Proteins > Cytochrome P450 11B1, mitochondrial
Page last updated: 2024-08-07 13:01:46
Cytochrome P450 11B1, mitochondrial
A cytochrome P450 11B that is a translation product of the CYP11B1 gene in human. [PRO:DNx, UniProtKB:P15538]
Synonyms
CYPXIB1;
Cytochrome P-450c11;
Cytochrome P450C11;
Steroid 11-beta-hydroxylase, CYP11B1;
1.14.15.4
Research
Bioassay Publications (39)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (5.13) | 18.2507 |
2000's | 9 (23.08) | 29.6817 |
2010's | 27 (69.23) | 24.3611 |
2020's | 1 (2.56) | 2.80 |
Compounds (17)
Drugs with Inhibition Measurements
Design, synthesis, and evaluation of (2S,4R)-Ketoconazole sulfonamide analogs as potential treatments for Metabolic Syndrome.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.ACS medicinal chemistry letters, , Aug-11, Volume: 2, Issue:8, 2011
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Accelerated skin wound healing by selective 11β-Hydroxylase (CYP11B1) inhibitors.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Identification of 4-(4-nitro-2-phenethoxyphenyl)pyridine as a promising new lead for discovering inhibitors of both human and rat 11β-Hydroxylase.European journal of medicinal chemistry, , Volume: 96, 2015
Discovery of new 7-substituted-4-imidazolylmethyl coumarins and 4'-substituted-2-imidazolyl acetophenones open analogues as potent and selective inhibitors of steroid-11β-hydroxylase.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Potent 11β-hydroxylase inhibitors with inverse metabolic stability in human plasma and hepatic S9 fractions to promote wound healing.Journal of medicinal chemistry, , Sep-25, Volume: 57, Issue:18, 2014
Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type.Journal of medicinal chemistry, , Aug-08, Volume: 56, Issue:15, 2013
First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.ACS medicinal chemistry letters, , Aug-11, Volume: 2, Issue:8, 2011
N-(Pyridin-3-yl)benzamides as selective inhibitors of human aldosterone synthase (CYP11B2).Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
1-Phenylsulfinyl-3-(pyridin-3-yl)naphthalen-2-ols: a new class of potent and selective aldosterone synthase inhibitors.European journal of medicinal chemistry, , Jan-07, Volume: 89, 2015
Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Tetrahydropyrroloquinolinone type dual inhibitors of aromatase/aldosterone synthase as a novel strategy for breast cancer patients with elevated cardiovascular risks.Journal of medicinal chemistry, , Jan-24, Volume: 56, Issue:2, 2013
Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.Journal of medicinal chemistry, , Aug-08, Volume: 56, Issue:15, 2013
Modulation of cytochromes P450 with xanthone-based molecules: from aromatase to aldosterone synthase and steroid 11β-hydroxylase inhibition.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.Journal of medicinal chemistry, , Aug-23, Volume: 55, Issue:16, 2012
Design, synthesis, and biological evaluation of imidazolyl derivatives of 4,7-disubstituted coumarins as aromatase inhibitors selective over 17-α-hydroxylase/C17-20 lyase.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
Fine-tuning the selectivity of aldosterone synthase inhibitors: structure-activity and structure-selectivity insights from studies of heteroaryl substituted 1,2,5,6-tetrahydropyrrolo[3,2,1-ij]quinolin-4-one derivatives.Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Novel aldosterone synthase inhibitors with extended carbocyclic skeleton by a combined ligand-based and structure-based drug design approach.Journal of medicinal chemistry, , Oct-09, Volume: 51, Issue:19, 2008
In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Overcoming undesirable CYP1A2 inhibition of pyridylnaphthalene-type aldosterone synthase inhibitors: influence of heteroaryl derivatization on potency and selectivity.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Pyridyl-substituted tetrahydrocyclopropa[a]naphthalenes: highly active and selective inhibitors of P450 arom.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2).Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.Journal of medicinal chemistry, , Aug-08, Volume: 56, Issue:15, 2013
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.Journal of medicinal chemistry, , Jul-08, Volume: 53, Issue:13, 2010
Novel CYP17 inhibitors: synthesis, biological evaluation, structure-activity relationships and modelling of methoxy- and hydroxy-substituted methyleneimidazolyl biphenyls.European journal of medicinal chemistry, , Volume: 44, Issue:7, 2009
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Synthesis, biological evaluation, and molecular modeling of abiraterone analogues: novel CYP17 inhibitors for the treatment of prostate cancer.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Optimization of the First Selective Steroid-11β-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.ACS medicinal chemistry letters, , Aug-11, Volume: 2, Issue:8, 2011
First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases.ACS medicinal chemistry letters, , Jan-13, Volume: 2, Issue:1, 2011
