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Identification
- Summary
Fluocinonide is a high potency corticosteroid commonly used topically for a number of inflammatory skin conditions.
- Brand Names
- Lidemol, Lidex, Lyderm, Tiamol, Vanos
- Generic Name
- Fluocinonide
- DrugBank Accession Number
- DB01047
- Background
A topical glucocorticoid used in the treatment of eczema.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Fluocinonide (DB01047)
- Weight
- Average: 494.5249
Monoisotopic: 494.211609788 - Chemical Formula
- C26H32F2O7
- Synonyms
- Fluocinonida
- Fluocinonide
- Fluocinonido
- Fluocinonidum
- External IDs
- NSC-101791
Pharmacology
- Indication
A topical anti-inflammatory product for the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Dermatoses •••••••••••• Used in combination to treat Inflammation Combination Product in combination with: Neomycin (DB00994), Nystatin (DB00646), Gramicidin D (DB00027) •••••••••••• Used in combination to treat Pruritus Combination Product in combination with: Neomycin (DB00994), Nystatin (DB00646), Gramicidin D (DB00027) •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Fluocinonide is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders such as eczema. It mediates its effects to relieve itching, redness, dryness, crusting, scaling, inflammation, and discomfort associated with inflammatory skin conditions.
- Mechanism of action
Fluocinonide is a potent glucocorticoid steroid used topically as anti-inflammatory agent for the treatment of skin disorders such as eczema. Fluocinonide binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. Cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In another words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. Like other glucocorticoid agents Fluocinolone acetonide acts as a physiological antagonist to insulin by decreasing glycogenesis (formation of glycogen). It also promotes the breakdown of lipids (lipolysis), and proteins, leading to the mobilization of extrahepatic amino acids and ketone bodies. This leads to increased circulating glucose concentrations (in the blood). There is also decreased glycogen formation in the liver.
Target Actions Organism ASteroid hormone receptor ERR1 modulatorHumans ASteroid hormone receptor ERR2 modulatorHumans AEstrogen-related receptor gamma modulatorHumans AGlucocorticoid receptor agonistHumans UProtein smoothened agonistHumans - Absorption
The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle, the integrity of the epidermal barrier, and the use of occlusive dressings. In general, percutaneous absorption is minimal.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys.
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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Side effects may include acne-like eruptions, burning, dryness, excessive hair growth, infection of the skin, irritation, itching, lack of skin colour, prickly heat, skin inflammation, skin loss or softening, stretch marks.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Fluocinonide can be increased when it is combined with Abametapir. Abatacept The risk or severity of adverse effects can be increased when Fluocinonide is combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Fluocinonide. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Fluocinonide. Acarbose The risk or severity of hyperglycemia can be increased when Fluocinonide is combined with Acarbose. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Fluonex / Lonide / Lyderm (Taro) / Metosyn (Bioglan) / Topsymin / Topsyn (Syntex)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fluocinol Pak Cream; Kit 1 mg/1g Topical PureTek Corporation 2020-07-02 Not applicable US 
