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CYP11B1

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Target not currently curated in GtoImmuPdb

Target id: 1359

Nomenclature: CYP11B1

Abbreviated Name: Steroid 11β-hydroxylase

Family: CYP11, CYP17, CYP19, CYP20 and CYP21 families

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 503 8q24.3 CYP11B1 cytochrome P450 family 11 subfamily B member 1
Mouse - 501 15 34.29 cM Cyp11b1 cytochrome P450, family 11, subfamily b, polypeptide 1
Rat - 499 7q34 Cyp11b1 cytochrome P450, family 11, subfamily b, polypeptide 1
Previous and Unofficial Names Click here for help
cytochrome P450, subfamily XIB, polypeptide 1 | cytochrome P450 11B1, mitochondrial | steroid 11-beta-hydroxylase | cytochrome P450, family 11, subfamily B, polypeptide 1 | cytochrome P450, family 11, subfamily b, polypeptide 1 | cytochrome P450
Database Links Click here for help
Alphafold P15538 (Hs), P15393 (Rn)
BRENDA 1.14.15.4
ChEMBL Target CHEMBL1908 (Hs), CHEMBL4970 (Rn)
DrugBank Target P15538 (Hs)
Ensembl Gene ENSG00000160882 (Hs), ENSMUSG00000075604 (Mm), ENSRNOG00000068909 (Rn)
Entrez Gene 1584 (Hs), 110115 (Mm), 500892 (Rn)
Human Protein Atlas ENSG00000160882 (Hs)
KEGG Enzyme 1.14.15.4
KEGG Gene hsa:1584 (Hs), mmu:110115 (Mm), rno:500892 (Rn)
OMIM 610613 (Hs)
Orphanet ORPHA120949 (Hs)
Pharos P15538 (Hs)
UniProtKB P15538 (Hs), P15393 (Rn)
Wikipedia CYP11B1 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.14.15.4

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
fadrozole Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 8.7 pKi 1
⤷ pKi 8.7 (Ki 2.2x10-9 M) [1]
azalanstat Small molecule or natural product Bt Inhibition 7.5 pKi 4
⤷ pKi 7.5 (Ki 3.5x10-8 M) [4]
osilodrostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.5 pIC50 5
⤷ pIC50 8.5 (IC50 2.9x10-9 M) [5]
metyrapone Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 6
⤷ pIC50 7.8 (IC50 1.46x10-8 M) [6]
(2S,4S)-ketoconazole Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.9 pIC50 3
⤷ pIC50 6.9 [3]
levoketoconazole Small molecule or natural product Approved drug Ligand has a PDB structure Bt Inhibition 6.2 pIC50 3
⤷ pIC50 6.2 (IC50 6.08x10-7 M) [3]
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Immuno Process:  Inflammation
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Congenital adrenal hyperplasia due to 11-beta-hydroxylase deficiency
Synonyms: Congenital adrenal hyperplasia [Disease Ontology: DOID:12255]
Disease Ontology: DOID:12255
OMIM: 202010
Orphanet: ORPHA90795
References:  2
Disease:  Familial hyperaldosteronism type I
Synonyms: Glucocorticoid-remediable aldosteronism; GRA [OMIM: 103900]
OMIM: 103900
Orphanet: ORPHA403

References

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1. LaSala D, Shibanaka Y, Jeng AY. (2009) Coexpression of CYP11B2 or CYP11B1 with adrenodoxin and adrenodoxin reductase for assessing the potency and selectivity of aldosterone synthase inhibitors. Anal Biochem, 394 (1): 56-61. [PMID:19622340]

2. No authors listed. (2004) Natalizumab: AN 100226, anti-4alpha integrin monoclonal antibody. Drugs R D, 5 (2): 102-7. [PMID:15293871]

3. Rotstein DM, Kertesz DJ, Walker KA, Swinney DC. (1992) Stereoisomers of ketoconazole: preparation and biological activity. J Med Chem, 35 (15): 2818-25. [PMID:1495014]

4. Walker KA, Kertesz DJ, Rotstein DM, Swinney DC, Berry PW, So OY, Webb AS, Watson DM, Mak AY, Burton PM et al.. (1993) Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. J Med Chem, 36 (15): 2235-7. [PMID:8340925]

5. Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW. (2014) Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors. J Med Chem, 57 (12): 5179-89. [PMID:24899257]

6. Zimmer C, Hafner M, Zender M, Ammann D, Hartmann RW, Vock CA. (2011) N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2). Bioorg Med Chem Lett, 21 (1): 186-90. [PMID:21129965]

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