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Identification
- Summary
Desonide is a topical corticosteroid used for the symptomatic treatment of inflammatory and pruritic manifestations of corticosteroid responsive dermatoses.
- Brand Names
- Desonate, Desowen, Desrx, Lokara, Tridesilon, Verdeso
- Generic Name
- Desonide
- DrugBank Accession Number
- DB01260
- Background
A nonfluorinated corticosteroid anti-inflammatory agent used topically for dermatoses.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Desonide (DB01260)
- Weight
- Average: 416.5073
Monoisotopic: 416.219888756 - Chemical Formula
- C24H32O6
- Synonyms
- 11β,21-dihydroxy-16α,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-dione
- 11β,21-dihydroxy-16α,17-isopropylidenedioxypregna-1,4-diene-3,20-dione
- 11β,21-dihydroxy-16α,17α-isopropylidenedioxypregna-1,4-diene-3,20-dione
- 16α-hydroxyprednisole-16,17-acetonide
- 16α-hydroxyprednisolone-16α,17-acetonide
- 16α,17α-isopropylidenedioxyprednisolone
- Desfluorotriamcinolone acetonide
- Desonida
- Desonide
- Desonidum
- External IDs
- D-2083
- D2083
Pharmacology
- Indication
For the relief of the inflammatory and pruritic manifestations of corticosteroid responsive dermatose.
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Dermatoses •••••••••••• •••••• ••••••••• ••••••• ••••••••• •••••••• Symptomatic treatment of Eye inflammation ••• ••• •••••••• • ••••• Management of Mild atopic dermatitis •••••••••••• •••••••• ••••• ••• Management of Moderate atopic dermatitis •••••••••••• •••••••• ••••• ••• - 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
Desonide is a synthetic nonfluorinated corticosteroid for topical dermatologic use. The corticosteroids constitute a class of primarily synthetic steroids used topically as anti-inflammatory and antipruritic agents.
- Mechanism of action
Like other topical corticosteroids, desonide has anti-inflammatory, antipruritic and vasoconstrictive properties. The drug binds to cytosolic glucocorticoid receptors. This complex migrates to the nucleus and binds to genetic elements on the DNA. This activates and represses various genes. However corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.
Target Actions Organism ASteroid hormone receptor ERR1 modulatorHumans ASteroid hormone receptor ERR2 modulatorHumans AEstrogen-related receptor gamma modulatorHumans AGlucocorticoid receptor agonistHumans - Absorption
Topical corticosteroids can be absorbed from normal intact skin, inflammation and/or other disease processes in the skin may increase percutaneous absorption.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- 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 Desonide can be increased when it is combined with Abametapir. Acarbose The risk or severity of hyperglycemia can be increased when Desonide is combined with Acarbose. Acetohexamide The risk or severity of hyperglycemia can be increased when Desonide is combined with Acetohexamide. Acetyldigitoxin The risk or severity of adverse effects can be increased when Desonide is combined with Acetyldigitoxin. Albiglutide The risk or severity of hyperglycemia can be increased when Desonide is combined with Albiglutide. - 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
- Desocort (Galderma) / Tridesilon (Bayer)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Desocort Cream 0.05% Cream .05 % Topical Galderma 1994-12-31 2007-08-02 Canada 
Desocort Lotion - 0.05% Lotion .05 % Topical Galderma 1994-12-31 2016-08-04 Canada Desocort Ointment - 0.05% Ointment .05 % Topical Galderma 1994-12-31 2016-08-04 Canada Desonate Gel 0.5 mg/1g Topical SkinMedica 2007-03-30 Not applicable US 
Desonate Gel 0.5 mg/1g Topical LEO Pharma Inc. 2018-10-01 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Desonide Lotion 0.5 mg/1g Topical Physicians Total Care, Inc. 2004-05-17 Not applicable US Desonide Gel 0.5 mg/1g Topical Cintex Services, Llc 2020-07-09 Not applicable US Desonide Ointment 0.5 mg/1g Topical Glenmark Pharmaceuticals Inc., USA 2017-09-15 2023-02-01 US Desonide Cream 0.5 mg/1g Topical Zydus Lifesciences Limited 2019-11-25 Not applicable US Desonide Ointment 0.5 mg/1g Topical E. Fougera & Co. a division of Fougera Pharmaceuticals Inc. 2001-03-12 2025-03-31 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image APOLAR N Desonide (0.5 mg/g) + Neomycin sulfate (5 mg/g) Cream Actavis 2018-11-08 2023-07-09 Indonesia 
