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Identification
Name Dexamethasone
Accession Number DB01234 (APRD00674)
Type small molecule
Groups approved
Description

An anti-inflammatory 9-fluoro-glucocorticoid. [PubChem]
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
Desametasone
Desametasone [DCIT]
Desamethasone
Dexametasona [INN-Spanish]
Dexamethasone Acetate
Dexamethasone Sodium Phosphate
Dexamethasonum [INN-Latin]
Dexamethazone
Fluormethylprednisolone
Salts Not Available
Brand names
Name Company
Adexone
Aeroseb-D
Aeroseb-Dex
Anaflogistico
Aphtasolon
Aphthasolone
Auxiron
Azium
Bisu Ds
Calonat
Corson
Corsone
Cortisumman
Decacort
Decacortin
Decaderm
Decadron
Decadron Tablets, Elixir
Decadron-La
Decagel
Decalix
Decasone
Decaspray
Dectancyl
Dekacort
Deltafluorene
Dergramin
Deronil
Desadrene
Desameton
Deseronil
Dex-Ide
Dexa
Dexa Mamallet
Dexa-Cortidelt
Dexa-Cortisyl
Dexa-Mamallet
Dexa-Scheroson
Dexa-Sine
Dexacort
Dexacortal
Dexacortin
Dexadeltone
Dexafarma
Dexalona
Dexaltin
Dexameth
Dexamethasone Intensol
Dexamonozon
Dexapolcort
Dexapos
Dexaprol
Dexason
Dexasone
Dexinolon
Dexinoral
Dexone
Dexone 0.5
Dexone 0.75
Dexone 1.5
Dexone 4
Dexonium
Dextelan
Dezone
Dinormon
Fluormone
Fluorocort
Fortecortin
Gammacorten
Hexadecadrol
Hexadrol
Hexadrol Elixir
Hexadrol Tablets
Hl-Dex
IontoDex
Isopto-Dex
Lokalison F
Loverine
Luxazone
Maxidex
Mediamethasone
Mexidex
Millicorten
Mymethasone
Ocu-Trol
Oradexon
Pet Derm Iii
Pet-Derm Iii
Policort
Posurdex
Prednisolon F
Prednisolone F
Sk-Dexamethasone
Spoloven
Sunia Sol D
Superprednol
Turbinaire
Visumetazone
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Brand mixtures
Brand Name Ingredients
Ak Trol Suspension Dexamethasone + Neomycin Sulfate + Polymyxin B Sulfate
Ciprodex Ciprofloxacin (Ciprofloxacin Hydrochloride) + Dexamethasone
Cresophene Liq Camphor + Chlorophenol + Dexamethasone + Thymol
Dioptrol Ointment Dexamethasone + Neomycin Sulfate + Polymyxin B Sulfate
Dioptrol Suspension Dexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate
Endomethasone Ivory Dexamethasone + Hydrocortisone Acetate + Paraformaldehyde + Thymol Iodide
Maxitrol Dexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate
Maxitrol Ont Dexamethasone + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate
Naquasone Bolus Dexamethasone + Trichlormethiazide
Naquasone Inj Dexamethasone + Trichlormethiazide
Neodecadron Eye Ear Soln 0.1% Dexamethasone Phosphate (Dexamethasone Sodium Phosphate) + Neomycin Sulfate
Pendamine Chlorpheniramine Maleate + Dexamethasone + Dihydrostreptomycin Sulfate + Penicillin G Procaine
Sandoz Opticort Dexamethasone (Dexamethasone Sodium Metasulphobenzoate) + Framycetin Sulfate + Gramicidin
Septomixine Forte Dexamethasone + Halethazole Tartrate + Neomycin (Neomycin Sulfate) + Polymyxin B Sulfate + Tyrothricin
Sofracort Ear/Eye Ointment Dexamethasone + Framycetin Sulfate + Gramicidin
Sofracort Eye/Ear Drops Dexamethasone Sodium Metasulphobenzoate + Framycetin Sulfate + Gramicidin
Sofracort Sterile Ear/Eye Drops Dexamethasone (Dexamethasone Sodium Metasulphobenzoate) + Framycetin Sulfate + Gramicidin
Sofracort Sterile Ear/Eye Ointment Dexamethasone + Framycetin Sulfate + Gramicidin
Tobradex Oph Ointment Dexamethasone + Tobramycin
Tobradex Oph Sus Dexamethasone + Tobramycin
Tresaderm Dermatologic Solution Dexamethasone + Neomycin (Neomycin Sulfate) + Thiabendazole
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Categories
  • Anti-inflammatory Agents
  • Adrenergic Agents
  • Antiemetics
  • Antineoplastic Agents, Hormonal
  • Glucocorticoids
CAS number 50-02-2
Weight Average: 392.4611
Monoisotopic: 392.199902243
Chemical Formula C22H29FO5
InChI Key InChIKey=UREBDLICKHMUKA-CXSFZGCWSA-N
InChI
InChI=1S/C22H29FO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1
Plain Text
IUPAC Name
(1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
SMILES
