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Identification
- Summary
Azathioprine is an immunosuppressant used to prevent renal transplant rejection, treat rheumatoid arthritis, Crohn's disease, and ulcerative colitis.
- Brand Names
- Azasan, Imuran
- Generic Name
- Azathioprine
- DrugBank Accession Number
- DB00993
- Background
Azathioprine is a prodrug of 6-mercaptopurine, first synthesized in 1956 by Gertrude Elion, William Lange, and George Hitchings in an attempt to produce a derivative of 6-mercaptopurine with a better therapeutic index.9,10,11 Azathioprine is used to treat inflammatory conditions like rheumatoid arthritis and as an immunosuppressant in the prevention of renal transplant rejection.12
Azathiprine was granted FDA approval on 20 March 1968.12
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Azathioprine (DB00993)
- Weight
- Average: 277.263
Monoisotopic: 277.038193193 - Chemical Formula
- C9H7N7O2S
- Synonyms
- 6-((1-Methyl-4-nitro-1H-imidazol-5-yl)thio)-1H-purine
- 6-(1'-Methyl-4'-nitro-5'-imidazolyl)-mercaptopurine
- Azamun
- Azathioprine
- Azathioprinum
- Azatioprina
- External IDs
- BW 57-322
- BW-57-322
- NSC-39084
Pharmacology
- Indication
Azathioprine is indicated to treat rheumatoid arthritis and prevent renal transplant rejection.12
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 Atopic dermatitis (ad) ••• ••••• Management of Crohn disease ••• ••••• Management of Immune thrombocytopenia ••• ••••• Prophylaxis of Kidney transplant rejection •••••••••••• Management of Lupus nephritis ••• ••••• - 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
Azathioprine is an immunosuppressive agent which functions through modulation of rac1 to induce T cell apoptosis, as well as other unknown immunosuppressive functions.5 It has a long duration of action as it is given daily, and has a narrow therapeutic index.12 Patients should be counselled regarding the risk of malignancies of the skin and lymphomas.12
- Mechanism of action
Azathioprine's mechanism of action is not entirely understood but it may be related to inhibition of purine synthesis, along with inhibition of B and T cells.5
6-thioguanine triphosphate, a metabolite of azathioprine, modulates activation of rac1 when costimulated with CD28, inducing T cell apoptosis.5 This may be mediated through rac1's action on mitogen-activated protein kinase, NF-kappaB.5
Target Actions Organism AAmidophosphoribosyltransferase inhibitorHumans URas-related C3 botulinum toxin substrate 1 modulatorHumans - Absorption
Oral azathioprine is well absorbed, with a Tmax of 1-2h.12 Further data regarding the absorption of azathioprine is not readily available.6,7
- Volume of distribution
Data regarding the volume of distribution of azathioprine is not readily available.6,7
- Protein binding
Azathioprine is 30%12 bound to proteins such as human serum albumin in circulation.1
- Metabolism
Azathioprine is converted to 6-mercaptopurine nonenzymatically.4 6-mercaptopurine is then metabolized to 6-methylmercaptopurine by thiopurine methyltransferase, 6-thiouric acid by xanthine oxidase, or 6-thiosine-5'-monophosphate by hypoxanthine phosphoribosyltransferase.4 6-thiosine-5'-monophosphate is metabolized to 6-methylthiosine-5'-monophosphate by thiopurine methyltransferase or 6-thioxanthylic acid by inosine monophosphate dehydrogenase.4 6-thioxanthylic acid is metabolized by guanosine monophosphate synthetase to 6-thioguanine monophosphate, the first of the 6-thioguanine nucleotides.4 6-thioguanine monophosphate is phosphorylated to produce the remaining 6-thioguanine nucleotides, 6-thioguanine diphosphate and 6-thioguanine triphosphate.4
Hover over products below to view reaction partners
- Route of elimination
Azathioprine and mercaptopurine are not detectable in urine after 8 hours.12 Further data regarding the route of elimination of azathioprine are not available.8
- Half-life
The half life of azathioprine is approximately 5 hours.12
- Clearance
Data regarding the clearance of azathioprine is not readily available.6,7
- 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
The oral LD50 in mice is 2500mg/kg and in rats is 400mg/kg.12
Patients experiencing an overdose may present with bone marrow hypoplasia, bleeding, and infection, which may progress to death.12 Patients should be treated with supportive and symptomatic treatments. 8 hour hemodialysis may remove 45% of a dose from serum.12
- Pathways
Pathway Category Azathioprine Action Pathway Drug action Azathioprine Metabolism Pathway Drug metabolism - Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Thiopurine S-methyltransferase TPMT*2 (G;G) / (C;G) G Allele ADR Directly Studied Patients with this genotype have reduced metabolism of azathioprine resulting in increased toxicity. Details Thiopurine S-methyltransferase TPMT*3A (A;A) / (A;G) A Allele ADR Directly Studied Patients with this genotype have reduced metabolism of azathioprine resulting in increased toxicity. Details Thiopurine S-methyltransferase TPMT*3C (G;G) / (A;G) G Allele ADR Directly Studied Patients with this genotype have reduced metabolism of azathioprine resulting in increased toxicity. Details Thiopurine S-methyltransferase TPMT*3B Not Available c.460G>A ADR Inferred Myelosuppression Details Thiopurine S-methyltransferase TPMT*4A Not Available G > A ADR Inferred Myelosuppression Details
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 softwareAbacavir Azathioprine may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Azathioprine can be increased when it is combined with Abametapir. Abatacept The metabolism of Azathioprine can be increased when combined with Abatacept. Abiraterone The serum concentration of Azathioprine can be increased when it is combined with Abiraterone. Aceclofenac Aceclofenac may decrease the excretion rate of Azathioprine which could result in a higher serum level. - Food Interactions
- Take with food. Food reduces irritation.
