Identification

Name
Cisplatin
Accession Number
DB00515
Description

Cisplatin, cisplatinum or cis-diamminedichloroplatinum(II) (CDDP) is a platinum-based chemotherapy drug used to treat various types of cancers, including sarcomas, some carcinomas (e.g. small cell lung cancer, and ovarian cancer), lymphomas and germ cell tumors. It was the first member of its class, which now also includes carboplatin and oxaliplatin.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 300.05
Monoisotopic: 298.955596
Chemical Formula
Cl2H6N2Pt
Synonyms
  • CDDP
  • Cis-DDP
  • cis-diamminedichloroplatinum(II)
  • Cisplatin
  • cisplatino

Pharmacology

Indication

For the treatment of metastatic testicular tumors, metastatic ovarian tumors and advanced bladder cancer.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Cisplatin is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.

Mechanism of action

Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.

TargetActionsOrganism
ADNA
cross-linking/alkylation
Humans
UDNA-3-methyladenine glycosylaseNot AvailableHumans
UAlpha-2-macroglobulinNot AvailableHumans
USerotransferrinNot AvailableHumans
UCopper transport protein ATOX1Not AvailableHumans
Absorption

Following cisplatin doses of 20 to 120 mg/m^2, the concentrations of platinum are highest in liver, prostate, and kidney; somewhat lower in bladder, muscle, testicle, pancreas, and spleen; and lowest in bowel, adrenal, heart, lung, cerebrum, and cerebellum. Platinum is present in tissues for as long as 180 days after the last administration.

Volume of distribution

Volume of distribution at steady state = 11-12 L/m^2

Protein binding

Cisplatin does not undergo instantaneous and reversible binding to plasma protein that is characteristic of normal drug-protein binding. However, the platinum itself is capable of binding to plasma proteins, including albumin, transferrin, and gamma globulin. Three hours after a bolus injection and two hours after the end of a three-hour infusion, 90% of the plasma platinum is protein bound.

Metabolism
Not Available
Route of elimination

The parent compound, cisplatin, is excreted in the urine. Although small amounts of platinum are present in the bile and large intestine after administration of cisplatin, the fecal excretion of platinum appears to be insignificant.

Half-life

Cisplatin decays monoexponentially with a half life of 20 to 30 minutes following administrations of 50 or 100 mg/m^2. Cisplatin has a plasma half-life of 30 minutes. The complexes between albumin and the platinum from cisplatin do not dissociate to a significant extent and are slowly eliminated with a minimum half-life of five days or more.

Clearance
  • 15-16 L/h/m^2 [total body clearance, 7-hour infusion of 100 mg/m^2]
  • 62 mL/min/m^2 [renal clearance, 2-hour infusion of 100 mg/m^2]
  • 50 mL/min/m^2 [renal clearance, 6- to 7-hour infusion of 100 mg/m^2] The renal clearance of free (ultrafilterable) platinum also exceeds the glomerular filtration rate indicating that cisplatin or other platinum-containing molecules are actively secreted by the kidneys. The renal clearance of free platinum is nonlinear and variable and is dependent on dose, urine flow rate, and individual variability in the extent of active secretion and possible tubular reabsorption.
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Glutathione S-transferase Mu 1GSTM1Not Availablepresence of functional GSTM1ADR Directly StudiedPatients with this genotype have increased risk of ototoxicity with [durg: cisplatin].Details
Low-density lipoprotein receptor-related protein 2---(A;A) / (A;G)---ADR Directly StudiedPatients with this genotype have increased risk of ototoxicity with [durg: cisplatin].Details
Glutathione S-transferase P---(A;G) / (G;G)---ADR Directly StudiedPatients with this genotype have increased risk of ototoxicity with [durg: cisplatin].Details
DNA repair protein complementing XP-C cells---(C;C)---ADR Directly StudiedPatients with this genotype have increased risk of ototoxicity with [durg: cisplatin].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.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Cisplatin which could result in a higher serum level.
AbataceptThe risk or severity of adverse effects can be increased when Cisplatin is combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Cisplatin.
AcarboseAcarbose may decrease the excretion rate of Cisplatin which could result in a higher serum level.
AcebutololCisplatin may increase the bradycardic activities of Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Cisplatin which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Cisplatin which could result in a higher serum level.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Cisplatin.
AcetaminophenAcetaminophen may decrease the excretion rate of Cisplatin which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Cisplatin which could result in a lower serum level and potentially a reduction in efficacy.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
  • Avoid echinacea. Echinacea should be used with caution, if at all, in patients receiving therapeutic immunosuppressants. Monitor for reduced efficacy of the immunosuppressant during concomitant use.

