | | 著者 | Mpakali, A, Stratikos, E, Giastas, P, Papakyriakou, A. | | 登録日 | 2022-05-24 | | 公開日 | 2022-07-20 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (2.81 Å) | | 主引用文献 | 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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7SH0
 | | CRYSTAL STRUCTURE OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 2 (ERAP2) COMPLEX WITH A HIGHLY SELECTIVE AND POTENT SMALL MOLECULE | | 分子名称: | (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, ... | | 著者 | Li, L, Bouvier, M. | | 登録日 | 2021-10-07 | | 公開日 | 2022-07-20 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (3.2 Å) | | 主引用文献 | 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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7Z28
 | | High-resolution crystal structure of ERAP1 with bound bestatin analogue inhibitor | | 分子名称: | 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, ... | | 著者 | Giastas, P, Papakyriakou, A, Stratikos, E, Vourloumis, D. | | 登録日 | 2022-02-26 | | 公開日 | 2022-07-27 | | 最終更新日 | 2024-01-31 | | 実験手法 | X-RAY DIFFRACTION (1.55 Å) | | 主引用文献 | 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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7U0L
 | | Crystal structure of the CCoV-HuPn-2018 RBD (domain B) in complex with canine APN | | 分子名称: | 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, ... | | 著者 | Tortorici, M.A, Veesler, D, Seattle Structural Genomics Center for Infectious Disease (SSGCID) | | 登録日 | 2022-02-18 | | 公開日 | 2022-08-24 | | 最終更新日 | 2023-10-18 | | 実験手法 | X-RAY DIFFRACTION (3.3 Å) | | 主引用文献 | Structure, receptor recognition, and antigenicity of the human coronavirus CCoV-HuPn-2018 spike glycoprotein.
Cell, 185, 2022
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8EZ2
 | | Plasmodium falciparum M1 in complex with inhibitor 15ag | | 分子名称: | DIMETHYL SULFOXIDE, GLYCEROL, M1 family aminopeptidase, ... | | 著者 | Calic, P.P.S, McGowan, S, Webb, C.T. | | 登録日 | 2022-10-31 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation.
Eur.J.Med.Chem., 248, 2022
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8EX3
 | | Plasmodium falciparum M1 in complex with inhibitor 9aa | | 分子名称: | GLYCEROL, M1 family aminopeptidase, MAGNESIUM ION, ... | | 著者 | Calic, P.P.S, McGowan, S, Webb, C.T. | | 登録日 | 2022-10-24 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation.
Eur.J.Med.Chem., 248, 2022
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8EYE
 | | Plasmodium falciparum M1 in complex with inhibitor 9aj | | 分子名称: | DIMETHYL SULFOXIDE, GLYCEROL, M1 family aminopeptidase, ... | | 著者 | Calic, P.P.S, McGowan, S, Webb, C.T. | | 登録日 | 2022-10-26 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation.
Eur.J.Med.Chem., 248, 2022
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8EYD
 | | Plasmodium falciparum M1 in complex with inhibitor 15ah | | 分子名称: | GLYCEROL, M1 family aminopeptidase, N-[(1R)-1-(4-bromophenyl)-2-(hydroxyamino)-2-oxoethyl]-N~2~-(4-fluorophenyl)glycinamide, ... | | 著者 | Calic, P.P.S, McGowan, S, Webb, C.T. | | 登録日 | 2022-10-26 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (1.83 Å) | | 主引用文献 | Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation.
Eur.J.Med.Chem., 248, 2022
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8EWZ
 | | Plasmodium falciparum M1 in complex with inhibitor 9c | | 分子名称: | (2R)-2-(cyclopentylcarbamamido)-N-hydroxy-2-(3',4',5'-trifluoro[1,1'-biphenyl]-4-yl)acetamide, DIMETHYL SULFOXIDE, GLYCEROL, ... | | 著者 | Calic, P.P.S, McGowan, S, Webb, C.T. | | 登録日 | 2022-10-24 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (1.75 Å) | | 主引用文献 | Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation.
