3HF6
Crystal structure of human tryptophan hydroxylase type 1 with bound LP-521834 and FE
Summary for 3HF6
| Entry DOI | 10.2210/pdb3hf6/pdb |
| Descriptor | Tryptophan 5-hydroxylase 1, FE (III) ION, 4-(4-amino-6-{[(1R)-1-naphthalen-2-ylethyl]amino}-1,3,5-triazin-2-yl)-L-phenylalanine, ... (4 entities in total) |
| Functional Keywords | tryptophan 5-hydroxylase 1, alternative splicing, iron, metal-binding, monooxygenase, oxidoreductase, phosphoprotein, serotonin biosynthesis |
| Biological source | Homo sapiens (human) |
| Total number of polymer chains | 1 |
| Total formula weight | 33772.24 |
| Authors | Tari, L.W.,Swanson, R.V.,Hunter, M.J. (deposition date: 2009-05-11, release date: 2009-11-24, Last modification date: 2024-02-21) |
| Primary citation | Cianchetta, G.,Stouch, T.,Yu, W.,Shi, Z.-C.,Tari, L.W.,Swanson, R.V.,Hunter, M.J.,Hoffman, I.D.,Liu, Q. Mechanism of Inhibition of Novel Tryptophan Hydroxylase Inhibitors Revealed by Co-crystal Structures and Kinetic Analysis Curr Chem Genomics, 4:19-26, 2010 Cited by PubMed Abstract: Tryptophan hydroxylase (TPH) is a key enzyme in the synthesis of serotonin. As a neurotransmitter, serotonin plays important physiological roles both peripherally and centrally. Here we describe the discovery of substituted triazines as a novel class of tryptophan hydroxylase inhibitors. This class of TPH inhibitors can selectively reduce serotonin levels in murine intestine after oral administration without affecting levels in the brain. These TPH inhibitors may provide novel treatments for gastrointestinal disorders associated with dysregulation of the serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome. PubMed: 19631532DOI: 10.2174/1875397301004010019 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.8 Å) |
Structure validation
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