Products

International/Other Brands
Abiplatin / Cisplatyl / Platidiam / Platin (Cadila Healthcare)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CisplatinInjection, powder, lyophilized, for solution1 mg/1mLIntravenousWG Critical Care, LLC2019-04-05Not applicableUS flag
CISplatinInjection, solution1 mg/1mLIntravenousWG Critical Care, LLC2012-01-13Not applicableUS flag
CISplatinInjection, solution1 mg/1mLIntravenousWG Critical Care, LLC2015-04-15Not applicableUS flag
CISplatinInjection, solution1 mg/1mLIntravenousWG Critical Care, LLC2012-01-13Not applicableUS flag
Cisplatin Inj 0.5mg/mlLiquidIntravenousDavid Bull Laboratories (Pty) Ltd.1985-12-311996-09-10Canada flag
Cisplatin Inj 1mg/mlLiquidIntravenousDavid Bull Laboratories (Pty) Ltd.1986-12-311998-08-13Canada flag
Cisplatin InjectionSolutionIntravenousOmega Laboratories LtdNot applicableNot applicableCanada flag
Cisplatin InjectionSolutionIntravenousStrides Pharma Canada IncNot applicableNot applicableCanada flag
Cisplatin InjectionSolutionIntravenousFresenius KabiNot applicableNot applicableCanada flag
Cisplatin InjectionSolutionIntravenousTEVA Canada Limited2013-08-29Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CisplatinInjection1 mg/1mLIntravenousPfizer Laboratories Div Pfizer Inc.2012-04-192016-12-31US flag
CISplatinInjection1 mg/1mLIntravenousWest-Ward Pharmaceuticals Corp2000-11-07Not applicableUS flag
CisplatinInjection1 mg/1mLIntravenousBluePoint Laboratories2016-08-02Not applicableUS flag
CisplatinInjection, solution1 mg/1mLIntravenousBedford Pharmaceuticals2004-10-012011-01-31US flag
CisplatinInjection, solution1 mg/1mLIntravenousGland Pharma Limited2017-04-03Not applicableUS flag
CisplatinInjection, solution1 mg/1mLIntravenousAthenex Pharmaceutical Division, Llc.2017-06-12Not applicableUS flag
CisplatinInjection, solution50 mg/50mLIntravenousAlvogen Inc.2017-09-252020-03-01US flag
CisplatinInjection, solution1 mg/1mLIntravenousBedford Pharmaceuticals2004-10-082010-10-31US flag
CisplatinInjection1 mg/1mLIntravenousMylan Institutional2012-04-192017-12-31US flag
CisplatinInjection, solution100 mg/100mLIntravenousTeva Parenteral Medicines, Inc.2000-06-01Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more

Categories

ATC Codes
L01XA01 — Cisplatin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of inorganic compounds known as transition metal chlorides. These are inorganic compounds in which the largest halogen atom is Chlorine, and the heaviest metal atom is a transition metal.
Kingdom
Inorganic compounds
Super Class
Mixed metal/non-metal compounds
Class
Transition metal salts
Sub Class
Transition metal chlorides
Direct Parent
Transition metal chlorides
Alternative Parents
Inorganic chloride salts
Substituents
Inorganic chloride salt / Inorganic salt / Transition metal chloride
Molecular Framework
Not Available
External Descriptors
diamminedichloroplatinum (CHEBI:27899)

Chemical Identifiers

UNII
BW0OY6ZTD4
CAS number
15663-27-1
InChI Key
LXZZYRPGZAFOLE-UHFFFAOYSA-L
InChI
InChI=1S/2ClH.2H3N.Pt/h2*1H;2*1H3;/q;;;;+2/p-2
IUPAC Name
dichloroplatinumdiamine
SMILES
[H][N]([H])([H])[Pt](Cl)(Cl)[N]([H])([H])[H]

References

Synthesis Reference

Murray A. Kaplan, Alphonse P. Granatek, "Process for the preparation of microcrystalline cisplatin." U.S. Patent US4322391, issued March 30, 1982.

