Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T84634
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| Former ID |
TTDC00232
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| Target Name |
Cytochrome P450 26
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| Gene Name |
CYP26A1
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| Synonyms |
Cytochrome P450RAI; HP450RAI; P450 retinoic acid-inactivating 1; P450RAI; Retinoic acid 4-hydroxylase; Retinoic acid inducible enzyme; Retinoic acid-metabolizing cytochrome; CYP26A1
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| Target Type |
Clinical Trial
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| 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.
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| BioChemical Class |
Oxidoreductases acting on paired donors
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| Target Validation |
T84634
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| UniProt ID | |||||
| EC Number |
EC 1.14.-.-
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| Sequence |
MGLPALLASALCTFVLPLLLFLAAIKLWDLYCVSGRDRSCALPLPPGTMGFPFFGETLQM
VLQRRKFLQMKRRKYGFIYKTHLFGRPTVRVMGADNVRRILLGEHRLVSVHWPASVRTIL GSGCLSNLHDSSHKQRKKVIMRAFSREALECYVPVITEEVGSSLEQWLSCGERGLLVYPE VKRLMFRIAMRILLGCEPQLAGDGDSEQQLVEAFEEMTRNLFSLPIDVPFSGLYRGMKAR NLIHARIEQNIRAKICGLRASEAGQGCKDALQLLIEHSWERGERLDMQALKQSSTELLFG GHETTASAATSLITYLGLYPHVLQKVREELKSKGLLCKSNQDNKLDMEILEQLKYIGCVI KETLRLNPPVPGGFRVALKTFELNGYQIPKGWNVIYSICDTHDVAEIFTNKEEFNPDRFM LPHPEDASRFSFIPFGGGLRSCVGKEFAKILLKIFTVELARHCDWQLLNGPPTMKTSPTV YPVDNLPARFTHFHGEI |
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| Drugs and Mode of Action | |||||
| Drug(s) | LIAROZOLE | Drug Info | Phase 2/3 | Dermatological disease | [1], [2] |
| Rambazole | Drug Info | Phase 2 | Psoriasis | [3] | |
| Inhibitor | 4-((+/-)-(1H-imidazol-1-yl)-(E)-methylretinoate | Drug Info | [4] | ||
| 4-((+/-)-(1H-imidazol-1-yl)-(E)-retinoic acid | Drug Info | [4] | |||
| LIAROZOLE | Drug Info | [5] | |||
| Rambazole | Drug Info | [3] | |||
| 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 1 | (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 2 | ClinicalTrials.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 3 | Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. | ||||
| REF 4 | J 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 5 | Bioorg 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. | ||||
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