3TK2
 
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3E2T
 | | The catalytic domain of chicken tryptophan hydroxylase 1 with bound tryptophan | | Descriptor: | FE (III) ION, IMIDAZOLE, SULFATE ION, ... | | Authors: | Windahl, M.S, Petersen, C.R, Christensen, H.E.C, Harris, P. | | Deposit date: | 2008-08-06 | | Release date: | 2008-11-04 | | Last modified: | 2023-11-01 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Crystal structure of tryptophan hydroxylase with bound amino acid substrate
Biochemistry, 47, 2008
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4Q3Y
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4Q3Z
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4Q3W
 | | Crystal structure of C. violaceum phenylalanine hydroxylase D139E mutation | | Descriptor: | 1,2-ETHANEDIOL, COBALT (II) ION, Phenylalanine-4-hydroxylase | | Authors: | Ronau, J.A, Abu-Omar, M.M, Das, C. | | Deposit date: | 2014-04-12 | | Release date: | 2015-02-18 | | Last modified: | 2023-09-20 | | Method: | X-RAY DIFFRACTION (1.4 Å) | | Cite: | A conserved acidic residue in phenylalanine hydroxylase contributes to cofactor affinity and catalysis.
Biochemistry, 53, 2014
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4Q3X
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6ZZU
 | | Partial structure of the substrate-free tyrosine hydroxylase (apo-TH). | | Descriptor: | FE (III) ION, Tyrosine 3-monooxygenase | | Authors: | Bueno-Carrasco, M.T, Cuellar, J, Santiago, C, Valpuesta, J.M, Martinez, A, Flydal, M.I. | | Deposit date: | 2020-08-05 | | Release date: | 2021-11-17 | | Last modified: | 2024-07-10 | | Method: | ELECTRON MICROSCOPY (3.5 Å) | | Cite: | Structural mechanism for tyrosine hydroxylase inhibition by dopamine and reactivation by Ser40 phosphorylation.
Nat Commun, 13, 2022
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3HFB
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3HF6
 | | Crystal structure of human tryptophan hydroxylase type 1 with bound LP-521834 and FE | | Descriptor: | 4-(4-amino-6-{[(1R)-1-naphthalen-2-ylethyl]amino}-1,3,5-triazin-2-yl)-L-phenylalanine, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Tari, L.W, Swanson, R.V, Hunter, M.J. | | Deposit date: | 2009-05-11 | | Release date: | 2009-11-24 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.8 Å) | | Cite: | Mechanism of Inhibition of Novel Tryptophan Hydroxylase Inhibitors Revealed by Co-crystal Structures and Kinetic Analysis
Curr Chem Genomics, 4, 2010
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3HF8
 | | Crystal structure of human tryoptophan hydroxylase type 1 with bound LP-533401 and Fe | | Descriptor: | 4-{2-amino-6-[(1R)-2,2,2-trifluoro-1-(3'-fluorobiphenyl-4-yl)ethoxy]pyrimidin-4-yl}-L-phenylalanine, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Tari, L.W, Swanson, R.V, Hunter, M.J. | | Deposit date: | 2009-05-11 | | Release date: | 2010-04-21 | | Last modified: | 2024-02-21 | | Method: | X-RAY DIFFRACTION (1.85 Å) | | Cite: | Mechanism of Inhibition of Novel Tryptophan Hydroxylase Inhibitors Revealed by Co-crystal Structures and Kinetic Analysis.
Curr Chem Genomics, 4, 2010
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5J6D
 | | Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors | | Descriptor: | 2-AMINO-2-HYDROXYMETHYL-PROPANE-1,3-DIOL, 4-[(N-{[2-(3-methoxyphenoxy)-6-(piperidin-1-yl)phenyl]methyl}carbamimidoyl)carbamoyl]-L-phenylalanine, FE (III) ION, ... | | Authors: | Stein, A.J, Goldberg, D.R, De Lombaert, S. | | Deposit date: | 2016-04-04 | | Release date: | 2016-05-25 | | Last modified: | 2023-09-27 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors.
Bioorg.Med.Chem.Lett., 26, 2016
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5JK8
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5JK6
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5JK5
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5L01
 | | Tryptophan 5-hydroxylase in complex with inhibitor (3~{S})-8-[2-azanyl-6-[(1~{R})-1-(4-chloranyl-2-phenyl-phenyl)-2,2,2-tris(fluoranyl)ethoxy]pyrimidin-4-yl]-2,8-diazaspiro[4.5]decane-3-carboxylic acid | | Descriptor: | (3~{S})-8-[2-azanyl-6-[(1~{R})-1-(4-chloranyl-2-phenyl-phenyl)-2,2,2-tris(fluoranyl)ethoxy]pyrimidin-4-yl]-2,8-diazaspiro[4.5]decane-3-carboxylic acid, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Stein, A.J, Goldberg, D.R, De Lombaert, S, Holt, M.C. | | Deposit date: | 2016-07-26 | | Release date: | 2017-01-25 | | Last modified: | 2023-10-04 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors.
