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. 2019 Nov 11;176(Suppl 1):S297–S396. doi: 10.1111/bph.14752
Nomenclature http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1240 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2527 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1243 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2486
Common abbreviation TAT DBH
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:8582, http://www.uniprot.org/uniprot/P00439 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:11573, http://www.uniprot.org/uniprot/P17735 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:11782, http://www.uniprot.org/uniprot/P07101 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2689, http://www.uniprot.org/uniprot/P09172
EC number http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.16.1: http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3313 + O2 ‐> http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4791 http://www.genome.jp/dbget‐bin/www_bget?ec:2.6.1.5: http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4791 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3636 ‐> http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6629 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1369 http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.16.2: http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4791 + O2 ‐> http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3639 http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.17.1: http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=940 + O2 = http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=505 + H2O
Endogenous substrates http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3313 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4791
Products http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4791 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3639
Cofactors http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5276 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5249 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5276, Fe2+ http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4164, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=4781
Endogenous activators Protein kinase A‐mediated phosphorylation (Rat) [http://www.ncbi.nlm.nih.gov/pubmed/182695?dopt=AbstractPlus] Protein kinase A‐mediated phosphorylation [http://www.ncbi.nlm.nih.gov/pubmed/33381?dopt=AbstractPlus]
Selective inhibitors http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5093 [http://www.ncbi.nlm.nih.gov/pubmed/944951?dopt=AbstractPlus] – Rat, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5240 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5095, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5114, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=5117, http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6956 http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6630 (pIC50 8) [http://www.ncbi.nlm.nih.gov/pubmed/9283721?dopt=AbstractPlus]
Comments PAH is an iron bound homodimer or ‐tetramer from the same structural family as tyrosine 3‐monooxygenase and the tryptophan hydroxylases. Deficiency or loss‐of‐function of PAH is associated with http://omim.org/entry/612349 Tyrosine may also be metabolized in the liver by tyrosine transaminase to generate http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=6629, which can be further metabolized to homogentisic acid. TAT is a homodimer, where loss‐of‐function mutations are associated with http://omim.org/entry/276600. TH is a homotetramer, which is inhibited by dopamine and other catecholamines in a physiological negative feedback pathway [http://www.ncbi.nlm.nih.gov/pubmed/21176768?dopt=AbstractPlus]. DBH is a homotetramer. A protein structurally‐related to DBH (http://www.genenames.org/data/hgnc_data.php?hgnc_id=21063, http://www.uniprot.org/uniprot/Q6UVY6) has been described and for which a function has yet to be identified [http://www.ncbi.nlm.nih.gov/pubmed/9751809?dopt=AbstractPlus].