DESOLEX-N Desonide (0.05 %) + Neomycin sulfate (0.5 %) Cream Surya Dermato Medica Laboratories 2018-09-24 2028-04-11 Indonesia DESONIDA CLIOQUINOL CREMA. Desonide (0.1 g) + Clioquinol (3 g) Cream Topical ALTEA FARMACEUTICA S.A. 2006-11-10 Not applicable Colombia 
MEPROLAR-N Desonide (0.5 mg/g) + Neomycin sulfate (5 mg/g) Cream Topical Meprofarm 2019-07-29 2024-07-29 Indonesia PRECORT-A KREM Desonide (0.125 %) + Clioquinol (3 %) Cream Topical KOÇAK FARMA İLAÇ VE KİMYA SAN. A.Ş. 2011-12-28 Not applicable Turkey 
Categories
- ATC Codes
- S01BA11 — Desonide
- S01BA — Corticosteroids, plain
- S01B — ANTIINFLAMMATORY AGENTS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- D07BB — Corticosteroids, moderately potent, combinations with antiseptics
- D07B — CORTICOSTEROIDS, COMBINATIONS WITH ANTISEPTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- Drug Categories
- Adrenal Cortex Hormones
- Anti-Inflammatory Agents
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids, Moderately Potent (Group II)
- 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 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Fused-Ring Compounds
- Immunosuppressive Agents
- Ophthalmologicals
- Pregnadienes
- Pregnadienetriols
- Pregnanes
- Sensory Organs
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Hydroxysteroids
- Direct Parent
- 21-hydroxysteroids
- Alternative Parents
- Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 3-oxo delta-1,4-steroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Ketals / Alpha-hydroxy ketones / 1,3-dioxolanes / Secondary alcohols / Cyclic ketones show 5 more
- Substituents
- 11-beta-hydroxysteroid / 11-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Acetal / Alcohol / Aliphatic heteropolycyclic compound / Alpha-hydroxy ketone show 18 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- 11beta-hydroxy steroid, cyclic ketal, 20-oxo steroid, 3-oxo-Delta(1),Delta(4)-steroid, corticosteroid, 21-hydroxy steroid (CHEBI:204734)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- J280872D1O
- CAS number
- 638-94-8
- InChI Key
- WBGKWQHBNHJJPZ-LECWWXJVSA-N
- InChI
- InChI=1S/C24H32O6/c1-21(2)29-19-10-16-15-6-5-13-9-14(26)7-8-22(13,3)20(15)17(27)11-23(16,4)24(19,30-21)18(28)12-25/h7-9,15-17,19-20,25,27H,5-6,10-12H2,1-4H3/t15-,16-,17-,19+,20+,22-,23-,24+/m0/s1
- IUPAC Name
- (1S,2S,4R,8S,9S,11S,12S,13R)-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one
- SMILES
- [H][C@@]12C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
References
- Synthesis Reference
Bernstein, S. and Allen, G.R., Jr.; U.S. Patent 2,990,401; June 27, 1961; assigned to American Cyanamid Company. Diassi, P.A. and Principe, P.A.; U.S.Patent 3,549,498; December 22, 1970; assigned to E.R. Squibb & Sons, inc.
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0015389
- KEGG Drug
- D03696
- PubChem Compound
- 5311066
- PubChem Substance
- 46506186
- ChemSpider
- 4470603
- 3254
- ChEBI
- 204734
- ChEMBL
- CHEMBL1201109
- ZINC
- ZINC000004212851
- Therapeutic Targets Database
- DAP001188
- PharmGKB
- PA164776996
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Desonide
- MSDS
- Download (73.7 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 data4 Completed Treatment Atopic Dermatitis 3 somestatus stop reason just information to hide 4 Completed Treatment Hyperpigmentation 1 somestatus stop reason just information to hide 4 Withdrawn Treatment Psoriasis 1 somestatus stop reason just information to hide 3 Completed Treatment Atopic Dermatitis 2 somestatus stop reason just information to hide 3 Unknown Status Treatment Atopic Dermatitis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Actavis Group
- Ameri-Pac Inc.
