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Literature summary for 1.14.16.4 extracted from

  • Petrassi, M.; Barber, R.; Be, C.; Beach, S.; Cox, B.; DSouza, A.M.; Duggan, N.; Hussey, M.; Fox, R.; Hunt, P.; Jarai, G.; Kosaka, T.; Oakley, P.; Patel, V.; Press, N.; Rowlands, D.; Scheufler, C.; Schmidt, O.; Srinivas, H.; Turner, M.; Turner, R.; Westwick, J.; Wolfreys, A.; Pathan, N.; Watson, S.; Thomas, M.
    Identification of a novel allosteric inhibitory site on tryptophan hydroxylase 1 enabling unprecedented selectivity over all related hydroxylases (2017), Front. Pharmacol., 8, 240 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.14.16.4

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21 Rosetta (DE3) cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-Chlorophenylalanine
-
 Homo sapiens
LP533401
-
 Homo sapiens
NVS-TPH120
-
 Homo sapiens
NVS-TPH146
-
 Homo sapiens
NVS-TPH176
-
 Homo sapiens
NVS-TPH180
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-tryptophan + tetrahydrobiopterin + O2 Homo sapiens
-
 5-hydroxy-L-tryptophan + 4a-hydroxytetrahydrobiopterin
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
Ni-NTA column chromatography and Superdex SPX200 gel filtration Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
BON-1 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-tryptophan + tetrahydrobiopterin + O2
-
 Homo sapiens 5-hydroxy-L-tryptophan + 4a-hydroxytetrahydrobiopterin
-
 ?

Synonyms

Synonyms Comment Organism
TPH-1 isoform Homo sapiens
TPH-2 isoform Homo sapiens
tryptophan hydroxylase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000021
-
 isoform TPH-1, at pH 7.0 and 25°C Homo sapiens NVS-TPH120
0.000039
-
 isoform TPH-1, at pH 7.0 and 25°C Homo sapiens NVS-TPH180
0.000103
-
 isoform TPH-1, at pH 7.0 and 25°C Homo sapiens LP533401
0.000103
-
 isoform TPH-2, at pH 7.0 and 25°C Homo sapiens LP533401
0.000174
-
 isoform TPH-1, at pH 7.0 and 25°C Homo sapiens NVS-TPH176
0.000271
-
 isoform TPH-1, at pH 7.0 and 25°C Homo sapiens NVS-TPH146
0.00155
-
 isoform TPH-2, at pH 7.0 and 25°C Homo sapiens 4-Chlorophenylalanine
0.00449
-
 isoform TPH-1, at pH 7.0 and 25°C Homo sapiens 4-Chlorophenylalanine
0.01
-
 IC50 above 0.01 mM, isoform TPH-2, at pH 7.0 and 25°C Homo sapiens NVS-TPH146
0.01
-
 IC50 above 0.01 mM, isoform TPH-2, at pH 7.0 and 25°C Homo sapiens NVS-TPH176
0.01
-
 IC50 above 0.01 mM, isoform TPH-2, at pH 7.0 and 25°C Homo sapiens NVS-TPH180
0.01
-
 IC50 above 0.01 mM, isoform TPH-2, at pH 7.0 and 25°C Homo sapiens NVS-TPH120