Page last updated: 2024-08-07 12:43:32
Cytochrome P450 26A1
A cytochrome P450 26A1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43174]
Synonyms
EC 1.14.13.-;
Cytochrome P450 retinoic acid-inactivating 1;
Cytochrome P450RAI;
hP450RAI;
Retinoic acid 4-hydroxylase;
Retinoic acid-metabolizing cytochrome
Research
Bioassay Publications (9)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (44.44) | 29.6817 |
| 2010's | 5 (55.56) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (5)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| ketoconazole | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| liarozole | Homo sapiens (human) | IC50 | 3.2900 | 8 | 8 |
| bexarotene | Homo sapiens (human) | IC50 | 13.5000 | 1 | 1 |
| sr 11237 | Homo sapiens (human) | IC50 | 7.8000 | 1 | 1 |
| r 115866 | Homo sapiens (human) | IC50 | 0.0051 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| liarozole | Homo sapiens (human) | EC50 | 7.0000 | 1 | 1 |
| r 115866 | Homo sapiens (human) | EC50 | 0.0050 | 1 | 1 |
Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Synthesis and biological evaluation of 3-phenyl-3-aryl carboxamido propanoic acid derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26A1).Bioorganic & medicinal chemistry, , Mar-15, Volume: 23, Issue:6, 2015
Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors.Bioorganic & medicinal chemistry, , Oct-15, Volume: 23, Issue:20, 2015
Synthesis and biological evaluation of 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-[4-(naphthalen-2-ylamino)phenyl]propyl derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26).Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26): synthesis and biological evaluation of imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Design and synthesis of substituted imidazole and triazole N-phenylbenzo[d]oxazolamine inhibitors of retinoic acid metabolizing enzyme CYP26.Journal of enzyme inhibition and medicinal chemistry, , Volume: 24, Issue:2, 2009
Novel azolyl-(phenylmethyl)]aryl/heteroarylamines: potent CYP26 inhibitors and enhancers of all-trans retinoic acid activity in neuroblastoma cells.Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
Novel tetralone-derived retinoic acid metabolism blocking agents: synthesis and in vitro evaluation with liver microsomal and MCF-7 CYP26A1 cell assays.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Potent and selective [2-imidazol-1-yl-2-(6-alkoxy-naphthalen-2-yl)-1-methyl-ethyl]-dimethyl-amines as retinoic acid metabolic blocking agents (RAMBAs).Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Development and Characterization of Novel and Selective Inhibitors of Cytochrome P450 CYP26A1, the Human Liver Retinoic Acid Hydroxylase.Journal of medicinal chemistry, , Mar-24, Volume: 59, Issue:6, 2016
Design and synthesis of substituted imidazole and triazole N-phenylbenzo[d]oxazolamine inhibitors of retinoic acid metabolizing enzyme CYP26.Journal of enzyme inhibition and medicinal chemistry, , Volume: 24, Issue:2, 2009
Enables
This protein enables 9 target(s):
| Target | Category | Definition |
|---|
| retinoic acid binding | molecular function | Binding to retinoic acid, 3,7-dimethyl-9-(2,6,-trimethyl-1-cyclohexen-1-yl)-2,4,6,8-nonatetraenoic acid. [GOC:hjd] |
| iron ion binding | molecular function | Binding to an iron (Fe) ion. [GOC:ai] |
| retinoic acid 4-hydroxylase activity | molecular function | Catalysis of the conversion of retinoic acid to 4-hydroxy-retinoic acid. [PMID:19519282, PMID:9250660] |
| oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, NAD(P)H as one donor, and incorporation of one atom of oxygen | molecular function | Catalysis of an oxidation-reduction (redox) reaction in which hydrogen or electrons are transferred from NADH or NADPH and one other donor, and one atom of oxygen is incorporated into one donor. [GOC:mah] |
| oxygen binding | molecular function | Binding to oxygen (O2). [GOC:jl] |
| heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
| all-trans retinoic acid 4-hydrolase activity | molecular function | Catalysis of the reaction: all-trans-retinoate + O2 + reduced [NADPH--hemoprotein reductase] = all-trans-(4S)-hydroxyretinoate + H+ + H2O + oxidized [NADPH--hemoprotein reductase]. [PMID:9250660, PMID:9716180, RHEA:51492] |
| all-trans retinoic acid 18-hydroxylase activity | molecular function | Catalysis of the reaction: all-trans-retinoate + O2 + reduced [NADPH--hemoprotein reductase] = all-trans-18-hydroxyretinoate + H+ + H2O + oxidized [NADPH--hemoprotein reductase]. [PMID:22020119, RHEA:55856] |
| monooxygenase activity | molecular function | Catalysis of the incorporation of one atom from molecular oxygen into a compound and the reduction of the other atom of oxygen to water. [ISBN:0198506732] |
Located In
This protein is located in 1 target(s):
| Target | Category | Definition |
|---|
| endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
Involved In
This protein is involved in 9 target(s):
| Target | Category | Definition |
|---|
| kidney development | biological process | The process whose specific outcome is the progression of the kidney over time, from its formation to the mature structure. The kidney is an organ that filters the blood and/or excretes the end products of body metabolism in the form of urine. [GOC:dph, GOC:mtg_kidney_jan10, ISBN:0124020607, ISBN:0721662544] |
| vitamin metabolic process | biological process | The chemical reactions and pathways involving vitamins. Vitamin is a general term for a number of unrelated organic substances that occur in many foods in small amounts and that are necessary in trace amounts for the normal metabolic functioning of the body. Vitamins may be water-soluble or fat-soluble and usually serve as components of coenzyme systems. [GOC:ai] |
| xenobiotic metabolic process | biological process | The chemical reactions and pathways involving a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:cab2, GOC:krc] |
| response to retinoic acid | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a retinoic acid stimulus. [GOC:sl] |
| response to vitamin A | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a vitamin A stimulus. [GOC:sl] |
| retinoic acid catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of retinoic acid, one of the three components that makes up vitamin A. [GOC:BHF, GOC:mah] |
| retinoic acid metabolic process | biological process | The chemical reactions and pathways involving retinoic acid, one of the three components that makes up vitamin A. [GOC:jl, http://www.indstate.edu/thcme/mwking/vitamins.html] |
| negative regulation of retinoic acid receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of retinoic acid receptor signaling pathway activity. [GOC:dgh] |
| sterol metabolic process | biological process | The chemical reactions and pathways involving sterols, steroids with one or more hydroxyl groups and a hydrocarbon side-chain in the molecule. [ISBN:0198547684] |