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.- Product Ingredients
Ingredient UNII CAS InChI Key Azathioprine sodium AM94R510MS 55774-33-9 WISNYKIQFMKSDQ-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Azamun (Ascent) / Azanin (Tanabe Mitsubishi Pharma) / Imurek (Aspen) / Imurel (GlaxoSmithKline)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Azathioprine Tablet 50 mg Oral Sanis Health Inc 2010-02-16 2017-07-31 Canada 
Azathioprine Tablet 50 mg / tab Oral Bdh Inc. 1998-10-08 2000-08-03 Canada Azathioprine Sodium for Injection Powder, for solution 100 mg / vial Intravenous Novopharm Limited Not applicable Not applicable Canada Azathioprine-50 Tablet 50 mg Oral Pro Doc Limitee 2009-06-10 2023-07-10 Canada Imuran Injection, powder, lyophilized, for solution 100 mg/1mL Intravenous Prometheus Laboratories 1974-07-19 2001-05-21 US 
- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-azathioprine Tablet 50 mg Oral Apotex Corporation 2000-10-17 Not applicable Canada Azasan Tablet 75 mg/1 Oral Salix Pharmaceuticals 2003-04-01 Not applicable US Azasan Tablet 100 mg/1 Oral Salix Pharmaceuticals 2003-04-01 Not applicable US Azathioprine Tablet 25 mg/1 Oral Zydus Pharmaceuticals USA Inc. 2017-12-02 Not applicable US Azathioprine Tablet 50 mg/1 Oral Roxane Laboratories 1996-02-16 2017-04-01 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image IMURAN 25 MG TABLET, 100 ADET Azathioprine (25 mg) Tablet Oral VLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ. 2018-05-29 Not applicable Turkey 
IMURAN 50 MG TABLET, 100 ADET Azathioprine (50 mg) Tablet Oral VLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ. 2018-05-29 Not applicable Turkey
Categories
- ATC Codes
- L04AX01 — Azathioprine
- Drug Categories
- Antimetabolites
- Antineoplastic and Immunomodulating Agents
- Antirheumatic Agents
- Carbohydrates
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Glycosides
- Heterocyclic Compounds, Fused-Ring
- Immunologic Factors
- Immunosuppressive Agents
- Immunotherapy
- Noxae
- Nucleic Acid Synthesis Inhibitors
- Nucleic Acids, Nucleotides, and Nucleosides
- Nucleosides
- P-glycoprotein substrates
- Purine Antimetabolite
- Purines
- Sulfhydryl Compounds
- Sulfur Compounds
- Thionucleosides
- Thiopurine Analogs
- Toxic Actions
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as diarylthioethers. These are organosulfur compounds containing a thioether group that is substituted by two aryl groups.