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Steroids and Steroid Derivatives
Substructures
  • Steroids and Steroid Derivatives
  • Hydroxy Compounds
  • Alkanes and Alkenes
  • Alkyl Halides
  • Alcohols and Polyols
  • Ketones
Pharmacology
Indication Injection: for the treatment of endocrine disorders, rheumatic D=disorders, collagen diseases, dermatologic diseases, allergic statesc, ophthalmic diseases, gastrointestinal diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, cerebral edema.
Ophthalmic ointment and solution: for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe.
Ophthalmic solution only: for the treatment of steroid responsive inflammatory conditions of the external auditory meatus
Topic cream: for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses
Oral aerosol: for the treatment of bronchial asthma and related corticosteroid responsive bronchospastic states intractable to adequate trial of conventional therapy
Intranasal aerosol: for the treatment of allergic ot inflammatory nasal conditions, and nasal polyps
Pharmacodynamics Dexamethasone and its derivatives, dexamethasone sodium phosphate and dexamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties and ability to penetrate the CNS, dexamethasone is used alone to manage cerebral edema and with tobramycin to treat corticosteroid-responsive inflammatory ocular conditions.
Mechanism of action Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. This complex binds to DNA elements (glucocorticoid response elements) which results in a modification of transcription and, hence, protein synthesis in order to achieve inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The antiinflammatory actions of dexamethasone are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Absorption 80-90%
Volume of distribution Not Available
Protein binding 70%
Metabolism Hepatic.
Route of elimination Not Available
Half life 36-54 hours
Clearance Not Available
Toxicity Oral, rat LD50: >3 gm/kg. Signs of overdose include retinal toxicity, glaucoma, subcapsular cataract, gastrointestinal bleeding, pancreatitis, aseptic bone necrosis, osteoporosis, myopathies, obesity, edemas, hypertension, proteinuria, diabetes, sleep disturbances, psychiatric syndromes, delayed wound healing, atrophy and fragility of the skin, ecchymosis, and pseudotumor cerebri.
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Allergan herbert div allergan inc
  • Merck and co inc
  • Roxane laboratories inc
  • Alpharma us pharmaceuticals division
  • Sti pharma llc
  • Wockhardt eu operations (swiss) ag
  • Organon usa inc
  • Allergan inc
  • Watson laboratories inc
  • Alcon laboratories inc
  • Ecr pharmaceuticals
  • Impax laboratories inc
  • Mutual pharmaceutical co inc
  • Par pharmaceutical inc
  • Phoenix laboratories inc
  • Private formulations inc
  • Sandoz inc
  • Upsher smith laboratories inc
  • Whiteworth towne paulsen inc
  • Solvay pharmaceuticals
  • Merck research laboratories div merck co inc
  • Ucb inc
  • Central pharmaceuticals inc
  • Abraxis pharmaceutical products
  • App pharmaceuticals llc
  • Akorn inc
  • Akorn strides llc
  • Baxter healthcare corp anesthesia and critical care
  • Bel mar laboratories inc
  • Dell laboratories inc
  • International medication systems ltd
  • Luitpold pharmaceuticals inc
  • Teva parenteral medicines inc
  • Wyeth ayerst laboratories
  • Pharmafair inc
  • Sola barnes hind
  • Alcon universal ltd
  • Bausch and lomb pharmaceuticals inc
Packagers
Dosage forms
Form Route Strength
Elixir Oral
Liquid Intramuscular
Liquid Intravenous
Liquid Oral
Ointment Ophthalmic
Solution Intravenous
Solution Ophthalmic
Solution / drops Ophthalmic
Tablet Oral
Prices
Unit description Cost Unit
Ozurdex 0.7 mg implant 1554.0 USD implant
Maxidex 0.1% Suspension 15ml Bottle 97.96 USD bottle
Maxitrol 0.1-5-10000 Ointment 3.5 gm Tube 87.3 USD tube