US4322391
General References
Not Available
Human Metabolome Database
HMDB0014656
KEGG Drug
D00275
KEGG Compound
C06911
PubChem Compound
2767
PubChem Substance
46504561
ChemSpider
76401
BindingDB
50028111
RxNav
2555
ChEBI
27899
ChEMBL
CHEMBL2068237
Therapeutic Targets Database
DAP000215
PharmGKB
PA449014
PDBe Ligand
CPT
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cisplatin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
1a2e / 1a84 / 1aio / 1au5 / 1ckt / 1da4 / 1da5 / 1ddp / 1i1p / 1ksb
show 55 more
FDA label
Download (413 KB)
MSDS
Download (76.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentSquamous Non-small-cell Lung Cancer1
4CompletedNot AvailableEsophageal Cancers1
4CompletedSupportive CareAnemia / Cervical Cancers1
4CompletedTreatmentEsophageal Cancers1
4CompletedTreatmentHead and Neck Squamous Cell Carcinoma (HNSCC)1
4CompletedTreatmentLocally Advanced Malignant Neoplasm1
4CompletedTreatmentNeoplasms, Head and Neck1
4CompletedTreatmentNon-Small Cell Lung Carcinoma (NSCLC)5
4CompletedTreatmentSquamous Cell Carcinoma (SCC)1
4RecruitingTreatmentCentral Nervous System Embryonal Tumors / Medulloblastomas1

