General Information of the Protein
| Protein ID |
PT00817
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| Protein Name |
Cytochrome P450 2D6
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| Secondarily Protein Name |
CYPIID6
Cholesterol 25-hydroxylase
Cytochrome P450-DB1
Debrisoquine 4-hydroxylase
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| Gene Name |
CYP2D6
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| Secondarily Gene Name |
CYP2DL1
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| Sequence |
MGLEALVPLAVIVAIFLLLVDLMHRRQRWAARYPPGPLPLPGLGNLLHVDFQNTPYCFDQLRRRFGDVFSLQLAWTPVVVLNGLAAVREALVTHGEDTADRPPVPITQILGFGPRSQGVFLARYGPAWREQRRFSVSTLRNLGLGKKSLEQWVTEEAACLCAAFANHSGRPFRPNGLLDKAVSNVIASLTCGRRFEYDDPRFLRLLDLAQEGLKEESGFLREVLNAVPVLLHIPALAGKVLRFQKAFLTQLDELLTEHRMTWDPAQPPRDLTEAFLAEMEKAKGNPESSFNDENLRIVVADLFSAGMVTTSTTLAWGLLLMILHPDVQRRVQQEIDDVIGQVRRPEMGDQAHMPYTTAVIHEVQRFGDIVPLGVTHMTSRDIEVQGFRIPKGTTLITNLSSVLKDEAVWEKPFRFHPEHFLDAQGHFVKPEAFLPFSAGRRACLGEPLARMELFLFFTSLLQHFSFSVPTGQPRPSHHGVFAFLVSPSPYELCAVPR
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| Organism |
Homo sapiens, Human
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| Protein Classification |
Enzyme
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Cytochrome P450
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Cytochrome P450 family 2
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Cytochrome P450 family 2D
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Cytochrome P450 2D6
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| Function |
A cytochrome P450 monooxygenase involved in the metabolism of fatty acids, steroids and retinoids (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18698000, PubMed:19965576, PubMed:20972997, PubMed:21289075, PubMed:21576599). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:19965576, PubMed:20972997). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 20-hydroxyeicosatetraenoic acid ethanolamide (20-HETE-EA) and 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:18698000, PubMed:21289075). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Catalyzes the oxidative transformations of all-trans retinol to all-trans retinal, a precursor for the active form all-trans-retinoic acid (PubMed:10681376). Also involved in the oxidative metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
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| Uniprot ID |
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| Subcellular Location |
Endoplasmic reticulum membrane
Microsome membrane
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Map of Molecular Bioactivity Related to the Protein
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Map of Molecular Bioactivity Related to the Protein Protein Cell Line Compound Bioactivity Value: <= 0.1 μM > 0.1 μM and <= 10 μM > 10 μM Imprecise Activity |
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Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000023 , BTI-Tn-5B1-4
Cell Line ID: CL000006 , HEK293
Biochemical Assays
Clinical Information about the Protein
Target 1 ( Debrisoquine 4-hydroxylase (CYP2D6) )
| Target Type | Successful Target | ||||
|---|---|---|---|---|---|
| Disease | 3 Target-related Diseases | 3 | |||
| 1 | Insomnia [ICD-11: 7A00-7A0Z] | ||||
| 2 | Malaria [ICD-11: 1F40-1F45] | ||||
| 3 | Migraine [ICD-11: 8A80] | ||||
| Approved Drug(s) | 1 Approved Drug | 1 | |||
| 1 | Glutethimide | Approved | |||
| Clinical Trial Drug(s) | 1 Clinical Trial Drug | 1 | |||
| 1 | ISOQUINE | Phase 1 | |||
| Investigative Drug(s) | 1 Investigative Drug | 1 | |||
| 1 | BMS-694153 | Investigative | |||