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Amino acid hydroxylases C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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The amino acid hydroxylases (monooxygenases), EC.1.14.16.-, are iron-containing enzymes which utilise molecular oxygen and sapropterin as co-substrate and co-factor, respectively. In humans, as well as in other mammals, there are two distinct L-Tryptophan hydroxylase 2 genes. In humans, these genes are located on chromosomes 11 and 12 and encode two different homologous enzymes, TPH1 and TPH2.

Enzymes

1241
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Targets of relevance to immunopharmacology are highlighted in blue

L-Phenylalanine hydroxylase C Show summary » More detailed page go icon to follow link

L-Tyrosine hydroxylase C Show summary » More detailed page go icon to follow link

L-Tryptophan hydroxylase 1 C Show summary »


Target Id 1241
Nomenclature L-Tryptophan hydroxylase 1
Previous and unofficial names tryptophan 5-monooxygenase | tryptophan 5-hydroxylase 1 | TPH | TPRH | Tryptophan 5-monooxygenase 1
Genes TPH1 (Hs), Tph1 (Mm), Tph1 (Rn)
Ensembl ID ENSG00000129167 (Hs), ENSMUSG00000040046 (Mm), ENSRNOG00000011672 (Rn)
UniProtKB AC P17752 (Hs), P17532 (Mm), P09810 (Rn)
EC number
1.14.16.4
Endogenous activators Protein kinase A-mediated phosphorylation  [7]
Endogenous substrates
L-tryptophan
Products
5-hydroxy-L-tryptophan
Inhibitors
TPT-004 pKd 8.5 [10]
rodatristat pIC50 7.5 [4]
compound 23a [PMID: 33417443] pIC50 7.4 [2]
telotristat ethyl pIC50 7.2 [2,8]
TPT-004 pIC50 7.1 [10]
LP533401 pIC50 6.2 [2]
Selective inhibitors
fenfluramine
α-propyldopacetamide
6-fluorotryptophan [9]
fenclonine

L-Tryptophan hydroxylase 2 C Show summary »

Further reading

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References

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How to cite this family page

Database page citation:

Amino acid hydroxylases. Accessed on 22/05/2024. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=249.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: Enzymes. Br J Pharmacol. 180 Suppl 2:S289-373.