Eur.J.Med.Chem., 248, 2022
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8EYF
 | | Plasmodium falciparum M1 in complex with inhibitor 15aa | | 分子名称: | DIMETHYL SULFOXIDE, GLYCEROL, M1 family aminopeptidase, ... | | 著者 | Calic, P.P.S, McGowan, S, Webb, C.T. | | 登録日 | 2022-10-26 | | 公開日 | 2023-01-18 | | 最終更新日 | 2023-10-25 | | 実験手法 | X-RAY DIFFRACTION (1.9 Å) | | 主引用文献 | Structure-based development of potent Plasmodium falciparum M1 and M17 aminopeptidase selective and dual inhibitors via S1'-region optimisation.
Eur.J.Med.Chem., 248, 2022
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8AVA
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8AWH
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8SW0
 | | Puromycin sensitive aminopeptidase | | 分子名称: | 1,4-DIETHYLENE DIOXIDE, 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, Puromycin-sensitive aminopeptidase, ... | | 著者 | Rodgers, D.W, Sampath, S. | | 登録日 | 2023-05-17 | | 公開日 | 2023-07-26 | | 実験手法 | X-RAY DIFFRACTION (2.301 Å) | | 主引用文献 | Structure of puromycin-sensitive aminopeptidase and polyglutamine binding.
Plos One, 18, 2023
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8SW1
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8QPN
 | | LTA4 hydrolase in complex with compound 6(S) | | 分子名称: | (2S)-2-azanyl-3-[5-[4-(5-chloranyl-3-fluoranyl-pyridin-2-yl)oxyphenyl]-1,2,3,4-tetrazol-2-yl]propan-1-ol, ACETATE ION, IMIDAZOLE, ... | | 著者 | Srinivas, H. | | 登録日 | 2023-10-02 | | 公開日 | 2023-12-06 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2 Å) | | 主引用文献 | Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase.
J.Med.Chem., 66, 2023
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8QOW
 | | LTA4 hydrolase in complex with compound 2(S) | | 分子名称: | (2~{S})-2-azanyl-3-[3-[4-[3-fluoranyl-5-(1~{H}-pyrazol-5-yl)pyridin-2-yl]oxyphenyl]pyrazol-1-yl]propan-1-ol, ACETATE ION, IMIDAZOLE, ... | | 著者 | Srinivas, H. | | 登録日 | 2023-09-29 | | 公開日 | 2023-12-06 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (2.35 Å) | | 主引用文献 | Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase.
J.Med.Chem., 66, 2023
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8QQ4
 | | LTA4 hydrolase in complex with compound 6(R) | | 分子名称: | (2R)-2-azanyl-3-[5-[4-(5-chloranyl-3-fluoranyl-pyridin-2-yl)oxyphenyl]-1,2,3,4-tetrazol-2-yl]propan-1-ol, ACETATE ION, IMIDAZOLE, ... | | 著者 | Srinivas, H. | | 登録日 | 2023-10-03 | | 公開日 | 2023-12-06 | | 最終更新日 | 2023-12-27 | | 実験手法 | X-RAY DIFFRACTION (1.6 Å) | | 主引用文献 | Discovery of Amino Alcohols as Highly Potent, Selective, and Orally Efficacious Inhibitors of Leukotriene A4 Hydrolase.
J.Med.Chem., 66, 2023
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8CGP
 | | Insulin regulated aminopeptidase (IRAP) in complex with an allosteric aryl sulfonamide inhibitor | | 分子名称: | 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, ... | | 著者 | Mpakali, A, Stratikos, E, Giastas, P. | | 登録日 | 2023-02-06 | | 公開日 | 2024-01-31 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (2.62 Å) | | 主引用文献 | Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase.
J.Mol.Biol., 436, 2024
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8CGW
 | | Insulin-regulated aminopeptidase (IRAP) in complex with an allosteric benzopyran-based inhibitor | | 分子名称: | 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, ... | | 著者 | Mpakali, A, Stratikos, E, Giastas, P. | | 登録日 | 2023-02-06 | | 公開日 | 2024-01-31 | | 最終更新日 | 2024-02-14 | | 実験手法 | X-RAY DIFFRACTION (3.03 Å) | | 主引用文献 | Mechanisms of Allosteric Inhibition of Insulin-Regulated Aminopeptidase.
J.Mol.Biol., 436, 2024
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