Fluocinonide Cream 0.5 mg/1g Topical A S Medication Solutions 1984-06-26 Not applicable US Fluocinonide Solution 0.5 mg/1mL Topical County Line Pharmaceuticals, LLC 2014-02-28 2019-10-01 US Fluocinonide Cream 0.5 mg/1g Topical A S Medication Solutions 1984-06-26 Not applicable US Fluocinonide Cream 0.5 mg/1g Topical Lake Erie Medical DBA Quality Care Products LLC 1984-06-26 2018-02-08 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fluocinonide Cream 1 mg/1g Topical Teligent Pharma, Inc. 2018-03-15 Not applicable US Fluocinonide Solution 0.5 mg/1mL Topical bryant ranch prepack 2019-04-19 Not applicable US Fluocinonide Cream 0.5 mg/1g Topical Preferred Pharmaceuticals, Inc. 2014-07-30 2019-09-23 US Fluocinonide Gel 0.5 mg/1g Topical H.J. Harkins Company 2011-01-20 Not applicable US Fluocinonide Ointment 0.5 mg/1g Topical Teva Pharmaceuticals USA, Inc. 1992-05-01 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Flumethovix Fluocinonide (1 mg/1g) + Dimethicone (1.8 g/100g) + Zinc oxide (2 g/100g) Kit Topical Primary Pharmaceuticals, Inc. 2021-02-19 2024-01-31 US Hexicinide Fluocinonide (1 mg/1g) + Chlorhexidine gluconate (4 g/100mL) Kit Topical PureTek Corporation 2014-01-14 Not applicable US Lidecomb Cream Fluocinonide (0.5 mg / g) + Gramicidin D (0.25 mg / g) + Neomycin sulfate (5 mg / g) + Nystatin (100000 unit / g) Cream Topical Medicis Pharmaceutical Corporation 1980-12-31 1998-09-25 Canada 
Trisyn Fluocinonide (.0925 mg / g) + Ciprocinonide (.021 mg / g) + Procinonide (.0365 mg / g) Cream Topical Baker Cummins Inc 1987-12-31 1998-08-03 Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Fluocinol Pak Fluocinonide (1 mg/1g) Cream; Kit Topical PureTek Corporation 2020-07-02 Not applicable US Fluocinonide 0.05% / Hyaluronic Acid Sodium Salt 0.5% / Niacinamide 4% Fluocinonide (0.05 g/100g) + Sodium hyaluronate (0.5 g/100g) Cream Topical Sincerus Florida, LLC 2019-05-22 Not applicable US Fluopar Fluocinonide (1 mg/1g) + Dimethicone (50 mg/1mL) Cream; Kit Topical PureTek Corporation 2014-01-14 Not applicable US
Categories
- ATC Codes
- C05AA11 — Fluocinonide
- C05AA — Corticosteroids
- C05A — AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- D07AC — Corticosteroids, potent (group III)
- D07A — CORTICOSTEROIDS, PLAIN
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- Drug Categories
- Adrenal Cortex Hormones
- Anti-Allergic Agents
- Anti-Inflammatory Agents
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Potent (Group III)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (strength unknown)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Fused-Ring Compounds
- Glucocorticoids
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Immunosuppressive Agents
- Pregnadienes
- Pregnanes
- Steroids
- Steroids, Fluorinated
- Thyroxine-binding globulin inhibitors
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Pregnane steroids
- Direct Parent
- Gluco/mineralocorticoids, progestogins and derivatives
- Alternative Parents
- 20-oxosteroids / 11-beta-hydroxysteroids / 3-oxo delta-1,4-steroids / Halogenated steroids / Delta-1,4-steroids / Alpha-acyloxy ketones / Ketals / 1,3-dioxolanes / Fluorohydrins / Cyclic ketones show 9 more
- Substituents
- 11-beta-hydroxysteroid / 11-hydroxysteroid / 20-oxosteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 6-halo-steroid / 9-halo-steroid / Acetal / Alcohol / Aliphatic heteropolycyclic compound show 28 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 2W4A77YPAN
- CAS number
- 356-12-7
- InChI Key
- WJOHZNCJWYWUJD-IUGZLZTKSA-N
- InChI
- InChI=1S/C26H32F2O7/c1-13(29)33-12-20(32)26-21(34-22(2,3)35-26)10-15-16-9-18(27)17-8-14(30)6-7-23(17,4)25(16,28)19(31)11-24(15,26)5/h6-8,15-16,18-19,21,31H,9-12H2,1-5H3/t15-,16-,18-,19-,21+,23-,24-,25-,26+/m0/s1
- IUPAC Name
- 2-[(1S,2S,4R,8S,9S,11S,12R,13S,19S)-12,19-difluoro-11-hydroxy-6,6,9,13-tetramethyl-16-oxo-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-8-yl]-2-oxoethyl acetate
- SMILES
- [H][C@@]12C[C@@]3([H])[C@]4([H])C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@@]4(F)[C@@H](O)C[C@]3(C)[C@@]1(OC(C)(C)O2)C(=O)COC(C)=O
References
- Synthesis Reference
US. Patent 3,197,469.
