4Q6R
 
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6END
 | | LTA4 hydrolase in complex with Compound15 | | Descriptor: | 4-([1,3]thiazolo[4,5-b]pyridin-2-yloxy)benzaldehyde, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2017-10-04 | | Release date: | 2017-12-13 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (2.24 Å) | | Cite: | Feasibility and physiological relevance of designing highly potent aminopeptidase-sparing leukotriene A4 hydrolase inhibitors.
Sci Rep, 7, 2017
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8AYH
 | | Structure of Complement C5 in Complex with small molecule inhibitor and CVF | | Descriptor: | 5-methoxy-2-[[(1~{S})-1-(2-methoxyphenyl)ethyl]carbamoylamino]-4-(4-methylpentoxy)benzoic acid, Cobra venom factor, Complement C5 alpha chain, ... | | Authors: | Srinivas, H. | | Deposit date: | 2022-09-02 | | Release date: | 2022-12-21 | | Last modified: | 2024-10-09 | | Method: | ELECTRON MICROSCOPY (3.35 Å) | | Cite: | A small-molecule inhibitor of C5 complement protein.
Nat.Chem.Biol., 15, 2019
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6ENC
 | | LTA4 hydrolase in complex with Compound11 | | Descriptor: | 1-[[4-(1,3-benzothiazol-2-yloxy)phenyl]methyl]piperidine-4-carboxylic acid, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2017-10-04 | | Release date: | 2017-12-13 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.95 Å) | | Cite: | Feasibility and physiological relevance of designing highly potent aminopeptidase-sparing leukotriene A4 hydrolase inhibitors.
Sci Rep, 7, 2017
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6ENB
 | | LTA4 hydrolase (E297Q) mutant in complex with Pro-Gly-Pro peptide | | Descriptor: | ACETATE ION, IMIDAZOLE, Leukotriene A-4 hydrolase, ... | | Authors: | Srinivas, H. | | Deposit date: | 2017-10-04 | | Release date: | 2017-12-13 | | Last modified: | 2024-05-08 | | Method: | X-RAY DIFFRACTION (1.84 Å) | | Cite: | Feasibility and physiological relevance of designing highly potent aminopeptidase-sparing leukotriene A4 hydrolase inhibitors.
Sci Rep, 7, 2017
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8QQ4
 | | LTA4 hydrolase in complex with compound 6(R) | | Descriptor: | (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, ... | | Authors: | Srinivas, H. | | Deposit date: | 2023-10-03 | | Release date: | 2023-12-06 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (1.6 Å) | | Cite: | 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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8QPN
 | | LTA4 hydrolase in complex with compound 6(S) | | Descriptor: | (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, ... | | Authors: | Srinivas, H. | | Deposit date: | 2023-10-02 | | Release date: | 2023-12-06 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2 Å) | | Cite: | 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) | | Descriptor: | (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, ... | | Authors: | Srinivas, H. | | Deposit date: | 2023-09-29 | | Release date: | 2023-12-06 | | Last modified: | 2023-12-27 | | Method: | X-RAY DIFFRACTION (2.35 Å) | | Cite: | 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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8RX9
 | | LTA4 hydrolase in complex with compound3 | | Descriptor: | 1-[[5-[5-(1~{H}-pyrazol-5-yl)pyridin-2-yl]oxypyridin-2-yl]methyl]piperidin-4-ol, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2024-02-06 | | Release date: | 2024-03-20 | | Last modified: | 2024-04-10 | | Method: | X-RAY DIFFRACTION (2.9 Å) | | Cite: | Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor.
J.Med.Chem., 67, 2024
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8RX7
 | | LTA4 hydrolase in complex with compound2 | | Descriptor: | 5-(4-phenoxyphenyl)-1~{H}-imidazole, ACETATE ION, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2024-02-06 | | Release date: | 2024-03-20 | | Last modified: | 2024-04-10 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor.
J.Med.Chem., 67, 2024
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8RX3
 | | LTA4 hydrolase in complex with CTX-4430 | | Descriptor: | ACETATE ION, Acebilustat, IMIDAZOLE, ... | | Authors: | Srinivas, H. | | Deposit date: | 2024-02-06 | | Release date: | 2024-03-20 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Structure-Guided Elaboration of a Fragment-Like Hit into an Orally Efficacious Leukotriene A4 Hydrolase Inhibitor.
J.Med.Chem., 67, 2024
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6SJ7
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6GG0
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6TD5
 | | Leishmania tarentolae proteasome 20S subunit complexed with LXE408 and bortezomib | | Descriptor: | N-[(1R)-1-(DIHYDROXYBORYL)-3-METHYLBUTYL]-N-(PYRAZIN-2-YLCARBONYL)-L-PHENYLALANINAMIDE, Proteasome endopeptidase complex, Proteasome subunit alpha type, ... | | Authors: | Srinivas, H. | | Deposit date: | 2019-11-07 | | Release date: | 2020-08-26 | | Last modified: | 2020-10-21 | | Method: | ELECTRON MICROSCOPY (3.2 Å) | | Cite: | Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
J.Med.Chem., 63, 2020
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6TCZ
 | | Leishmania tarentolae proteasome 20S subunit complexed with LXE408 | | Descriptor: | Proteasome endopeptidase complex, Proteasome subunit alpha type, Proteasome subunit beta, ... | | Authors: | Srinivas, H. | | Deposit date: | 2019-11-07 | | Release date: | 2020-08-26 | | Last modified: | 2024-05-22 | | Method: | ELECTRON MICROSCOPY (3.4 Å) | | Cite: | Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases.
J.Med.Chem., 63, 2020
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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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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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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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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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7ZYJ
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6UD7
 | | Crystal structure of full-length human DCAF15-DDB1(deltaBPB)-DDA1-RBM39 in complex with indisulam | | Descriptor: | DDB1- and CUL4-associated factor 15, DET1- and DDB1-associated protein 1, DNA damage-binding protein 1,DNA damage-binding protein 1, ... | | Authors: | Bussiere, D.E, Shu, W, Xie, L, Knapp, M. | | Deposit date: | 2019-09-18 | | Release date: | 2019-12-18 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (2.3 Å) | | Cite: | Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex.
Nat.Chem.Biol., 16, 2020
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6UE5
 | | Crystal structure of full-length human DCAF15-DDB1-deltaPBP-DDA1-RBM39 in complex with 4-(aminomethyl)-N-(3-cyano-4-methyl-1H-indol-7-yl)benzenesulfonamide | | Descriptor: | 4-(aminomethyl)-N-(3-cyano-4-methyl-1H-indol-7-yl)benzene-1-sulfonamide, DDB1- and CUL4-associated factor 15, DET1- and DDB1-associated protein 1, ... | | Authors: | Knapp, M.S, Shu, W, Xie, L, Bussiere, D.E. | | Deposit date: | 2019-09-20 | | Release date: | 2019-12-18 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.61 Å) | | Cite: | Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex.
Nat.Chem.Biol., 16, 2020
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