Target Information

Target General Infomation
Target ID
T84634
Former ID
TTDC00232
Target Name
Cytochrome P450 26
Gene Name
CYP26A1
Synonyms
Cytochrome P450RAI; HP450RAI; P450 retinoic acid-inactivating 1; P450RAI; Retinoic acid 4-hydroxylase; Retinoic acid inducible enzyme; Retinoic acid-metabolizing cytochrome; CYP26A1
Target Type
Clinical Trial
Disease Dermatological disease [ICD10: L00-L99]
Psoriasis [ICD9: 696; ICD10: L40]
Function
Plays a key role in retinoic acid metabolism. Acts on retinoids, including all-trans-retinoic acid (RA) and its stereoisomer 9-cis-RA. Capable of both 4-hydroxylation and 18- hydroxylation. Responsible for generation of several hydroxylated forms of RA, including 4-OH-RA, 4-oxo-RA and 18-OH-RA.
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T84634
UniProt ID
O43174
EC Number
EC 1.14.-.-
Sequence
MGLPALLASALCTFVLPLLLFLAAIKLWDLYCVSGRDRSCALPLPPGTMGFPFFGETLQM
VLQRRKFLQMKRRKYGFIYKTHLFGRPTVRVMGADNVRRILLGEHRLVSVHWPASVRTIL
GSGCLSNLHDSSHKQRKKVIMRAFSREALECYVPVITEEVGSSLEQWLSCGERGLLVYPE
VKRLMFRIAMRILLGCEPQLAGDGDSEQQLVEAFEEMTRNLFSLPIDVPFSGLYRGMKAR
NLIHARIEQNIRAKICGLRASEAGQGCKDALQLLIEHSWERGERLDMQALKQSSTELLFG
GHETTASAATSLITYLGLYPHVLQKVREELKSKGLLCKSNQDNKLDMEILEQLKYIGCVI
KETLRLNPPVPGGFRVALKTFELNGYQIPKGWNVIYSICDTHDVAEIFTNKEEFNPDRFM
LPHPEDASRFSFIPFGGGLRSCVGKEFAKILLKIFTVELARHCDWQLLNGPPTMKTSPTV
YPVDNLPARFTHFHGEI
Drugs and Mode of Action
Drug(s) LIAROZOLE Drug Info Phase 2/3 Dermatological disease [468265], [521791]
Rambazole Drug Info Phase 2 Psoriasis [537117]
Inhibitor 4-((+/-)-(1H-imidazol-1-yl)-(E)-methylretinoate Drug Info [527351]
4-((+/-)-(1H-imidazol-1-yl)-(E)-retinoic acid Drug Info [527351]
LIAROZOLE Drug Info [529651]
Rambazole Drug Info [537117]
Pathways
KEGG Pathway Retinol metabolism
Metabolic pathways
PathWhiz Pathway Retinol Metabolism
WikiPathways Vitamin A and Carotenoid Metabolism
Metapathway biotransformation
Oxidation by Cytochrome P450
Nuclear Receptors in Lipid Metabolism and Toxicity
Adipogenesis
Phase 1 - Functionalization of compounds
References
Ref 468265(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5210).
Ref 521791ClinicalTrials.gov (NCT00282724) Efficacy and Safety of Two Doses of Liarozole vs. Placebo for the Treatment of Lamellar Ichthyosis. U.S. National Institutes of Health.
Ref 537117Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.
Ref 527351J Med Chem. 2004 Dec 30;47(27):6716-29.Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.
Ref 529651Bioorg Med Chem. 2008 Sep 1;16(17):8301-13. Epub 2007 Jun 29.Novel azolyl-(phenylmethyl)]aryl/heteroarylamines: potent CYP26 inhibitors and enhancers of all-trans retinoic acid activity in neuroblastoma cells.
Ref 537117Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63.

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