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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=1337 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1338 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1339 http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1340
HGNC, UniProt https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2637, http://www.uniprot.org/uniprot/P08684 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2638, http://www.uniprot.org/uniprot/P20815 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:2640, http://www.uniprot.org/uniprot/P24462 https://www.genenames.org/data/gene‐symbol‐report/#!/hgnc_id/HGNC:17450, http://www.uniprot.org/uniprot/Q9HB55
EC number http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.14.56: 1,8‐cineole + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3041 + O2 = 2‐exo‐hydroxy‐1,8‐cineole + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3045 + H2O http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.13.97: Taurochenodeoxycholate + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3041 + O2 = taurohyocholate + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3045 + H2O Lithocholate + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3041 + O2 = hyodeoxycholate + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3045 + H2O http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.14.55: http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2510 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3041 + O2 = 3‐hydroxyquinine + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3045 + http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2448 http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.14.1 http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.14.1 http://www.genome.jp/dbget‐bin/www_bget?ec:1.14.14.1
Substrates http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2514 [http://www.ncbi.nlm.nih.gov/pubmed/3514607?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=3342 [http://www.ncbi.nlm.nih.gov/pubmed/12124305?dopt=AbstractPlus]
Inhibitors http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=10209 (pK i 7.8) [http://www.ncbi.nlm.nih.gov/pubmed/26002732?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2568 (pK i 7) [http://www.ncbi.nlm.nih.gov/pubmed/25923589?dopt=AbstractPlus], http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8804 (pK i >7) [http://www.ncbi.nlm.nih.gov/pubmed/18285471?dopt=AbstractPlus] http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=8804 (pK i 6.9) [http://www.ncbi.nlm.nih.gov/pubmed/16248836?dopt=AbstractPlus]
Comments Metabolises a vast range of xenobiotics, including antidepressants, benzodiazepines, calcium channel blockers, and chemotherapeutic agents [http://www.ncbi.nlm.nih.gov/pubmed/18473749?dopt=AbstractPlus]. The active site is plastic, with both homotropic and heterotropic cooperativity observed with some substrates [http://www.ncbi.nlm.nih.gov/pubmed/26002732?dopt=AbstractPlus]. CYP3A4 catalyses the 25‐hydroxylation of http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=2767 in liver microsomes [http://www.ncbi.nlm.nih.gov/pubmed/9931427?dopt=AbstractPlus]. CYP3A5 is expressed extrahepatically, including in the small intestine. It has overlapping substrate specificity with CYP3A4 [http://www.ncbi.nlm.nih.gov/pubmed/16430309?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12124305?dopt=AbstractPlus]. Fetal form, rarely expressed in adults. Has overlapping substrate specificity with CYP3A4 [http://www.ncbi.nlm.nih.gov/pubmed/16430309?dopt=AbstractPlus, http://www.ncbi.nlm.nih.gov/pubmed/12124305?dopt=AbstractPlus]. Fetal expression only and considered an orphan fCYP [http://www.ncbi.nlm.nih.gov/pubmed/21737533?dopt=AbstractPlus]. Testosterone may be a substrate [http://www.ncbi.nlm.nih.gov/pubmed/11160875?dopt=AbstractPlus].