Bioorg. Med. Chem. Lett., 27, 2017
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7WIY
 | | Cryo-EM structure of human TPH2 tetramer | | Descriptor: | FE (III) ION, IMIDAZOLE, Tryptophan 5-hydroxylase 2 | | Authors: | Zhu, K.F, Liu, C, Zhang, H.W, Wang, D.P. | | Deposit date: | 2022-01-05 | | Release date: | 2022-10-05 | | Last modified: | 2024-06-26 | | Method: | ELECTRON MICROSCOPY (3.09 Å) | | Cite: | Cryo-EM Structure and Activator Screening of Human Tryptophan Hydroxylase 2.
Front Pharmacol, 13, 2022
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8CJL
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor TPT-004 | | Descriptor: | 3-ethyl-8-[(2-methyl-5~{H}-imidazo[2,1-b][1,3]thiazol-6-yl)methyl]-7-(oxetan-3-ylmethyl)purine-2,6-dione, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.83 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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8CJO
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-06-004 | | Descriptor: | 1-[(3~{S})-3-(4-chloranyl-2-fluoranyl-phenyl)-1,4,8-triazatricyclo[7.4.0.0^{2,7}]trideca-2(7),8-dien-4-yl]-2-(2-ethyl-6-methyl-pyridin-3-yl)oxy-ethanone, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.86633706 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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8CJM
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-07-047 | | Descriptor: | 7-(cyclobutylmethyl)-3-ethyl-8-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-2-ylmethyl)purine-2,6-dione, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.9 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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8CJK
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-06-098 | | Descriptor: | 3-ethyl-8-[(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)methyl]-7-[[4-(1-methylpyrazol-3-yl)phenyl]methyl]purine-2,6-dione, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.45914972 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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8CJI
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-07-052 | | Descriptor: | FE (III) ION, Tryptophan 5-hydroxylase 1, methyl (2~{S})-2-azanyl-3-[[3-[[3-ethyl-2,6-bis(oxidanylidene)-8-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-2-ylmethyl)purin-7-yl]methyl]phenyl]carbonylamino]propanoate | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.65 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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8CJJ
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-06-057 | | Descriptor: | 3-ethyl-7-(phenylmethyl)-8-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-2-ylmethyl)purine-2,6-dione, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.66415656 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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8CJN
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor KM-06-070 | | Descriptor: | 3-ethyl-7-[(4-phenylphenyl)methyl]-8-(5,6,7,8-tetrahydroimidazo[1,2-a]pyridin-2-ylmethyl)purine-2,6-dione, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2023-02-13 | | Release date: | 2024-01-10 | | Method: | X-RAY DIFFRACTION (1.68080938 Å) | | Cite: | Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 66, 2023
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7ZIH
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor AG-01-128 | | Descriptor: | 8-(1~{H}-benzimidazol-2-ylmethyl)-3-ethyl-7-(phenylmethyl)purine-2,6-dione, DI(HYDROXYETHYL)ETHER, FE (III) ION, ... | | Authors: | Schuetz, A, Gogolin, A, Pfeifer, J, Mallow, K, Nazare, M, Specker, E, Heinemann, U. | | Deposit date: | 2022-04-08 | | Release date: | 2022-09-07 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (1.46890831 Å) | | Cite: | Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 65, 2022
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7ZIK
 | | Crystal structure of human tryptophan hydroxylase 1 in complex with inhibitor LP533401 | | Descriptor: | (2~{R})-2-azanyl-3-[4-[2-azanyl-6-[(1~{R})-1-[4-chloranyl-2-(3-methylpyrazol-1-yl)phenyl]-2,2,2-tris(fluoranyl)ethoxy]pyrimidin-4-yl]phenyl]propanoic acid, FE (III) ION, Tryptophan 5-hydroxylase 1 | | Authors: | Schuetz, A, Heinemann, U. | | Deposit date: | 2022-04-08 | | Release date: | 2022-09-07 | | Last modified: | 2024-01-31 | | Method: | X-RAY DIFFRACTION (2.58925915 Å) | | Cite: | Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.
J.Med.Chem., 65, 2022
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