Pharmacoeconomics

Manufacturers
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Pharmachemie bv
  • Teva parenteral medicines inc
  • Bristol myers co
Packagers
  • APP Pharmaceuticals
  • APPD
  • Baxter International Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Bristol-Myers Squibb Co.
  • Mead Johnson and Co.
  • Pharmachemie BV
  • Sicor Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
Injection, solution, concentrateIntravenous10 mg/20mL
Injection, powder, for solutionIntravenous10 mg
Injection, powder, for solutionIntravenous50 mg
Injection, solution, concentrateIntravenous10 mg/10mL
SolutionIntravenous1 mg
SolutionParenteral1 mg/mL
Injection
InjectionIntravenous1 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous1 mg/1mL
Injection, solutionIntravenous1 mg/1mL
Injection, solutionIntravenous100 mg/100mL
Injection, solutionIntravenous50 mg/50mL
InjectionParenteral0.5 mg/ml
Injection, solution, concentrateIntravenous1 mg/ml
Injection, solution
Injection, solutionIntravenous10 mg/10ml
SolutionIntravenous10 mg/20ml
SolutionIntravenous100 mg/100ml
Injection, solution, concentrateIntravenous25 mg/50ml
SolutionIntravenous50 mg/100ml
SolutionIntravenous
Injection, solution, concentrateIntravenous50 mg/100mL
InjectionIntravenous25 mg/50ml
InjectionIntravenous50 mg/100ml
SolutionIntravenous10 mg
SolutionIntravenous50 mg
Injection, solution, concentrateIntravenous; Parenteral1 MG/ML
Injection, solution10 MG/10ML
Injection, solution100 MG/100ML
Injection, solution50 MG/50ML
Injection, solution, concentrateIntravenous; Parenteral0.5 MG/ML
InjectionIntravenous50 mg
Injection10 mg/20ml
Injection25 mg/50ml
Injection50 mg/100ml
Injection, powder, for solution10 MG
Injection, powder, for solution25 MG
Injection, powder, for solution50 MG
Injection, solution, concentrateIntravenous50 mg/50mL
Injection, powder, lyophilized, for solutionIntravenous10 mg/10mL
Injection, powder, lyophilized, for solutionIntravenous50 mg/50mL
LiquidIntravenous
Injection, solutionParenteral10 MG/20ML
Injection, solutionParenteral25 MG/50ML
Injection, solutionParenteral50 MG/100ML
Prices
Unit descriptionCostUnit
Cisplatin 1 mg/ml vial0.41USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)270 dec °CPhysProp
water solubility2530 mg/L (at 25 °C)AMUNDSEN,AR & STERN,EW (1982)
logP-2.19HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility69.6 mg/mLALOGPS
logP-0.04ALOGPS
logS-0.64ALOGPS
Physiological Charge0ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area55.28 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity43.3 m3·mol-1ChemAxon
Polarizability10.95 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9637
Blood Brain Barrier+0.9469
Caco-2 permeable-0.5704
P-glycoprotein substrateNon-substrate0.8714
P-glycoprotein inhibitor INon-inhibitor0.9763
P-glycoprotein inhibitor IINon-inhibitor0.9843
Renal organic cation transporterNon-inhibitor0.9211
CYP450 2C9 substrateNon-substrate0.8069
CYP450 2D6 substrateNon-substrate0.7874
CYP450 3A4 substrateNon-substrate0.7495
CYP450 1A2 substrateNon-inhibitor0.7733
CYP450 2C9 inhibitorNon-inhibitor0.7808
CYP450 2D6 inhibitorNon-inhibitor0.9075
CYP450 2C19 inhibitorNon-inhibitor0.7995
CYP450 3A4 inhibitorNon-inhibitor0.8562
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9204
Ames testNon AMES toxic0.5661
CarcinogenicityCarcinogens 0.5146
BiodegradationNot ready biodegradable0.9213
Rat acute toxicity2.7612 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9774
hERG inhibition (predictor II)Non-inhibitor0.9344
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Nucleotide
Organism
Humans
Pharmacological action
Yes
Actions
Cross-linking/alkylation
DNA is the molecule of heredity, as it is responsible for the genetic propagation of most inherited traits. It is a polynucleic acid that carries genetic information on cell growth, division, and function. DNA consists of two long strands of nucleotides twisted into a double helix and held together by hydrogen bonds. The sequence of nucleotides determines hereditary characteristics. Each strand serves as the template for subsequent DNA replication and as a template for mRNA production, leading to protein synthesis via ribosomes.
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Garcia Sar D, Montes-Bayon M, Aguado Ortiz L, Blanco-Gonzalez E, Sierra LM, Sanz-Medel A: In vivo detection of DNA adducts induced by cisplatin using capillary HPLC-ICP-MS and their correlation with genotoxic damage in Drosophila melanogaster. Anal Bioanal Chem. 2008 Jan;390(1):37-44. Epub 2007 Oct 12. [PubMed:17932658]