- Kingdom
- Organic compounds
- Super Class
- Organosulfur compounds
- Class
- Thioethers
- Sub Class
- Aryl thioethers
- Direct Parent
- Diarylthioethers
- Alternative Parents
- 6-thiopurines / Nitroimidazoles / Nitroaromatic compounds / Pyrimidines and pyrimidine derivatives / Imidolactams / N-substituted imidazoles / Heteroaromatic compounds / Sulfenyl compounds / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds show 6 more
- Substituents
- 6-thiopurine / Allyl-type 1,3-dipolar organic compound / Aromatic heteropolycyclic compound / Azacycle / Azole / C-nitro compound / Diarylthioether / Heteroaromatic compound / Hydrocarbon derivative / Imidazole show 19 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- C-nitro compound, aryl sulfide, imidazoles, thiopurine (CHEBI:2948)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- MRK240IY2L
- CAS number
- 446-86-6
- InChI Key
- LMEKQMALGUDUQG-UHFFFAOYSA-N
- InChI
- InChI=1S/C9H7N7O2S/c1-15-4-14-7(16(17)18)9(15)19-8-5-6(11-2-10-5)12-3-13-8/h2-4H,1H3,(H,10,11,12,13)
- IUPAC Name
- 6-[(1-methyl-4-nitro-1H-imidazol-5-yl)sulfanyl]-7H-purine
- SMILES
- CN1C=NC(=C1SC1=NC=NC2=C1NC=N2)[N+]([O-])=O
References
- General References
- Sochacka J: Docking of thiopurine derivatives to human serum albumin and binding site analysis with Molegro Virtual Docker. Acta Pol Pharm. 2014 Mar-Apr;71(2):343-9. [Article]
- Van Os EC, Zins BJ, Sandborn WJ, Mays DC, Tremaine WJ, Mahoney DW, Zinsmeister AR, Lipsky JJ: Azathioprine pharmacokinetics after intravenous, oral, delayed release oral and rectal foam administration. Gut. 1996 Jul;39(1):63-8. doi: 10.1136/gut.39.1.63. [Article]
- Anstey A, Lear JT: Azathioprine: clinical pharmacology and current indications in autoimmune disorders. BioDrugs. 1998 Jan;9(1):33-47. [Article]
- Dubinsky MC: Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety. Clin Gastroenterol Hepatol. 2004 Sep;2(9):731-43. [Article]
- Tiede I, Fritz G, Strand S, Poppe D, Dvorsky R, Strand D, Lehr HA, Wirtz S, Becker C, Atreya R, Mudter J, Hildner K, Bartsch B, Holtmann M, Blumberg R, Walczak H, Iven H, Galle PR, Ahmadian MR, Neurath MF: CD28-dependent Rac1 activation is the molecular target of azathioprine in primary human CD4+ T lymphocytes. J Clin Invest. 2003 Apr;111(8):1133-45. [Article]
- Stocco G, Martelossi S, Arrigo S, Barabino A, Aloi M, Martinelli M, Miele E, Knafelz D, Romano C, Naviglio S, Favretto D, Cuzzoni E, Franca R, Decorti G, Ventura A: Multicentric Case-Control Study on Azathioprine Dose and Pharmacokinetics in Early-onset Pediatric Inflammatory Bowel Disease. Inflamm Bowel Dis. 2017 Apr;23(4):628-634. doi: 10.1097/MIB.0000000000001051. [Article]
- Pelin M, Genova E, Fusco L, Marisat M, Hofmann U, Favretto D, Lucafo M, Taddio A, Martelossi S, Ventura A, Stocco G, Schwab M, Decorti G: Pharmacokinetics and pharmacodynamics of thiopurines in an in vitro model of human hepatocytes: Insights from an innovative mass spectrometry assay. Chem Biol Interact. 2017 Sep 25;275:189-195. doi: 10.1016/j.cbi.2017.08.009. Epub 2017 Aug 12. [Article]
- Schusziarra V, Ziekursch V, Schlamp R, Siemensen HC: Pharmacokinetics of azathioprine under haemodialysis. Int J Clin Pharmacol Biopharm. 1976 Dec;14(4):298-302. [Article]
- Wright S, Sanders DS, Lobo AJ, Lennard L: Clinical significance of azathioprine active metabolite concentrations in inflammatory bowel disease. Gut. 2004 Aug;53(8):1123-8. doi: 10.1136/gut.2003.032896. [Article]
- Elion GB: The purine path to chemotherapy. Science. 1989 Apr 7;244(4900):41-7. doi: 10.1126/science.2649979. [Article]
- Elion G, Lange W, Hitchings G: Studies on Condensed Pyrimidine Systems. XIII. Some Amino-substituted Derivatives of Guanine and 6-Thioguanine Journal of the American Chemical Society. 1956 Jan 1;78(1):217-220. [Article]
- FDA Approved Drug Products: Imuran Azathioprine Oral Tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0015128
- KEGG Drug
- D00238
- KEGG Compound
- C06837
- PubChem Compound
- 2265
- PubChem Substance
- 46508252
- ChemSpider
- 2178
- BindingDB
- 50373919
- 1256
- ChEBI
- 2948
- ChEMBL
- CHEMBL1542
- ZINC
- ZINC000004258316
- Therapeutic Targets Database
- DAP000782
- PharmGKB
- PA448515
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Azathioprine
- FDA label
- Download (212 KB)
- MSDS
- Download (75.4 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 Treatment End Stage Renal Disease (ESRD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Azathioprine / Inosine Triphosphate Pyrophosphatase / Polymorphism, Genetic / Thiopurine S-methyl Transferase (TPMT) 1 somestatus stop reason just information to hide Not Available Completed Not Available Renal Failure, Chronic Renal Failure 1 somestatus stop reason just information to hide Not Available Recruiting Not Available Children / Immunosuppressive Treatment / Lupus Nephritis / Steroid therapy 1 somestatus stop reason just information to hide Not Available Recruiting Not Available Ocular Myasthenia Gravis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Aaipharma llc
- Mylan pharmaceuticals inc
- Roxane laboratories inc
- Zydus pharmaceuticals usa inc
- Prometheus laboratories inc
- Bedford laboratories div ben venue laboratories inc
- Packagers
- AAIPharma Inc.
