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CYP11B2

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Target id: 1360

Nomenclature: CYP11B2

Abbreviated Name: Aldosterone synthase

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 CYP11B2 cytochrome P450 family 11 subfamily B member 2
Mouse - 500 15 34.29 cM Cyp11b2 cytochrome P450, family 11, subfamily b, polypeptide 2
Rat - - Cyp11b2 cytochrome P450, family 11, subfamily b, polypeptide 2
Previous and Unofficial Names Click here for help
ALDOS | aldosterone-synthesizing enzyme | cytochrome P450, subfamily XIB (steroid 11-beta-hydroxylase), polypeptide 2 | cytochrome P450 11B2, mitochondrial | Cytochrome P450 subfamily XIB polypeptide 2 (aldosterone synthase) | cytochrome P450, family 11, subfamily b, polypeptide 2 | cytochrome P450
Database Links Click here for help
Alphafold P19099 (Hs), P15539 (Mm), P30100 (Rn), P30099 (Rn)
BRENDA 1.14.15.4, 1.14.15.5
ChEMBL Target CHEMBL2722 (Hs), CHEMBL3621020 (Mm), CHEMBL3237 (Rn)
Ensembl Gene ENSG00000179142 (Hs), ENSMUSG00000022589 (Mm), ENSRNOG00000030111 (Rn)
Entrez Gene 1585 (Hs), 13072 (Mm), 24294 (Rn)
Human Protein Atlas ENSG00000179142 (Hs)
KEGG Enzyme 1.14.15.4, 1.14.15.5
KEGG Gene hsa:1585 (Hs), mmu:13072 (Mm), rno:24294 (Rn)
OMIM 124080 (Hs)
Pharos P19099 (Hs)
SynPHARM 81950 (in complex with fadrozole)
UniProtKB P19099 (Hs), P15539 (Mm), P30100 (Rn), P30099 (Rn)
Wikipedia CYP11B2 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.14.15.4
EC Number: 1.14.15.5

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 9.1 pKi 3
⤷ pKi 9.1 (Ki 8x10-10 M) [3]
lorundrostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.9 pKi 5
⤷ pKi 8.9 (Ki 1.27x10-9 M) [5]
Description: Measuring inhibition of aldosterone generation from the substrate 11-DOC in the mitochondrial fraction of V79 cells stably expressing hCYP11B2
baxdrostat Small molecule or natural product Monkey Inhibition 8.4 pKi 1
⤷ pKi 8.4 (Ki 4x10-9 M) [1]
baxdrostat Small molecule or natural product Hs Inhibition 7.9 pKi 1
⤷ pKi 7.9 (Ki 1.3x10-8 M) [1]
osilodrostat Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.7 pIC50 6
⤷ pIC50 9.7 (IC50 2x10-10 M) [6]
dexfadrostat Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 4
⤷ pIC50 8.0 (IC50 1.08x10-8 M) [4]
vicadrostat Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 2
⤷ pIC50 7.8 (IC50 1.6x10-8 M) [2]
metyrapone Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.1 pIC50 7
⤷ pIC50 7.1 [7]
View species-specific inhibitor tables

References

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1. Bogman K, Schwab D, Delporte ML, Palermo G, Amrein K, Mohr S, De Vera Mudry MC, Brown MJ, Ferber P. (2017) Preclinical and Early Clinical Profile of a Highly Selective and Potent Oral Inhibitor of Aldosterone Synthase (CYP11B2). Hypertension, 69 (1): 189-196. [PMID:27872236]

2. Burke J, Cogan D, Lord J, Marshall DR, McBikken BP, Yu M, Zhang Y, Cerny MA, Fader L, Frederick KS et al.. (2016) Aldosterone synthase inhibitors. Patent number: WO2016014736A1. Assignee: Boehringer Ingelheim International Gmbh. Priority date: 23/07/2015. Publication date: 28/01/2016.

3. 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]

4. Pignatti E, Kollar J, Hafele E, Schuster D, Steele RE, Vogt B, Schumacher C, Groessl M. (2023) Structural and clinical characterization of CYP11B2 inhibition by dexfadrostat phosphate. J Steroid Biochem Mol Biol, 235: 106409. [PMID:37827219]

5. Shimizu H, Tortorici MA, Ohta Y, Ogawa K, Rahman SMA, Fujii A, Hiraga Y, Kawai M, Sugimoto-Kawabata K, van Iersel MT et al.. (2024) First-in-human study evaluating safety, pharmacokinetics, and pharmacodynamics of lorundrostat, a novel and highly selective aldosterone synthase inhibitor. Clin Transl Sci, 17 (8): e70000. [PMID:39152532]

6. 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]

7. 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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