  4. Sharma S, Gong P, Temple B, Bhattacharyya D, Dokholyan NV, Chaney SG: Molecular dynamic simulations of cisplatin- and oxaliplatin-d(GG) intrastand cross-links reveal differences in their conformational dynamics. J Mol Biol. 2007 Nov 9;373(5):1123-40. Epub 2007 Aug 23. [PubMed:17900616]
  5. Bloemink MJ, Reedijk J: Cisplatin and derived anticancer drugs: mechanism and current status of DNA binding. Met Ions Biol Syst. 1996;32:641-85. [PubMed:8640534]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Hydrolysis of the deoxyribose N-glycosidic bond to excise 3-methyladenine, and 7-methylguanine from the damaged DNA polymer formed by alkylation lesions.
Specific Function
Alkylbase dna n-glycosylase activity
Gene Name
MPG
Uniprot ID
P29372
Uniprot Name
DNA-3-methyladenine glycosylase
Molecular Weight
32868.365 Da
References
  1. Kartalou M, Samson LD, Essigmann JM: Cisplatin adducts inhibit 1,N(6)-ethenoadenine repair by interacting with the human 3-methyladenine DNA glycosylase. Biochemistry. 2000 Jul 11;39(27):8032-8. [PubMed:10891085]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Tumor necrosis factor binding
Specific Function
Is able to inhibit all four classes of proteinases by a unique 'trapping' mechanism. This protein has a peptide stretch, called the 'bait region' which contains specific cleavage sites for differen...
Gene Name
A2M
Uniprot ID
P01023
Uniprot Name
Alpha-2-macroglobulin
Molecular Weight
163289.945 Da
References
  1. Khalaila I, Bergamo A, Bussy F, Sava G, Dyson PJ: The role of cisplatin and NAMI-A plasma-protein interactions in relation to combination therapy. Int J Oncol. 2006 Jul;29(1):261-8. [PubMed:16773208]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Transferrin receptor binding
Specific Function
Transferrins are iron binding transport proteins which can bind two Fe(3+) ions in association with the binding of an anion, usually bicarbonate. It is responsible for the transport of iron from si...
Gene Name
TF
Uniprot ID
P02787
Uniprot Name
Serotransferrin
Molecular Weight
77063.195 Da
References
  1. Khalaila I, Bergamo A, Bussy F, Sava G, Dyson PJ: The role of cisplatin and NAMI-A plasma-protein interactions in relation to combination therapy. Int J Oncol. 2006 Jul;29(1):261-8. [PubMed:16773208]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Curator comments
Atox1 protein blocks cisplatin transport to DNA and may lead to drug resistance
General Function
Metallochaperone activity
Specific Function
Binds and deliver cytosolic copper to the copper ATPase proteins. May be important in cellular antioxidant defense.
Gene Name
ATOX1
Uniprot ID
O00244
Uniprot Name
Copper transport protein ATOX1
Molecular Weight
7401.575 Da
References
  1. Xi Z, Guo W, Tian C, Wang F, Liu Y: Copper binding modulates the platination of human copper chaperone Atox1 by antitumor trans-platinum complexes. Metallomics. 2014 Mar;6(3):491-7. doi: 10.1039/c3mt00338h. Epub 2014 Jan 28. [PubMed:24469739]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Peroxidase activity
Specific Function
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
Gene Name
MPO
Uniprot ID
P05164
Uniprot Name
Myeloperoxidase
Molecular Weight
83867.71 Da
References
  1. Erdogan S, Tosyali E, Duzguner V, Kucukgul A, Aslantas O, Celik S: Cisplatin reduces Brucella melitensis-infected cell number by inducing apoptosis, oxidant and pro-inflammatory cytokine production. Res Vet Sci. 2010 Apr;88(2):218-26. doi: 10.1016/j.rvsc.2009.09.002. Epub 2009 Oct 8. [PubMed:19818462]
  2. Ozen S, Akyol O, Iraz M, Sogut S, Ozugurlu F, Ozyurt H, Odaci E, Yildirim Z: Role of caffeic acid phenethyl ester, an active component of propolis, against cisplatin-induced nephrotoxicity in rats. J Appl Toxicol. 2004 Jan-Feb;24(1):27-35. [PubMed:14745844]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Xanthine oxidase activity
Specific 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. Ha...
Gene Name
XDH
Uniprot ID
P47989
Uniprot Name
Xanthine dehydrogenase/oxidase
Molecular Weight
146422.99 Da
References
  1. Yilmaz HR, Sogut S, Ozyurt B, Ozugurlu F, Sahin S, Isik B, Uz E, Ozyurt H: The activities of liver adenosine deaminase, xanthine oxidase, catalase, superoxide dismutase enzymes and the levels of malondialdehyde and nitric oxide after cisplatin toxicity in rats: protective effect of caffeic acid phenethyl ester. Toxicol Ind Health. 2005 May;21(3-4):67-73. [PubMed:15986578]