- Amerisource Health Services Corp.
- Bedford Labs
- Ben Venue Laboratories Inc.
- Cadila Healthcare Ltd.
- Cardinal Health
- Glenmark Generics Ltd.
- Heartland Repack Services LLC
- Mallinckrodt Inc.
- Medisca Inc.
- Mylan
- Nucare Pharmaceuticals Inc.
- Oso Biopharmaceuticals Manufacturing LLC
- Pharmedix
- Physicians Total Care Inc.
- Prometheus Laboratories Inc.
- Rebel Distributors Corp.
- Resolution Chemicals Ltd.
- Roxane Labs
- Salix Pharmaceuticals
- Sandoz
- UDL Laboratories
- Vangard Labs Inc.
- Xanodyne Pharmaceuticals Inc.
- Zydus Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet, film coated Oral 50 MG Tablet, film coated Oral 100 MG Tablet, film coated Oral 75 MG Tablet Oral 100 mg/1 Tablet Oral 75 mg/1 Tablet, film coated Oral 25 MG Powder Not applicable 1 g/1g Tablet Oral 25 mg/1 Tablet Oral 50 mg/1 Tablet Oral 50 1/1 Tablet Oral 50 mg / tab Tablet, film coated Oral 50 mg/1 Tablet Oral 50 mg Tablet Oral 50.0 mg Injection, powder, lyophilized, for solution Intravenous 100 mg/10mL Tablet, film coated Oral Injection, powder, lyophilized, for solution Intravenous 100 mg/1mL Powder, for solution Intravenous 50 mg / vial Tablet, coated Oral 50 mg Tablet Oral 25 mg Injection Intravenous 50 mg Powder, for solution Intravenous 100 mg / vial Suspension Oral 10 MG/ML Tablet Oral 50.000 mg Tablet Oral 50 mg/50mg - Prices
Unit description Cost Unit Azathioprine sod 100 mg vial 132.0USD vial Azathioprine powder 28.15USD g Azasan 100 mg tablet 5.8USD tablet Azasan 75 mg tablet 4.34USD tablet Imuran 50 mg Tablet 2.76USD tablet Azathioprine 50 mg tablet 0.94USD tablet Apo-Azathioprine 50 mg Tablet 0.57USD tablet Mylan-Azathioprine 50 mg Tablet 0.57USD tablet Novo-Azathioprine 50 mg Tablet 0.57USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 243.5 °C PhysProp water solubility Insoluble FDA label logP 0.10 HANSCH,C ET AL. (1995) pKa 7.87 (at 25 °C) MITRA,AK & NARURKAR,MM (1986) - Predicted Properties
Property Value Source Water Solubility 1.07 mg/mL ALOGPS logP 0.84 ALOGPS logP 1.17 Chemaxon logS -2.4 ALOGPS pKa (Strongest Acidic) 8.62 Chemaxon pKa (Strongest Basic) 2.16 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 115.42 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 69.94 m3·mol-1 Chemaxon Polarizability 24.37 Å3 Chemaxon Number of Rings 3 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 + 0.9607 Blood Brain Barrier + 0.9226 Caco-2 permeable + 0.5057 P-glycoprotein substrate Non-substrate 0.7766 P-glycoprotein inhibitor I Non-inhibitor 0.8049 P-glycoprotein inhibitor II Non-inhibitor 0.6683 Renal organic cation transporter Non-inhibitor 0.8493 CYP450 2C9 substrate Non-substrate 0.7861 CYP450 2D6 substrate Non-substrate 0.8273 CYP450 3A4 substrate Non-substrate 0.5944 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9231 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.9733 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7 Ames test AMES toxic 0.9152 Carcinogenicity Non-carcinogens 0.9182 Biodegradation Not ready biodegradable 0.9576 Rat acute toxicity 2.7519 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.7434 hERG inhibition (predictor II) Non-inhibitor 0.8449
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 166.5737147 predictedDarkChem Lite v0.1.0 [M-H]- 162.9815906 predictedDarkChem Lite v0.1.0 [M-H]- 162.1448147 predictedDarkChem Lite v0.1.0 [M-H]- 140.74017 predictedDeepCCS 1.0 (2019) [M+H]+ 167.2635147 predictedDarkChem Lite v0.1.0 [M+H]+ 165.7404921 predictedDarkChem Lite v0.1.0 [M+H]+ 163.8964147 predictedDarkChem Lite v0.1.0 [M+H]+ 143.63179 predictedDeepCCS 1.0 (2019) [M+Na]+ 166.7284147 predictedDarkChem Lite v0.1.0 [M+Na]+ 179.4226263 predictedDarkChem Lite v0.1.0 [M+Na]+ 163.1049147 predictedDarkChem Lite v0.1.0 [M+Na]+ 151.61162 predictedDeepCCS 1.0 (2019)
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Catalyzes the formation of phosphoribosylamine from phosphoribosylpyrophosphate (PRPP) and glutamine
- Specific Function
- 4 iron, 4 sulfur cluster binding
- Gene Name
- PPAT
- Uniprot ID
- Q06203
- Uniprot Name
- Amidophosphoribosyltransferase
- Molecular Weight
- 57398.52 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
- Unknown
- Actions
- Modulator
- General Function