Maxitrol 5-10000-0.1 Suspension 5ml Bottle 75.88 USD bottle
Maxidex 0.1% Suspension 5ml Bottle 53.57 USD bottle
Dexamethasone Sodium Phosphate 4 mg/ml Solution (1 Box = 25x1ml Vials) 41.99 USD box
Dexamethasone micronized powd 41.31 USD g
Dexamethasone powder 21.27 USD g
Dexamethasone Sodium Phosphate 0.1% Solution 5ml Bottle 19.99 USD bottle
Dexamethasone acetate powd 15.12 USD g
Dexamethasone sod ph powder 14.24 USD g
Dexamethasone Sodium Phosphate 4 mg/ml Solution 5ml Vial 13.99 USD vial
Dexamethasone Sodium Phosphate 10 mg/ml 4.78 USD ml
Dexamethasone Sodium Phosphate 4 mg/ml 1 Vial = 5ml 4.0 USD ml
Dexamethasone 0.1% eye drop 3.43 USD ml
Dexasol 0.1% eye drops 3.38 USD ml
Maxidex 0.1 % Ointment 2.69 USD g
Dexamethasone 10 mg/ml vial 2.56 USD ml
Maxidex 0.1% eye drops 2.36 USD ml
Dexamethasone Sodium Phosphate 4 mg/ml 1.77 USD ml
Maxidex 0.1 % Suspension 1.73 USD ml
Sandoz Dexamethasone Sod. Phosphate 0.1 % Solution 1.38 USD ml
Pms-Dexamethasone Sodium Phosp 10 mg/ml 1.34 USD ml
Dexamethasone 4 mg/ml vial 1.04 USD ml
Dexamethasone 6 mg tablet 1.01 USD tablet
Dexasone 4 mg Tablet 0.86 USD tablet
Apo-Dexamethasone 4 mg Tablet 0.8 USD tablet
Pms-Dexamethasone 4 mg Tablet 0.8 USD tablet
Ratio-Dexamethasone 4 mg Tablet 0.8 USD tablet
Dexamethasone 2 mg tablet 0.68 USD tablet
Dexamethasone 1 mg/1 ml soln 0.65 USD ml
Dexamethasone 4 mg tablet 0.6 USD tablet
Dexamethasone 1 mg tablet 0.49 USD tablet
Pms-Dexamethasone 0.75 mg Tablet 0.47 USD tablet
Pms-Dexamethasone 2 mg Tablet 0.43 USD tablet
Dexamethasone 0.5 mg/5ml Elixir 0.4 USD ml
Dexamethasone 0.75 mg tablet 0.38 USD tablet
Dexamethasone 1.5 mg tablet 0.35 USD tablet
Dexamethasone 0.5 mg tablet 0.31 USD tablet
Apo-Dexamethasone 0.5 mg Tablet 0.21 USD tablet
Pms-Dexamethasone 0.5 mg Tablet 0.2 USD tablet
Ratio-Dexamethasone 0.5 mg Tablet 0.18 USD tablet
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DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Country Patent Number Approved Expires (estimated)
United States 6899717 2003-11-01 2023-11-01
United States 6726918 2000-10-20 2020-10-20
Properties
State solid
Experimental Properties
Property Value Source
melting point 262 °C PhysProp
water solubility 89 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 1.83 HANSCH,C ET AL. (1995)
logS -3.64 ADME Research, USCD
Caco2 permeability -4.75 ADME Research, USCD
Predicted Properties
Property Value Source
water solubility 5.05e-02 g/l ALOGPS
logP 1.93 ALOGPS
logP 1.68 ChemAxon
logS -3.9 ALOGPS
pKa (strongest acidic) 12.42 ChemAxon
pKa (strongest basic) -3.3 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 94.83 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 102.49 ChemAxon
polarizability 40.83 ChemAxon
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
KEGG Drug D00292 Link_out
PubChem Compound 5743 Link_out
PubChem Substance 46508930 Link_out
ChemSpider 5541 Link_out
BindingDB 18207 Link_out
ChEBI 41879 Link_out
ChEMBL 41879 Link_out
Therapeutic Targets Database DAP000007 Link_out
PharmGKB PA449247 Link_out
IUPHAR 2768 Link_out
Guide to Pharmacology 2768 Link_out
HET DEX Link_out
Drug Product Database 664227 Link_out
RxList http://www.rxlist.com/cgi/generic/dexameth.htm Link_out
Drugs.com http://www.drugs.com/cdi/dexamethasone-drops.html Link_out
PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dec1118.shtml Link_out
Wikipedia http://en.wikipedia.org/wiki/Dexamethasone Link_out
ATC Codes
  • A01AC02
  • C05AA09
  • D07AB19
  • D07XB05
  • D10AA03
  • H02AB02
  • R01AD03
  • S01BA01
  • S01CB01
  • S02BA06
  • S03BA01
AHFS Codes
  • 52:08.08
  • 68:04.00
PDB Entries Not Available
FDA label show (96 KB)
MSDS show (74.8 KB)
Interactions
Drug Interactions
Drug Interaction
Acenocoumarol The corticosteroid, dexamethasone, alters the anticoagulant effect, acenocoumarol.
Acetylsalicylic acid The corticosteroid, dexamethasone, may decrease the effect of the salicylate, acetylsalicylic acid.