  2. Cetin R, Devrim E, Kilicoglu B, Avci A, Candir O, Durak I: Cisplatin impairs antioxidant system and causes oxidation in rat kidney tissues: possible protective roles of natural antioxidant foods. J Appl Toxicol. 2006 Jan-Feb;26(1):42-6. [PubMed:16158393]
  3. Erdogan S, Tosyali E, Duzguner V, Kucukgul A, Aslantas O, Celik S: Cisplatin reduces Brucella melitensis-infected cell number by inducing apoptosis, oxidant and pro-inflammatory cytokine production. Res Vet Sci. 2010 Apr;88(2):218-26. doi: 10.1016/j.rvsc.2009.09.002. Epub 2009 Oct 8. [PubMed:19818462]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Leukotriene-b4 20-monooxygenase activity
Specific Function
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 2...
Gene Name
CYP4A11
Uniprot ID
Q02928
Uniprot Name
Cytochrome P450 4A11
Molecular Weight
59347.31 Da
References
  1. Nakamura M, Imaoka S, Tanaka E, Misawa S, Funae Y: cis-Diamminedichloroplatinum induces peroxisomes as well as CYP4A1 in rat kidney. Res Commun Mol Pathol Pharmacol. 1998 Jan;99(1):23-32. [PubMed:9523352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Prostaglandin-endoperoxide synthase activity
Specific Function
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
Gene Name
PTGS2
Uniprot ID
P35354
Uniprot Name
Prostaglandin G/H synthase 2
Molecular Weight
68995.625 Da
References
  1. Tusgaard B, Norregaard R, Jensen AM, Wang G, Topcu SO, Wang Y, Nielsen S, Frokiaer J: Cisplatin decreases renal cyclooxygenase-2 expression and activity in rats. Acta Physiol (Oxf). 2011 May;202(1):79-90. doi: 10.1111/j.1748-1716.2011.02257.x. Epub 2011 Mar 22. [PubMed:21272267]
Kind
Protein
Organism
Mycobacterium tuberculosis
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Catalyzes the transfer of the acetyl group from acetyl coenzyme A to the free amino group of arylamines and hydrazines (PubMed:18795795). Is able to utilize not only acetyl-CoA, but also n-propionyl-CoA and acetoacetyl-CoA as acyl donors, although at a lower rate (PubMed:19014350). As acetyl-CoA and propionyl-CoA are products of cholesterol catabolism and the nat gene is likely present in the same operon than genes involved in cholesterol degradation, this enzyme could have a role in the utilization and regulation of these CoA species (PubMed:19014350).
Specific Function
Arylamine n-acetyltransferase activity
Gene Name
nat
Uniprot ID
P9WJI5
Uniprot Name
Arylamine N-acetyltransferase
Molecular Weight
31028.88 Da
References
  1. Ragunathan N, Dairou J, Pluvinage B, Martins M, Petit E, Janel N, Dupret JM, Rodrigues-Lima F: Identification of the xenobiotic-metabolizing enzyme arylamine N-acetyltransferase 1 as a new target of cisplatin in breast cancer cells: molecular and cellular mechanisms of inhibition. Mol Pharmacol. 2008 Jun;73(6):1761-8. doi: 10.1124/mol.108.045328. Epub 2008 Feb 29. [PubMed:18310302]
  2. Holzer AK, Samimi G, Katano K, Naerdemann W, Lin X, Safaei R, Howell SB: The copper influx transporter human copper transport protein 1 regulates the uptake of cisplatin in human ovarian carcinoma cells. Mol Pharmacol. 2004 Oct;66(4):817-23. Epub 2004 Jun 30. [PubMed:15229296]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Masek V, Anzenbacherova E, Machova M, Brabec V, Anzenbacher P: Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. Anticancer Drugs. 2009 Jun;20(5):305-11. [PubMed:19378397]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Masek V, Anzenbacherova E, Machova M, Brabec V, Anzenbacher P: Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. Anticancer Drugs. 2009 Jun;20(5):305-11. [PubMed:19378397]
  2. Walsky RL, Astuccio AV, Obach RS: Evaluation of 227 drugs for in vitro inhibition of cytochrome P450 2B6. J Clin Pharmacol. 2006 Dec;46(12):1426-38. [PubMed:17101742]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Identical protein binding
Specific Function
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name
BCHE
Uniprot ID
P06276
Uniprot Name
Cholinesterase
Molecular Weight
68417.575 Da
References
  1. Bodur E: Human serum butyrylcholinesterase interactions with cisplatin and cyclophosphamide. Biochimie. 2010 Aug;92(8):979-84. doi: 10.1016/j.biochi.2010.04.010. Epub 2010 Apr 24. [PubMed:20417682]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glutathione transferase activity
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Acts on 1,2-epoxy-3-(4-nitrophenoxy)propane, phenethylisothiocyanate 4-nitrobenzyl chlorid...