- Plasma membrane-associated small GTPase which cycles between active GTP-bound and inactive GDP-bound states. In its active state, binds to a variety of effector proteins to regulate cellular responses such as secretory processes, phagocytosis of apoptotic cells, epithelial cell polarization, neurons adhesion, migration and differentiation, and growth-factor induced formation of membrane ruffles (PubMed:1643658, PubMed:23512198, PubMed:28886345, PubMed:22843693). Rac1 p21/rho GDI heterodimer is the active component of the cytosolic factor sigma 1, which is involved in stimulation of the NADPH oxidase activity in macrophages. Essential for the SPATA13-mediated regulation of cell migration and adhesion assembly and disassembly. Stimulates PKN2 kinase activity (PubMed:9121475). In concert with RAB7A, plays a role in regulating the formation of RBs (ruffled borders) in osteoclasts (PubMed:1643658). In podocytes, promotes nuclear shuttling of NR3C2; this modulation is required for a proper kidney functioning. Required for atypical chemokine receptor ACKR2-induced LIMK1-PAK1-dependent phosphorylation of cofilin (CFL1) and for up-regulation of ACKR2 from endosomal compartment to cell membrane, increasing its efficiency in chemokine uptake and degradation. In neurons, is involved in dendritic spine formation and synaptic plasticity (By similarity). In hippocampal neurons, involved in spine morphogenesis and synapse formation, through local activation at synapses by guanine nucleotide exchange factors (GEFs), such as ARHGEF6/ARHGEF7/PIX (PubMed:12695502). In synapses, seems to mediate the regulation of F-actin cluster formation performed by SHANK3. In neurons, plays a crucial role in regulating GABA(A) receptor synaptic stability and hence GABAergic inhibitory synaptic transmission through its role in PAK1 activation and eventually F-actin stabilization (By similarity)
- Specific Function
- Enzyme binding
- Gene Name
- RAC1
- Uniprot ID
- P63000
- Uniprot Name
- Ras-related C3 botulinum toxin substrate 1
- Molecular Weight
- 21449.895 Da
References
- Tiede I, Fritz G, Strand S, Poppe D, Dvorsky R, Strand D, Lehr HA, Wirtz S, Becker C, Atreya R, Mudter J, Hildner K, Bartsch B, Holtmann M, Blumberg R, Walczak H, Iven H, Galle PR, Ahmadian MR, Neurath MF: CD28-dependent Rac1 activation is the molecular target of azathioprine in primary human CD4+ T lymphocytes. J Clin Invest. 2003 Apr;111(8):1133-45. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Converts guanine to guanosine monophosphate, and hypoxanthine to inosine monophosphate. Transfers the 5-phosphoribosyl group from 5-phosphoribosylpyrophosphate onto the purine. Plays a central role in the generation of purine nucleotides through the purine salvage pathway
- Specific Function
- Guanine phosphoribosyltransferase activity
- Gene Name
- HPRT1
- Uniprot ID
- P00492
- Uniprot Name
- Hypoxanthine-guanine phosphoribosyltransferase
- Molecular Weight
- 24579.155 Da
References
- Dubinsky MC: Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety. Clin Gastroenterol Hepatol. 2004 Sep;2(9):731-43. [Article]
- Reuther LO, Sonne J, Larsen NE, Larsen B, Christensen S, Rasmussen SN, Tofteng F, Haaber A, Johansen N, Kjeldsen J, Schmiegelow K: Pharmacological monitoring of azathioprine therapy. Scand J Gastroenterol. 2003 Sep;38(9):972-7. doi: 10.1080/00365520310005082. [Article]
- FDA Approved Drug Products: Imuran Azathioprine Oral Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- May catalyze the hydrolysis of nucleoside triphosphates including dGTP, dTTP, dCTP, their oxidized forms like 8-oxo-dGTP and the prodrug thiopurine derivatives 6-thio-dGTP and 6-thio-GTP (PubMed:26238318). Could also catalyze the hydrolysis of some nucleoside diphosphate derivatives (PubMed:22556419, PubMed:26238318). Hydrolyzes oxidized nucleosides triphosphates like 8-oxo-dGTP in vitro, but the specificity and efficiency towards these substrates are low. Therefore, the potential in vivo sanitizing role of this enzyme, that would consist in removing oxidatively damaged forms of nucleosides to prevent their incorporation into DNA, is unclear (PubMed:22556419, PubMed:26238318). Through the hydrolysis of thioguanosine triphosphates may participate in the catabolism of thiopurine drugs (PubMed:25108385, PubMed:26238318). May also have a role in DNA synthesis and cell cycle progression by stabilizing PCNA (PubMed:19419956). Exhibits decapping activity towards dpCoA-capped RNAs in vitro (By similarity)
- Specific Function
- 8-oxo-7,8-dihydrodeoxyguanosine triphosphate pyrophosphatase activity
- Gene Name
- NUDT15
- Uniprot ID
- Q9NV35
- Uniprot Name
- Nucleotide triphosphate diphosphatase NUDT15
- Molecular Weight