Ambenonium The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, ambenonium.
Aminoglutethimide Aminoglutethimide may decrease the effect of dexamethasone.
Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Anisindione The corticosteroid, dexamethasone, alters the anticoagulant effect of anisindione.
Aprepitant Aprepitant may increase the effect and toxicity of dexamethasone.
Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, dexamethasone.
Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, dexamethasone.
Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, dexamethasone.
Dabigatran etexilate P-Glycoprotein inducers such as dexamethasone may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
Dicumarol The corticosteroid, dexamethasone, alters the anticoagulant effect of dicumarol.
Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, dexamethasone.
Edrophonium The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, edrophonium.
Estradiol valerate/Dienogest Affects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, dexamethasone.
Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, dexamethasone.
Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, dexamethasone.
Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Imatinib Dexamethasone may decrease levels of imatinib.
Lurasidone Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated. Will decrease Cmax of lurasidone by 85%.
Magnesium salicylate The corticosteroid, dexamethasone, may decrease the effect of magnesium salicylate.
Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, dexamethasone.
Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, dexamethasone.
Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Midodrine Increased arterial pressure
Neostigmine The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, neostigmine.
Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, dexamethasone.
Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, dexamethasone.
Pyridostigmine The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, dexamethasone.
Rifampin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, dexamethasone.
Rilpivirine Strong inducers of CYP3A4 decrease the exposure of rilpivirine thus decreasing efficacy.
Roflumilast Affects CYP3A4 metabolism, decreases level or effect of roflumilast.
Salsalate The corticosteroid, dexamethasone, may decrease the effect of the salicylate, salsalate.
Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, dexamethasone.
Sunitinib Possible decrease in sunitinib levels
Tacrine Tacrine and Dexamethasone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
Talbutal The barbiturate, talbutal, may decrease the effect of the corticosteroid, dexamethasone.
Telithromycin Co-administration may cause decreased Telithromycin and increased Dexamethasone plasma concentrations. Consider alternate therapy.
Temsirolimus Dexamethasone may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
Thalidomide Increased risk of dermatologic adverse effects and venous thromboembolic events (VTE). Consider VTE prophylaxis during concomitant therapy and monitor for adverse dematologic effects.
Tramadol Dexamethasone may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Trazodone The CYP3A4 inducer, Dexamethasone, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Dexamethasone is initiated, discontinued or dose changed.
Vandetanib Decreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Dexamethasone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of dexamethasone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of dexamethasone if voriconazole is initiated, discontinued or dose changed.
Warfarin The corticosteroid, dexamethasone, alters the anticoagulant effect of warfarin.
Food Interactions
  • Avoid alcohol.
  • Avoid taking with grapefruit juice.
  • Take with food to reduce irritation.
Targets