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015181
- KEGG Drug
- D00325
- PubChem Compound
- 9642
- PubChem Substance
- 46504523
- ChemSpider
- 9265
- 4462
- ChEBI
- 5109
- ChEMBL
- CHEMBL1501
- ZINC
- ZINC000003977978
- Therapeutic Targets Database
- DAP000421
- PharmGKB
- PA449664
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Fluocinonide
- FDA label
- Download (818 KB)
- MSDS
- Download (75.1 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Cutaneous Lupus 1 somestatus stop reason just information to hide Not Available Completed Treatment Oral Lichen Planus 1 somestatus stop reason just information to hide Not Available Withdrawn Treatment Mycosis Fungoides (MF) 1 somestatus stop reason just information to hide 4 Completed Treatment Atopic Dermatitis 2 somestatus stop reason just information to hide 4 Recruiting Treatment Central Centrifugal Cicatricial Alopecia (CCCA) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Actavis Group
- Advanced Pharmaceutical Services Inc.
- A-S Medication Solutions LLC
- Contract Pharm
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- E. Fougera and Co.
- Gallipot
- Innoviant Pharmacy Inc.
- Major Pharmaceuticals
- Mason Distributors
- Medicis Pharmaceutical Co.
- Nycomed Inc.
- Palmetto Pharmaceuticals Inc.
- Patheon Inc.
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Qualitest
- Quality Care
- Rebel Distributors Corp.
- Stat Rx Usa
- Taro Pharmaceuticals USA
- Teva Pharmaceutical Industries Ltd.
- United Research Laboratories Inc.
- Dosage Forms
Form Route Strength Cream; kit Topical 1 mg/1g Cream Topical 0.5 mg/1g Gel Topical 0.5 mg/1g Ointment Topical 0.05 mg/1g Ointment Topical 0.5 mg/1g Solution Topical 0.5 mg/1mL Cream Topical Powder Not applicable 1 g/1g Cream; kit Topical Kit Topical 1 mg/1g Kit Topical Cream Topical 0.05 % w/w Cream; emulsion Topical .05 % Gel Topical 0.05 % w/w Ointment Topical 0.05 % w/w Cream Topical 0.01 % Ointment Topical 0.01 % Ointment Topical .05 % Gel Topical 0.05 % Ointment Topical 0.05 % Cream Topical .05 % Cream Topical 0.05 % Solution Nasal; Respiratory (inhalation) 0.05 g Solution Oral 0.05 % Cream Topical 15 MG/30G Gel Cutaneous 50.000 mg Gel Topical 15 MG/30G Ointment Topical 0.05 g/100g Solution Cutaneous 15 MG/30G Jelly Topical .5 mg / g Gel Topical Cream Topical 1 mg/1g - Prices
Unit description Cost Unit Vanos 0.1% Cream 60 gm Tube 275.75USD tube Fluocinonide powder 176.0USD g Vanos 0.1% Cream 30 gm Tube 155.34USD tube Fluocinonide 0.05% Ointment 60 gm Tube 50.96USD tube Fluocinonide 0.05% Gel 60 gm Tube 50.78USD tube Fluocinonide-E 0.05% Cream 60 gm Tube 47.84USD tube Fluocinonide 0.05% Gel 30 gm Tube 30.1USD tube Fluocinonide 0.05% Ointment 30 gm Tube 28.61USD tube Fluocinonide-E 0.05% Cream 30 gm Tube 28.6USD tube Fluocinonide 0.05% Solution 60ml Bottle 27.23USD bottle Fluocinonide 0.05% Cream 60 gm Tube 22.71USD tube Fluocinonide 0.05% Solution 20ml Bottle 21.99USD bottle Fluocinonide 0.05% Ointment 15 gm Tube 21.88USD tube Fluocinonide 0.05% Gel 15 gm Tube 21.85USD tube Fluocinonide-E 0.05% Cream 15 gm Tube 20.18USD tube Fluocinonide 0.05% Cream 30 gm Tube 13.54USD tube Fluocinonide 0.05% Cream 15 gm Tube 11.99USD tube Vanos 0.1% cream 4.13USD g Lidex 0.05% cream 3.57USD g Fluocinonide-e 0.05% cream 1.33USD g Fluocinonide 0.05% cream 0.6USD g Fluocinonide-emol 0.05% cream 0.4USD g Lyderm 0.05 % Gel 0.38USD g Lyderm 0.05 % Ointment 0.37USD g Lyderm 0.05 % Cream 0.29USD g Tiamol 0.05 % Emollient Cream 0.27USD g DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US7220424 No 2007-05-22 2023-01-07 US US7794738 No 2010-09-14 2022-09-11 US US8232264 No 2012-07-31 2023-03-09 US US6765001 No 2004-07-20 2021-12-21 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 309 °C PhysProp water solubility 4.74 mg/L Not Available logP 3.19 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.0168 mg/mL ALOGPS