- 18608.965 Da
References
- Reuther LO, Sonne J, Larsen NE, Larsen B, Christensen S, Rasmussen SN, Tofteng F, Haaber A, Johansen N, Kjeldsen J, Schmiegelow K: Pharmacological monitoring of azathioprine therapy. Scand J Gastroenterol. 2003 Sep;38(9):972-7. doi: 10.1080/00365520310005082. [Article]
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- FDA Approved Drug Products: Imuran Azathioprine Oral Tablets [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Has also low oxidase activity towards aldehydes (in vitro)
- Specific Function
- 2 iron, 2 sulfur cluster binding
- Gene Name
- XDH
- Uniprot ID
- P47989
- Uniprot Name
- Xanthine dehydrogenase/oxidase
- Molecular Weight
- 146422.99 Da
References
- Dubinsky MC: Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety. Clin Gastroenterol Hepatol. 2004 Sep;2(9):731-43. [Article]
- Reuther LO, Sonne J, Larsen NE, Larsen B, Christensen S, Rasmussen SN, Tofteng F, Haaber A, Johansen N, Kjeldsen J, Schmiegelow K: Pharmacological monitoring of azathioprine therapy. Scand J Gastroenterol. 2003 Sep;38(9):972-7. doi: 10.1080/00365520310005082. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the S-methylation of thiopurine drugs such as 6-mercaptopurine (also called mercaptopurine, 6-MP or its brand name Purinethol) and 6-thioguanine (also called tioguanine or 6-TG) using S-adenosyl-L-methionine as the methyl donor (PubMed:18484748, PubMed:657528). TPMT activity modulates the cytotoxic effects of thiopurine prodrugs. A natural substrate for this enzyme has yet to be identified
- Specific Function
- S-adenosyl-l-methionine binding
- Gene Name
- TPMT
- Uniprot ID
- P51580
- Uniprot Name
- Thiopurine S-methyltransferase
- Molecular Weight
- 28180.09 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Glutathione S-transferase that catalyzes the nucleophilic attack of the sulfur atom of glutathione on the electrophilic groups of a wide range of exogenous and endogenous compounds (Probable). Involved in the formation of glutathione conjugates of both prostaglandin A2 (PGA2) and prostaglandin J2 (PGJ2) (PubMed:9084911). It also catalyzes the isomerization of D5-androstene-3,17-dione (AD) into D4-androstene-3,17-dione and may therefore play an important role in hormone biosynthesis (PubMed:11152686). Through its glutathione-dependent peroxidase activity toward the fatty acid hydroperoxide (13S)-hydroperoxy-(9Z,11E)-octadecadienoate/13-HPODE it is also involved in the metabolism of oxidized linoleic acid (PubMed:16624487)
- Specific Function
- Fatty acid binding
- Gene Name
- GSTA1
- Uniprot ID
- P08263
- Uniprot Name
- Glutathione S-transferase A1
- Molecular Weight
- 25630.785 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Lucafo M, Stocco G, Martelossi S, Favretto D, Franca R, Malusa N, Lora A, Bramuzzo M, Naviglio S, Cecchin E, Toffoli G, Ventura A, Decorti G: Azathioprine Biotransformation in Young Patients with Inflammatory Bowel Disease: Contribution of Glutathione-S Transferase M1 and A1 Variants. Genes (Basel). 2019 Apr 4;10(4). pii: genes10040277. doi: 10.3390/genes10040277. [Article]
- Link [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the conjugation of glutathione to a large variety of electrophilic compounds
- Specific Function
- Glutathione transferase activity
- Gene Name
- GSTA2
- Uniprot ID
- P09210
- Uniprot Name
- Glutathione S-transferase A2
- Molecular Weight
- 25663.675 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Link [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Involved in the formation of glutathione conjugates of both prostaglandin A2 (PGA2) and prostaglandin J2 (PGJ2) (PubMed:9084911). Participates in the formation of novel hepoxilin regioisomers (PubMed:21046276)
- Specific Function
- Enzyme binding
- Gene Name
- GSTM1
- Uniprot ID
- P09488
- Uniprot Name
- Glutathione S-transferase Mu 1
- Molecular Weight
- 25711.555 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Lucafo M, Stocco G, Martelossi S, Favretto D, Franca R, Malusa N, Lora A, Bramuzzo M, Naviglio S, Cecchin E, Toffoli G, Ventura A, Decorti G: Azathioprine Biotransformation in Young Patients with Inflammatory Bowel Disease: Contribution of Glutathione-S Transferase M1 and A1 Variants. Genes (Basel). 2019 Apr 4;10(4). pii: genes10040277. doi: 10.3390/genes10040277. [Article]