Gene Name
GSTT1
Uniprot ID
P30711
Uniprot Name
Glutathione S-transferase theta-1
Molecular Weight
27334.755 Da
References
  1. Peters U, Preisler-Adams S, Hebeisen A, Hahn M, Seifert E, Lanvers C, Heinecke A, Horst J, Jurgens H, Lamprecht-Dinnesen A: Glutathione S-transferase genetic polymorphisms and individual sensitivity to the ototoxic effect of cisplatin. Anticancer Drugs. 2000 Sep;11(8):639-43. [PubMed:11081456]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Metallothioneins have a high content of cysteine residues that bind various heavy metals; these proteins are transcriptionally regulated by both heavy metals and glucocorticoids.
Gene Name
MT1A
Uniprot ID
P04731
Uniprot Name
Metallothionein-1A
Molecular Weight
6120.19 Da
References
  1. Meijer C, Timmer A, De Vries EG, Groten JP, Knol A, Zwart N, Dam WA, Sleijfer DT, Mulder NH: Role of metallothionein in cisplatin sensitivity of germ-cell tumours. Int J Cancer. 2000 Mar 15;85(6):777-81. [PubMed:10709094]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Metallothioneins have a high content of cysteine residues that bind various heavy metals; these proteins are transcriptionally regulated by both heavy metals and glucocorticoids.
Gene Name
MT2A
Uniprot ID
P02795
Uniprot Name
Metallothionein-2
Molecular Weight
6042.05 Da
References
  1. Meijer C, Timmer A, De Vries EG, Groten JP, Knol A, Zwart N, Dam WA, Sleijfer DT, Mulder NH: Role of metallothionein in cisplatin sensitivity of germ-cell tumours. Int J Cancer. 2000 Mar 15;85(6):777-81. [PubMed:10709094]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Destroys radicals which are normally produced within the cells and which are toxic to biological systems.
Gene Name
SOD1
Uniprot ID
P00441
Uniprot Name
Superoxide dismutase [Cu-Zn]
Molecular Weight
15935.685 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
S-nitrosoglutathione binding
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration.
Gene Name
GSTP1
Uniprot ID
P09211
Uniprot Name
Glutathione S-transferase P
Molecular Weight
23355.625 Da
References
  1. Peters U, Preisler-Adams S, Hebeisen A, Hahn M, Seifert E, Lanvers C, Heinecke A, Horst J, Jurgens H, Lamprecht-Dinnesen A: Glutathione S-transferase genetic polymorphisms and individual sensitivity to the ototoxic effect of cisplatin. Anticancer Drugs. 2000 Sep;11(8):639-43. [PubMed:11081456]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Superoxide dismutase activity
Specific Function
The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinons involved in detoxification pathways as well as in biosynthetic processes such as the vit...
Gene Name
NQO1
Uniprot ID
P15559
Uniprot Name
NAD(P)H dehydrogenase [quinone] 1
Molecular Weight
30867.405 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
Gene Name
GSTM1
Uniprot ID
P09488
Uniprot Name
Glutathione S-transferase Mu 1
Molecular Weight
25711.555 Da
References
  1. Peters U, Preisler-Adams S, Hebeisen A, Hahn M, Seifert E, Lanvers C, Heinecke A, Horst J, Jurgens H, Lamprecht-Dinnesen A: Glutathione S-transferase genetic polymorphisms and individual sensitivity to the ototoxic effect of cisplatin. Anticancer Drugs. 2000 Sep;11(8):639-43. [PubMed:11081456]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Khalaila I, Bergamo A, Bussy F, Sava G, Dyson PJ: The role of cisplatin and NAMI-A plasma-protein interactions in relation to combination therapy. Int J Oncol. 2006 Jul;29(1):261-8. [PubMed:16773208]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocyte...
Gene Name
ABCC3
Uniprot ID
O15438
Uniprot Name
Canalicular multispecific organic anion transporter 2
Molecular Weight
169341.14 Da
References
  1. 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:11323161]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name
ABCC5
Uniprot ID
O15440
Uniprot Name
Multidrug resistance-associated protein 5
Molecular Weight
160658.8 Da
References
  1. 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:11323161]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. 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:11323161]
  2. Demeule M, Brossard M, Beliveau R: Cisplatin induces renal expression of P-glycoprotein and canalicular multispecific organic anion transporter. Am J Physiol. 1999 Dec;277(6 Pt 2):F832-40. [PubMed:10600929]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Pan BF, Sweet DH, Pritchard JB, Chen R, Nelson JA: A transfected cell model for the renal toxin transporter, rOCT2. Toxicol Sci. 1999 Feb;47(2):181-6. [PubMed:10220855]