logP 2.93 ALOGPS logP 2.05 Chemaxon logS -4.5 ALOGPS pKa (Strongest Acidic) 13.6 Chemaxon pKa (Strongest Basic) -3.4 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 99.13 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 120.56 m3·mol-1 Chemaxon Polarizability 48.97 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9823 Blood Brain Barrier + 0.981 Caco-2 permeable - 0.5804 P-glycoprotein substrate Substrate 0.7813 P-glycoprotein inhibitor I Inhibitor 0.8103 P-glycoprotein inhibitor II Non-inhibitor 0.5782 Renal organic cation transporter Non-inhibitor 0.8178 CYP450 2C9 substrate Non-substrate 0.8667 CYP450 2D6 substrate Non-substrate 0.8951 CYP450 3A4 substrate Substrate 0.7219 CYP450 1A2 substrate Non-inhibitor 0.9045 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.9482 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.8309 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8455 Ames test Non AMES toxic 0.7768 Carcinogenicity Non-carcinogens 0.9166 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 3.1492 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9835 hERG inhibition (predictor II) Non-inhibitor 0.6907
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 216.898939 predictedDarkChem Lite v0.1.0 [M-H]- 208.06499 predictedDeepCCS 1.0 (2019) [M+H]+ 216.475839 predictedDarkChem Lite v0.1.0 [M+H]+ 210.14445 predictedDeepCCS 1.0 (2019) [M+Na]+ 217.046239 predictedDarkChem Lite v0.1.0 [M+Na]+ 216.1546 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Binds to an ERR-alpha response element (ERRE) containing a single consensus half-site, 5'-TNAAGGTCA-3'. Can bind to the medium-chain acyl coenzyme A dehydrogenase (MCAD) response element NRRE-1 and may act as an important regulator of MCAD promoter. Binds to the C1 region of the lactoferrin gene promoter. Requires dimerization and the coactivator, PGC-1A, for full activity. The ERRalpha/PGC1alpha complex is a regulator of energy metabolism. Induces the expression of PERM1 in the skeletal muscle
- Specific Function
- DNA-binding transcription factor activity
- Gene Name
- ESRRA
- Uniprot ID
- P11474
- Uniprot Name
- Steroid hormone receptor ERR1
- Molecular Weight
- 45509.11 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Transcription factor that binds a canonical ESRRB recognition (ERRE) sequence 5'TCAAGGTCA-3' localized on promoter and enhancer of targets genes regulating their expression or their transcription activity (PubMed:17920186, PubMed:19755138). Plays a role, in a LIF-independent manner, in maintainance of self-renewal and pluripotency of embryonic and trophoblast stem cells through different signaling pathways including FGF signaling pathway and Wnt signaling pathways. Upon FGF signaling pathway activation, interacts with KDM1A by directly binding to enhancer site of ELF5 and EOMES and activating their transcription leading to self-renewal of trophoblast stem cells. Also regulates expression of multiple rod-specific genes and is required for survival of this cell type (By similarity). Plays a role as transcription factor activator of GATA6, NR0B1, POU5F1 and PERM1 (PubMed:23836911). Plays a role as transcription factor repressor of NFE2L2 transcriptional activity and ESR1 transcriptional activity (PubMed:17920186, PubMed:19755138). During mitosis remains bound to a subset of interphase target genes, including pluripotency regulators, through the canonical ESRRB recognition (ERRE) sequence, leading to their transcriptional activation in early G1 phase. Can coassemble on structured DNA elements with other transcription factors like SOX2, POU5F1, KDM1A and NCOA3 to trigger ESRRB-dependent gene activation. This mechanism, in the case of SOX2 corecruitment prevents the embryonic stem cells (ESCs) to epiblast stem cells (EpiSC) transition through positive regulation of NR0B1 that inhibits the EpiSC transcriptional program. Also plays a role inner ear development by controlling expression of ion channels and transporters and in early placentation (By similarity)