- Link [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the conversion of inosine 5'-phosphate (IMP) to xanthosine 5'-phosphate (XMP), the first committed and rate-limiting step in the de novo synthesis of guanine nucleotides, and therefore plays an important role in the regulation of cell growth. Could also have a single-stranded nucleic acid-binding activity and could play a role in RNA and/or DNA metabolism. It may also have a role in the development of malignancy and the growth progression of some tumors
- Specific Function
- Dna binding
- Gene Name
- IMPDH1
- Uniprot ID
- P20839
- Uniprot Name
- Inosine-5'-monophosphate dehydrogenase 1
- Molecular Weight
- 55405.365 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the conversion of inosine 5'-phosphate (IMP) to xanthosine 5'-phosphate (XMP), the first committed and rate-limiting step in the de novo synthesis of guanine nucleotides, and therefore plays an important role in the regulation of cell growth (PubMed:7763314, PubMed:7903306). Could also have a single-stranded nucleic acid-binding activity and could play a role in RNA and/or DNA metabolism (PubMed:14766016). It may also have a role in the development of malignancy and the growth progression of some tumors
- Specific Function
- Dna binding
- Gene Name
- IMPDH2
- Uniprot ID
- P12268
- Uniprot Name
- Inosine-5'-monophosphate dehydrogenase 2
- Molecular Weight
- 55804.495 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Catalyzes the conversion of xanthine monophosphate (XMP) to GMP in the presence of glutamine and ATP through an adenyl-XMP intermediate
- Specific Function
- Atp binding
- Gene Name
- GMPS
- Uniprot ID
- P49915
- Uniprot Name
- GMP synthase [glutamine-hydrolyzing]
- Molecular Weight
- 76714.79 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Pyrophosphatase that hydrolyzes the non-canonical purine nucleotides inosine triphosphate (ITP), deoxyinosine triphosphate (dITP) as well as 2'-deoxy-N-6-hydroxylaminopurine triphosphate (dHAPTP) and xanthosine 5'-triphosphate (XTP) to their respective monophosphate derivatives. The enzyme does not distinguish between the deoxy- and ribose forms. Probably excludes non-canonical purines from RNA and DNA precursor pools, thus preventing their incorporation into RNA and DNA and avoiding chromosomal lesions
- Specific Function
- Ditp diphosphatase activity
- Gene Name
- ITPA
- Uniprot ID
- Q9BY32
- Uniprot Name
- Inosine triphosphate pyrophosphatase
- Molecular Weight
- 21445.495 Da
References
- Stocco G, Pelin M, Franca R, De Iudicibus S, Cuzzoni E, Favretto D, Martelossi S, Ventura A, Decorti G: Pharmacogenetics of azathioprine in inflammatory bowel disease: a role for glutathione-S-transferase? World J Gastroenterol. 2014 Apr 7;20(13):3534-41. doi: 10.3748/wjg.v20.i13.3534. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). 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) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:19965576, PubMed:9435160). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:11555828, PubMed:12865317). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2 (PubMed:11555828, PubMed:12865317). Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). May act as a major enzyme for all-trans retinoic acid biosynthesis in the liver. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376). Primarily catalyzes stereoselective epoxidation of the last double bond of polyunsaturated fatty acids (PUFA), displaying a strong preference for the (R,S) stereoisomer (PubMed:19965576). Catalyzes bisallylic hydroxylation and omega-1 hydroxylation of PUFA (PubMed:9435160). May also participate in eicosanoids metabolism by converting hydroperoxide species into oxo metabolites (lipoxygenase-like reaction, NADPH-independent) (PubMed:21068195). Plays a role in the oxidative metabolism of xenobiotics. Catalyzes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin (PubMed:14725854). Metabolizes caffeine via N3-demethylation (Probable)
- Specific Function
- Aromatase activity
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58406.915 Da
References
- Lampe JW, King IB, Li S, Grate MT, Barale KV, Chen C, Feng Z, Potter JD: Brassica vegetables increase and apiaceous vegetables decrease cytochrome P450 1A2 activity in humans: changes in caffeine metabolite ratios in response to controlled vegetable diets. Carcinogenesis. 2000 Jun;21(6):1157-62. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- Antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Sochacka J: Docking of thiopurine derivatives to human serum albumin and binding site analysis with Molegro Virtual Docker. Acta Pol Pharm. 2014 Mar-Apr;71(2):343-9. [Article]