Synthesis, biological evaluation, and molecular modeling of 1-benzyl-1H-imidazoles as selective inhibitors of aldosterone synthase (CYP11B2).Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Design, Synthesis, and Biological Evaluations of Pyridyl 4,5,6,7-Tetrahydro-4,7-Methanobenzo[Journal of medicinal chemistry, , 09-08, Volume: 65, Issue:17, 2022
Discovery of Novel Pyrazole-Based Selective Aldosterone Synthase (CYP11B2) Inhibitors: A New Template to Coordinate the Heme-Iron Motif of CYP11B2.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Lead Optimization Generates CYP11B1 Inhibitors of Pyridylmethyl Isoxazole Type with Improved Pharmacological Profile for the Treatment of Cushing's Disease.Journal of medicinal chemistry, , 06-22, Volume: 60, Issue:12, 2017
Novel pyridyl substituted 4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines as potent and selective aldosterone synthase inhibitors with improved in vitro metabolic stability.Journal of medicinal chemistry, , Mar-12, Volume: 58, Issue:5, 2015
Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.Journal of medicinal chemistry, , Dec-10, Volume: 58, Issue:23, 2015
Heteroatom insertion into 3,4-dihydro-1H-quinolin-2-ones leads to potent and selective inhibitors of human and rat aldosterone synthase.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
Aldosterone synthase inhibitors as promising treatments for mineralocorticoid dependent cardiovascular and renal diseases.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.Journal of medicinal chemistry, , Jun-26, Volume: 57, Issue:12, 2014
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Enables
This protein enables 4 target(s):
Target | Category | Definition |
steroid 11-beta-monooxygenase activity | molecular function | Catalysis of the reaction: a steroid + reduced adrenal ferredoxin + O2 = an 11-beta-hydroxysteroid + oxidized adrenal ferredoxin + H2O. [EC:1.14.15.4] |
iron ion binding | molecular function | Binding to an iron (Fe) ion. [GOC:ai] |
heme binding | molecular function | Binding to a heme, a compound composed of iron complexed in a porphyrin (tetrapyrrole) ring. [GOC:ai] |
corticosterone 18-monooxygenase activity | molecular function | Catalysis of the reaction: corticosterone + reduced adrenal ferredoxin + O2 = 18-hydroxycorticosterone + oxidized adrenal ferredoxin + H2O. [EC:1.14.15.5] |
Located In
This protein is located in 2 target(s):
Target | Category | Definition |
mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
mitochondrial inner membrane | cellular component | The inner, i.e. lumen-facing, lipid bilayer of the mitochondrial envelope. It is highly folded to form cristae. [GOC:ai] |
Involved In
This protein is involved in 13 target(s):
Target | Category | Definition |
C21-steroid hormone biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of C21-steroid hormones, steroid compounds containing 21 carbons which function as hormones. [GOC:ai] |
glucocorticoid biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of glucocorticoids, hormonal C21 corticosteroids synthesized from cholesterol. [ISBN:0198506732] |
immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
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] |
aldosterone biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of aldosterone, a corticosteroid hormone that is produced by the zona glomerulosa of the adrenal cortex and regulates salt (sodium and potassium) and water balance. [PMID:16527843] |
cellular response to hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah] |
cortisol biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of cortisol, the steroid hormone 11-beta-17,21-trihydroxypregn-4-ene-3,20-dione. Cortisol is synthesized from cholesterol in the adrenal gland and controls carbohydrate, fat and protein metabolism and has anti-inflammatory properties. [GOC:BHF, GOC:mah, GOC:rl] |
cellular response to potassium ion | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a potassium ion stimulus. [GOC:yaf] |
glucose homeostasis | biological process | Any process involved in the maintenance of an internal steady state of glucose within an organism or cell. [GOC:go_curators] |
cholesterol metabolic process | biological process | The chemical reactions and pathways involving cholesterol, cholest-5-en-3 beta-ol, the principal sterol of vertebrates and the precursor of many steroids, including bile acids and steroid hormones. It is a component of the plasma membrane lipid bilayer and of plasma lipoproteins and can be found in all animal tissues. [ISBN:0198506732] |
cortisol metabolic process | biological process | The chemical reactions and pathways involving cortisol, the steroid hormone 11-beta-17,21-trihydroxypregn-4-ene-3,20-dione. Cortisol is synthesized from cholesterol in the adrenal gland and controls carbohydrate, fat and protein metabolism and has anti-inflammatory properties. [GOC:BHF, GOC:mah, GOC:rl] |
cellular response to peptide hormone stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a peptide hormone stimulus. A peptide hormone is any of a class of peptides that are secreted into the blood stream and have endocrine functions in living animals. [GOC:mah] |