1. Glucocorticoid receptor

Pharmacological action: yes
Actions: agonist

Receptor for glucocorticoids (GC). Has a dual mode of action:as a transcription factor that binds to glucocorticoid response elements (GRE) and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. 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

Organism class: human
UniProt ID: P04150 Link_out
Gene: NR3C1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Warne JP, John CD, Christian HC, Morris JF, Flower RJ, Sugden D, Solito E, Gillies GE, Buckingham JC: Gene deletion reveals roles for annexin A1 in the regulation of lipolysis and IL-6 release in epididymal adipose tissue. Am J Physiol Endocrinol Metab. 2006 Dec;291(6):E1264-73. Epub 2006 Jul 11. Pubmed
  2. Grossman R, Yehuda R, Golier J, McEwen B, Harvey P, Maria NS: Cognitive effects of intravenous hydrocortisone in subjects with PTSD and healthy control subjects. Ann N Y Acad Sci. 2006 Jul;1071:410-21. Pubmed
  3. Funato H, Kobayashi A, Watanabe Y: Differential effects of antidepressants on dexamethasone-induced nuclear translocation and expression of glucocorticoid receptor. Brain Res. 2006 Oct 30;1117(1):125-34. Epub 2006 Sep 7. Pubmed
  4. Vaitkuviene A, Ulinskaite A, Meskys R, Duburs G, Klusa V, Liutkevicius E: Study of the interaction of 1,4-dihydropyridine derivatives with glucocorticoid hormone receptors from the rat liver. Pharmacol Rep. 2006 Jul-Aug;58(4):551-8. Pubmed
  5. Wang D, Zhang H, Lang F, Yun CC: Acute activation of NHE3 by dexamethasone correlates with activation of SGK1 and requires a functional glucocorticoid receptor. Am J Physiol Cell Physiol. 2007 Jan;292(1):C396-404. Epub 2006 Sep 13. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Nuclear receptor 0B1

Pharmacological action: unknown
Actions: stimulator

Receptor that may be a component of a cascade required for development of steroidogenic tissues. Acts as a dominant negative regulator of transcription mediated by the retinoic acid receptor

Organism class: human
UniProt ID: P51843 Link_out
Gene: NR0B1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Gummow BM, Scheys JO, Cancelli VR, Hammer GD: Reciprocal regulation of a glucocorticoid receptor-steroidogenic factor-1 transcription complex on the Dax-1 promoter by glucocorticoids and adrenocorticotropic hormone in the adrenal cortex. Mol Endocrinol. 2006 Nov;20(11):2711-23. Epub 2006 Jul 20. Pubmed
  2. Yu CC, Li PH: In vivo inhibition of steroidogenic acute regulatory protein expression by dexamethasone parallels induction of the negative transcription factor DAX-1. Endocrine. 2006 Dec;30(3):313-23. Pubmed

3. Annexin A1

Pharmacological action: unknown
Actions: agonist

Calcium/phospholipid-binding protein which promotes membrane fusion and is involved in exocytosis. This protein regulates phospholipase A2 activity. It seems to bind from two to four calcium ions with high affinity