- Tanaka M, Asahi Y, Masuda S, Ota T: Binding position of azathioprine with bovine serum albumin determined by measuring nuclear magnetic resonance relaxation time. Chem Pharm Bull (Tokyo). 1991 Nov;39(11):2771-4. doi: 10.1248/cpb.39.2771. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Bidirectional uniporter involved in the facilitative transport of nucleosides and nucleobases, and contributes to maintaining their cellular homeostasis (PubMed:10722669, PubMed:12527552, PubMed:12590919, PubMed:16214850, PubMed:21795683, PubMed:9396714, PubMed:9478986). Functions as a Na(+)-independent, passive transporter (PubMed:9478986). Involved in the transport of nucleosides such as inosine, adenosine, uridine, thymidine, cytidine and guanosine (PubMed:10722669, PubMed:12527552, PubMed:12590919, PubMed:16214850, PubMed:21795683, PubMed:9396714, PubMed:9478986). Also able to transport purine nucleobases (hypoxanthine, adenine, guanine) and pyrimidine nucleobases (thymine, uracil) (PubMed:16214850, PubMed:21795683). Involved in nucleoside transport at basolateral membrane of kidney cells, allowing liver absorption of nucleoside metabolites (PubMed:12527552). Mediates apical nucleoside uptake into Sertoli cells, thereby regulating the transport of nucleosides in testis across the blood-testis-barrier (PubMed:23639800). Mediates both the influx and efflux of hypoxanthine in skeletal muscle microvascular endothelial cells to control the amount of intracellular hypoxanthine available for xanthine oxidase-mediated ROS production (By similarity)
- Specific Function
- Adenine transmembrane transporter activity
- Gene Name
- SLC29A2
- Uniprot ID
- Q14542
- Uniprot Name
- Equilibrative nucleoside transporter 2
- Molecular Weight
- 50112.335 Da
References
- Conklin LS, Cuffari C, Okazaki T, Miao Y, Saatian B, Chen TE, Tse M, Brant SR, Li X: 6-Mercaptopurine transport in human lymphocytes: correlation with drug-induced cytotoxicity. J Dig Dis. 2012 Feb;13(2):82-93. doi: 10.1111/j.1751-2980.2011.00556.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-dependent, pyrimidine- and purine-selective (PubMed:11032837, PubMed:15861042, PubMed:16446384, PubMed:17140564, PubMed:21998139). Involved in the homeostasis of endogenous nucleosides (PubMed:11032837, PubMed:15861042). Exhibits the transport characteristics of the nucleoside transport system cib or N3 subtype (N3/cib) (with marked transport of both thymidine and inosine) (PubMed:11032837). Employs a 2:1 sodium/nucleoside ratio (PubMed:11032837). Transports uridine (PubMed:21795683). Also able to transport gemcitabine, 3'-azido-3'-deoxythymidine (AZT), ribavirin and 3-deazauridine (PubMed:11032837, PubMed:17140564)
- Specific Function
- Nucleoside
- Gene Name
- SLC28A3
- Uniprot ID
- Q9HAS3
- Uniprot Name
- Solute carrier family 28 member 3
- Molecular Weight
- 76929.61 Da
References
- Conklin LS, Cuffari C, Okazaki T, Miao Y, Saatian B, Chen TE, Tse M, Brant SR, Li X: 6-Mercaptopurine transport in human lymphocytes: correlation with drug-induced cytotoxicity. J Dig Dis. 2012 Feb;13(2):82-93. doi: 10.1111/j.1751-2980.2011.00556.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- Abc-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
- Conklin LS, Cuffari C, Okazaki T, Miao Y, Saatian B, Chen TE, Tse M, Brant SR, Li X: 6-Mercaptopurine transport in human lymphocytes: correlation with drug-induced cytotoxicity. J Dig Dis. 2012 Feb;13(2):82-93. doi: 10.1111/j.1751-2980.2011.00556.x. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent purine-selective nucleobase transporter which mediates the equilibrative transport of extracellular purine nucleobases such as adenine, guanine and hypoxanthine (PubMed:26455426, PubMed:32339528). May regulate fatty acid (FA) transport in adipocytes, acting as a positive regulator of FA efflux and as a negative regulator of FA uptake (By similarity)
- Specific Function
- Adenine transmembrane transporter activity
- Gene Name
- SLC43A3
- Uniprot ID
- Q8NBI5
- Uniprot Name
- Equilibrative nucleobase transporter 1
- Molecular Weight
- 54528.23 Da
References
- Ruel NM, Nguyen KH, Vilas G, Hammond JR: Characterization of 6-Mercaptopurine Transport by the SLC43A3-Encoded Nucleobase Transporter. Mol Pharmacol. 2019 Jun;95(6):584-596. doi: 10.1124/mol.118.114389. Epub 2019 Mar 25. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 14, 2024 04:03