- Contract Pharm
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- DPT Laboratories Ltd.
- E. Fougera and Co.
- Galderma Laboratories
- Intendis Inc.
- Ivax Pharmaceuticals
- Major Pharmaceuticals
- Medisca Inc.
- Nycomed Inc.
- Palmetto Pharmaceuticals Inc.
- Perrigo Co.
- Pharmedix
- Physicians Total Care Inc.
- Stiefel Labs
- Taro Pharmaceuticals USA
- Dosage Forms
Form Route Strength Cream Topical 0.1 g Emulsion Topical 0.05 g Cream Cutaneous 0.0005 g Emulsion Topical 0.050 mg Cream Topical 100 mg Lotion Topical .05 % Ointment 0.05 % Solution Topical 0.05 % Cream Gel Topical 0.5 mg/1g Cream Topical 0.05 g Lotion Topical 0.1 g Cream Topical Cream Topical .5 mg/1g Lotion Topical .5 mg/1g Lotion Topical 0.5 mg/1g Ointment Topical 0.5 mg/1g Ointment Topical 0.5 mg/01g Solution Topical Cream Cutaneous 0.050 g Cream Topical 0.5 mg/1g Emulsion Cutaneous 0.0500 g Lotion Topical 0.05 % Ointment Topical 0.05 % Lotion Topical 0.05 % w/w Lotion Topical 0.5 mg/1mL Cream Topical 0.5 mg/g Cream Topical 0.05 % Cream Topical 0.05 % w/w Ointment Topical 0.05 % w/w Ointment Topical 0.125 % Cream Topical 0125 % Ointment Topical Ointment Ophthalmic 0.25 % Ointment Ophthalmic 5 G Solution / drops Ophthalmic 0.25 % Solution / drops Ophthalmic 10 ml Cream Topical Solution Topical Lotion Topical Cream Topical 0.05 G/100G Ointment 0.05 G/100G Solution Topical 0.05 G/100G Cream Topical .05 % Ointment Topical .05 % Cream Topical 0.03 g/60g Cream Topical .5 mg / g Ointment Topical .5 mg / g Aerosol, foam Topical 0.05 % Aerosol, foam Topical 0.5 mg/1g - Prices
Unit description Cost Unit DesOwen Lot w/Cetaphil Cream 0.05% Kit Box 255.84USD box Desowen 0.05% ointment kit 217.2USD kit Desowen 0.05% cream kit 212.4USD kit DesOwen 0.05% Lotion 118ml Bottle 183.17USD bottle Desonide powder 152.39USD g DesOwen 0.05% Lotion 59ml Bottle 123.38USD bottle Desonide 0.05% Lotion 118ml Bottle 76.75USD bottle Desonide 0.05% Lotion 59ml Bottle 50.86USD bottle Desonide 0.05% Ointment 60 gm Tube 41.76USD tube Desonide 0.05% Cream 60 gm Tube 41.48USD tube Desonide 0.05% Ointment 15 gm Tube 16.09USD tube Desonide 0.05% Cream 15 gm Tube 16.07USD tube Desowen 0.05% cream 2.43USD g Desonide 0.05% cream 0.81USD g Desocort 0.05 % Ointment 0.32USD g Pms-Desonide 0.05 % Cream 0.28USD g Pms-Desonide 0.05 % Ointment 0.28USD g Desocort 0.05 % Lotion 0.16USD 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 US8460641 No 2013-06-11 2028-11-05 US US8962000 No 2015-02-24 2025-08-31 US US6730288 No 2004-05-04 2019-09-08 US US7029659 No 2006-04-18 2019-09-08 US US6387383 No 2002-05-14 2020-08-03 US US9492384 No 2016-11-15 2025-08-31 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 257-260 Bernstein, S. and Allen, G.R., Jr.; U.S. Patent 2,990,401; June 27, 1961; assigned to American Cyanamid Company. Diassi, P.A. and Principe, P.A.; U.S.Patent 3,549,498; December 22, 1970; assigned to E.R. Squibb & Sons, inc. water solubility Practically insoluble Not Available logP 1.4 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0594 mg/mL ALOGPS logP 2.31 ALOGPS logP 1.9 Chemaxon logS -3.8 ALOGPS pKa (Strongest Acidic) 13.75 Chemaxon pKa (Strongest Basic) -2.9 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 