Organism class: human
UniProt ID: P04083 Link_out
Gene: ANXA1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Morand EF, Hall P, Hutchinson P, Yang YH: Regulation of annexin I in rheumatoid synovial cells by glucocorticoids and interleukin-1. Mediators Inflamm. 2006;2006(2):73835. Pubmed
  2. John CD, Theogaraj E, Christian HC, Morris JF, Smith SF, Buckingham JC: Time-specific effects of perinatal glucocorticoid treatment on anterior pituitary morphology, annexin 1 expression and adrenocorticotrophic hormone secretion in the adult female rat. J Neuroendocrinol. 2006 Dec;18(12):949-59. Pubmed
  3. Davies E, Omer S, Buckingham JC, Morris JF, Christian HC: Expression and externalization of annexin 1 in the adrenal gland: structure and function of the adrenal gland in annexin 1-null mutant mice. Endocrinology. 2007 Mar;148(3):1030-8. Epub 2006 Dec 7. Pubmed
  4. Wang C, Wang J, Guo HF, Liu RY: Involvement of annexin I in the dexamethasone-mediated upregulation of A549 cells phagocytosis of apoptotic eosinophils. Immunol Lett. 2007 Aug 15;111(2):103-10. Epub 2007 Jul 2. Pubmed

4. Nitric oxide synthase, inducible

Pharmacological action: unknown
Actions: negative modulator

Produces nitric oxide (NO) which is a messenger molecule with diverse functions throughout the body. In macrophages, NO mediates tumoricidal and bactericidal actions

Organism class: human
UniProt ID: P35228 Link_out
Gene: NOS2A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Soderberg M, Raffalli-Mathieu F, Lang MA: Regulation of the murine inducible nitric oxide synthase gene by dexamethasone involves a heterogeneous nuclear ribonucleoprotein I (hnRNPI) dependent pathway. Mol Immunol. 2007 May;44(12):3204-10. Epub 2007 Mar 26. Pubmed
  2. Huang H, Lavoie-Lamoureux A, Moran K, Lavoie JP: IL-4 stimulates the expression of CXCL-8, E-selectin, VEGF, and inducible nitric oxide synthase mRNA by equine pulmonary artery endothelial cells. Am J Physiol Lung Cell Mol Physiol. 2007 May;292(5):L1147-54. Pubmed
  3. Nandi J, Saud B, Zinkievich JM, Palma DT, Levine RA: 5-Aminosalicylic Acid Improves Indomethacin-Induced Enteropathy by Inhibiting iNOS Transcription in Rats. Dig Dis Sci. 2007 May 15;. Pubmed
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
Enzymes

1. Cytochrome P450 3A4

Actions: substrate, inhibitor, inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Ekins S, Bravi G, Wikel JH, Wrighton SA: Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther. 1999 Oct;291(1):424-33. Pubmed

2. Cytochrome P450 3A5

Actions: substrate, inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P20815 Link_out
Gene: CYP3A5 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 3A7

Actions: substrate, inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P24462 Link_out
Gene: CYP3A7 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 2C9

Actions: inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cholesterol side-chain cleavage enzyme, mitochondrial

Actions: inhibitor

Catalyzes the side-chain cleavage reaction of cholesterol to pregnenolone

UniProt ID: P05108 Link_out
Gene: CYP11A1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

6. Cytochrome P450 17A1

Actions: inhibitor

Conversion of pregnenolone and progesterone to their 17- alpha-hydroxylated products and subsequently to dehydroepiandrosterone (DHEA) and androstenedione. Catalyzes both the 17-alpha-hydroxylation and the 17,20-lyase reaction. Involved in sexual development during fetal life and at puberty

UniProt ID: P05093 Link_out
Gene: CYP17A1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 19A1

Actions: inducer

Catalyzes the formation of aromatic C18 estrogens from C19 androgens

UniProt ID: P11511 Link_out
Gene: CYP19A1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 1A1

Actions: inhibitor, inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P04798 Link_out
Gene: CYP1A1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 1B1

Actions: inducer

Participates in the metabolism of an as-yet-unknown biologically active molecule that is a participant in eye development

UniProt ID: Q16678 Link_out
Gene: CYP1B1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

10. Cytochrome P450 2A6

Actions: inducer

Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase

UniProt ID: P11509 Link_out
Gene: CYP2A6
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

11. Cytochrome P450 2B6

Actions: inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics

UniProt ID: P20813 Link_out
Gene: CYP2B6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