- Specific Function
- cis-regulatory region sequence-specific DNA binding
- Gene Name
- ESRRB
- Uniprot ID
- O95718
- Uniprot Name
- Steroid hormone receptor ERR2
- Molecular Weight
- 48053.14 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Modulator
- General Function
- Orphan receptor that acts as a transcription activator in the absence of bound ligand. Binds specifically to an estrogen response element and activates reporter genes controlled by estrogen response elements (By similarity). Induces the expression of PERM1 in the skeletal muscle
- Specific Function
- AF-2 domain binding
- Gene Name
- ESRRG
- Uniprot ID
- P62508
- Uniprot Name
- Estrogen-related receptor gamma
- Molecular Weight
- 51305.485 Da
References
- Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor for glucocorticoids (GC) (PubMed:27120390, PubMed:37478846). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors (PubMed:28139699). Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling (PubMed:9590696). Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay (PubMed:25775514). Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity)
- Specific Function
- core promoter sequence-specific DNA binding
- Gene Name
- NR3C1
- Uniprot ID
- P04150
- Uniprot Name
- Glucocorticoid receptor
- Molecular Weight
- 85658.57 Da
References
- Jessop S, Whitelaw D, Jordaan F: Drugs for discoid lupus erythematosus. Cochrane Database Syst Rev. 2001;(1):CD002954. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- G protein-coupled receptor which associates with the patched protein (PTCH) to transduce hedgehog protein signaling. Binding of sonic hedgehog (SHH) to its receptor patched prevents inhibition of smoothened (SMO) by patched. When active, SMO binds to and sequesters protein kinase A catalytic subunit PRKACA at the cell membrane, preventing PRKACA-mediated phosphorylation of GLI transcription factors which releases the GLI proteins from PRKACA-mediated inhibition and allows for transcriptional activation of hedgehog pathway target genes (By similarity). Required for the accumulation of KIF7, GLI2 and GLI3 in the cilia (PubMed:19592253). Interacts with DLG5 at the ciliary base to induce the accumulation of KIF7 and GLI2 at the ciliary tip for GLI2 activation (By similarity)
- Specific Function
- cAMP-dependent protein kinase inhibitor activity
- Gene Name
- SMO
- Uniprot ID
- Q99835
- Uniprot Name
- Protein smoothened
- Molecular Weight
- 86395.95 Da
References
- Wang J, Lu J, Bond MC, Chen M, Ren XR, Lyerly HK, Barak LS, Chen W: Identification of select glucocorticoids as Smoothened agonists: potential utility for regenerative medicine. Proc Natl Acad Sci U S A. 2010 May 18;107(20):9323-8. doi: 10.1073/pnas.0910712107. Epub 2010 May 3. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, 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). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Moore CD, Roberts JK, Orton CR, Murai T, Fidler TP, Reilly CA, Ward RM, Yost GS: Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes. Drug Metab Dispos. 2013 Feb;41(2):379-89. doi: 10.1124/dmd.112.046318. Epub 2012 Nov 9. [Article]
- Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). 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). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
- Specific Function
- aromatase activity
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species
- Specific Function
- serine-type endopeptidase inhibitor activity
- Gene Name
- SERPINA6
- Uniprot ID
- P08185
- Uniprot Name
- Corticosteroid-binding globulin
- Molecular Weight
- 45140.49 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Drug created at June 13, 2005 13:24 / Updated at October 07, 2024 13:58