93.06 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 112.06 m3·mol-1 Chemaxon Polarizability 44.59 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9764 Blood Brain Barrier + 0.9382 Caco-2 permeable - 0.6162 P-glycoprotein substrate Substrate 0.7998 P-glycoprotein inhibitor I Non-inhibitor 0.5837 P-glycoprotein inhibitor II Inhibitor 0.6045 Renal organic cation transporter Non-inhibitor 0.7573 CYP450 2C9 substrate Non-substrate 0.8268 CYP450 2D6 substrate Non-substrate 0.9078 CYP450 3A4 substrate Substrate 0.7545 CYP450 1A2 substrate Non-inhibitor 0.909 CYP450 2C9 inhibitor Non-inhibitor 0.8729 CYP450 2D6 inhibitor Non-inhibitor 0.9544 CYP450 2C19 inhibitor Non-inhibitor 0.9521 CYP450 3A4 inhibitor Non-inhibitor 0.536 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9129 Ames test Non AMES toxic 0.8938 Carcinogenicity Non-carcinogens 0.949 Biodegradation Not ready biodegradable 0.9766 Rat acute toxicity 2.5316 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9573 hERG inhibition (predictor II) Non-inhibitor 0.67
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-1010-3976200000-f6fe91c3f6e1365460e0 Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0aos-0019300000-01815bbf8ebfd07f261f Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0001900000-17b6c8ca12503467a17d Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0a4i-0009200000-7116b5ae540ab754ddb0 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-05mk-1669100000-c198e63852fcb07f465e Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-0ap1-9648600000-06dbc00df26233321f42 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-056s-2693000000-9ab4d555bcd0712d785e Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 208.4013697 predictedDarkChem Lite v0.1.0 [M-H]- 207.5538697 predictedDarkChem Lite v0.1.0 [M-H]- 210.63345 predictedDeepCCS 1.0 (2019) [M+H]+ 207.6948697 predictedDarkChem Lite v0.1.0 [M+H]+ 207.7747697 predictedDarkChem Lite v0.1.0 [M+H]+ 212.52885 predictedDeepCCS 1.0 (2019) [M+Na]+ 206.8901697 predictedDarkChem Lite v0.1.0 [M+Na]+ 218.48996 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
- Russell GM, Henley DE, Leendertz J, Douthwaite JA, Wood SA, Stevens A, Woltersdorf WW, Peeters BW, Ruigt GS, White A, Veldhuis JD, Lightman SL: Rapid glucocorticoid receptor-mediated inhibition of hypothalamic-pituitary-adrenal ultradian activity in healthy males. J Neurosci. 2010 Apr 28;30(17):6106-15. doi: 10.1523/JNEUROSCI.5332-09.2010. [Article]
- Shaw JR, Gabor K, Hand E, Lankowski A, Durant L, Thibodeau R, Stanton CR, Barnaby R, Coutermarsh B, Karlson KH, Sato JD, Hamilton JW, Stanton BA: Role of glucocorticoid receptor in acclimation of killifish (Fundulus heteroclitus) to seawater and effects of arsenic. Am J Physiol Regul Integr Comp Physiol. 2007 Feb;292(2):R1052-60. Epub 2006 Oct 12. [Article]
- Otte C, Wust S, Zhao S, Pawlikowska L, Kwok PY, Whooley MA: Glucocorticoid receptor gene, low-grade inflammation, and heart failure: the Heart and Soul study. J Clin Endocrinol Metab. 2010 Jun;95(6):2885-91. doi: 10.1210/jc.2009-2251. Epub 2010 Apr 6. [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
Drug created at May 16, 2007 17:31 / Updated at September 15, 2024 21:55