12. Cytochrome P450 2C19

Actions: inducer

Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine

UniProt ID: P33261 Link_out
Gene: CYP2C19 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

13. Cytochrome P450 2C8

Actions: inducer

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme responsible for the metabolism the anti- cancer drug paclitaxel (taxol)

UniProt ID: P10632 Link_out
Gene: CYP2C8
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

14. Cytochrome P450 2D6

Actions: inducer

Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants

UniProt ID: P10635 Link_out
Gene: CYP2D6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

15. Cytochrome P450 2E1

Actions: inducer

Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms

UniProt ID: P05181 Link_out
Gene: CYP2E1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

16. Cytochrome P450 3A43

Actions: inducer

Exhibits low testosterone 6-beta-hydroxylase activity

UniProt ID: Q9HB55 Link_out
Gene: CYP3A43 Link_out
Protein Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

17. Cytochrome P450 4A11

Actions: inducer

Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity towards prostaglandins A1 and E1

UniProt ID: Q02928 Link_out
Gene: CYP4A11 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
Transporters

1. Bile salt export pump

Actions: inducer

Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes

UniProt ID: O95342 Link_out
Gene: ABCB11 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Fardel O, Payen L, Courtois A, Vernhet L, Lecureur V: Regulation of biliary drug efflux pump expression by hormones and xenobiotics. Toxicology. 2001 Oct 5;167(1):37-46. Pubmed

2. Multidrug resistance protein 1

Actions: substrate, inhibitor, inducer

Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells

UniProt ID: P08183 Link_out
Gene: ABCB1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Geick A, Eichelbaum M, Burk O: Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem. 2001 May 4;276(18):14581-7. Epub 2001 Jan 31. Pubmed
  2. Romiti N, Tramonti G, Chieli E: Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol. 2002 Sep 1;183(2):83-91. Pubmed
  3. Schuetz JD, Silverman JA, Thottassery JV, Furuya KN, Schuetz EG: Divergent regulation of the class II P-glycoprotein gene in primary cultures of hepatocytes versus H35 hepatoma by glucocorticoids. Cell Growth Differ. 1995 Oct;6(10):1321-32. Pubmed
  4. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. Pubmed
  5. Schwab D, Fischer H, Tabatabaei A, Poli S, Huwyler J: Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery. J Med Chem. 2003 Apr 24;46(9):1716-25. Pubmed
  6. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. Pubmed
  7. Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. Pubmed
  8. Schinkel AH, Wagenaar E, van Deemter L, Mol CA, Borst P: Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest. 1995 Oct;96(4):1698-705. Pubmed

3. Canalicular multispecific organic anion transporter 1

Actions: inducer

Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter

UniProt ID: Q92887 Link_out
Gene: ABCC2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Demeule M, Jodoin J, Beaulieu E, Brossard M, Beliveau R: Dexamethasone modulation of multidrug transporters in normal tissues. FEBS Lett. 1999 Jan 15;442(2-3):208-14. Pubmed
  2. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. Pubmed

4. Solute carrier organic anion transporter family member 1A2

Actions: inhibitor

Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity)

UniProt ID: P46721 Link_out
Gene: SLCO1A2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Kullak-Ublick GA, Fisch T, Oswald M, Hagenbuch B, Meier PJ, Beuers U, Paumgartner G: Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain. FEBS Lett. 1998 Mar 13;424(3):173-6. Pubmed
  2. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. Pubmed

5. ATP-binding cassette sub-family G member 2

Actions: inhibitor

Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. May be involved in brain-to-blood efflux. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. When overexpressed, the transfected cells become resistant to mitoxantrone, daunorubicin and doxorubicin, display diminished intracellular accumulation of daunorubicin, and manifest an ATP- dependent increase in the efflux of rhodamine 123

UniProt ID: Q9UNQ0 Link_out
Gene: ABCG2 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Elahian F, Kalalinia F, Behravan J: Evaluation of indomethacin and dexamethasone effects on BCRP-mediated drug resistance in MCF-7 parental and resistant cell lines. Drug Chem Toxicol. 2010 Apr;33(2):113-9. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:20