  2. Burger H, Zoumaro-Djayoon A, Boersma AW, Helleman J, Berns EM, Mathijssen RH, Loos WJ, Wiemer EA: Differential transport of platinum compounds by the human organic cation transporter hOCT2 (hSLC22A2). Br J Pharmacol. 2010 Feb;159(4):898-908. doi: 10.1111/j.1476-5381.2009.00569.x. Epub 2010 Jan 8. [PubMed:20067471]
  3. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper uptake transmembrane transporter activity
Specific Function
High-affinity, saturable copper transporter involved in dietary copper uptake.
Gene Name
SLC31A1
Uniprot ID
O15431
Uniprot Name
High affinity copper uptake protein 1
Molecular Weight
21090.545 Da
References
  1. Howell SB, Safaei R, Larson CA, Sailor MJ: Copper transporters and the cellular pharmacology of the platinum-containing cancer drugs. Mol Pharmacol. 2010 Jun;77(6):887-94. doi: 10.1124/mol.109.063172. Epub 2010 Feb 16. [PubMed:20159940]
  2. Kurokawa T, He G, Siddik ZH: Protein kinase inhibitors emodin and dichloro-ribofuranosylbenzimidazole modulate the cellular accumulation and cytotoxicity of cisplatin in a schedule-dependent manner. Cancer Chemother Pharmacol. 2010 Feb;65(3):427-36. doi: 10.1007/s00280-009-1045-2. Epub 2009 Jun 16. [PubMed:19529937]
  3. Jandial DD, Farshchi-Heydari S, Larson CA, Elliott GI, Wrasidlo WJ, Howell SB: Enhanced delivery of cisplatin to intraperitoneal ovarian carcinomas mediated by the effects of bortezomib on the human copper transporter 1. Clin Cancer Res. 2009 Jan 15;15(2):553-60. doi: 10.1158/1078-0432.CCR-08-2081. [PubMed:19147760]
  4. Liang ZD, Stockton D, Savaraj N, Tien Kuo M: Mechanistic comparison of human high-affinity copper transporter 1-mediated transport between copper ion and cisplatin. Mol Pharmacol. 2009 Oct;76(4):843-53. doi: 10.1124/mol.109.056416. Epub 2009 Jul 1. [PubMed:19570948]
  5. Rabik CA, Maryon EB, Kasza K, Shafer JT, Bartnik CM, Dolan ME: Role of copper transporters in resistance to platinating agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):133-42. doi: 10.1007/s00280-008-0860-1. Epub 2008 Nov 8. [PubMed:18998134]
  6. Pabla N, Murphy RF, Liu K, Dong Z: The copper transporter Ctr1 contributes to cisplatin uptake by renal tubular cells during cisplatin nephrotoxicity. Am J Physiol Renal Physiol. 2009 Mar;296(3):F505-11. doi: 10.1152/ajprenal.90545.2008. Epub 2009 Jan 14. [PubMed:19144690]
  7. Furukawa T, Komatsu M, Ikeda R, Tsujikawa K, Akiyama S: Copper transport systems are involved in multidrug resistance and drug transport. Curr Med Chem. 2008;15(30):3268-78. [PubMed:19075668]
  8. Holzer AK, Samimi G, Katano K, Naerdemann W, Lin X, Safaei R, Howell SB: The copper influx transporter human copper transport protein 1 regulates the uptake of cisplatin in human ovarian carcinoma cells. Mol Pharmacol. 2004 Oct;66(4):817-23. Epub 2004 Jun 30. [PubMed:15229296]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper ion transmembrane transporter activity
Specific Function
Involved in low-affinity copper uptake.
Gene Name
SLC31A2
Uniprot ID
O15432
Uniprot Name
Probable low affinity copper uptake protein 2
Molecular Weight
15681.29 Da
References
  1. Blair BG, Larson CA, Safaei R, Howell SB: Copper transporter 2 regulates the cellular accumulation and cytotoxicity of Cisplatin and Carboplatin. Clin Cancer Res. 2009 Jul 1;15(13):4312-21. doi: 10.1158/1078-0432.CCR-09-0311. Epub 2009 Jun 9. [PubMed:19509135]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Transporter activity
Specific Function
Isoform 1: May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4...
Gene Name
ABCC6
Uniprot ID
O95255
Uniprot Name
Multidrug resistance-associated protein 6
Molecular Weight
164904.81 Da
References
  1. Belinsky MG, Chen ZS, Shchaveleva I, Zeng H, Kruh GD: Characterization of the drug resistance and transport properties of multidrug resistance protein 6 (MRP6, ABCC6). Cancer Res. 2002 Nov 1;62(21):6172-7. [PubMed:12414644]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Li D, Jang SH, Kim J, Wientjes MG, Au JL: Enhanced drug-induced apoptosis associated with P-glycoprotein overexpression is specific to antimicrotubule agents. Pharm Res. 2003 Jan;20(1):45-50. [PubMed:12608535]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper-exporting atpase activity
Specific Function
Involved in the export of copper out of the cells, such as the efflux of hepatic copper into the bile.
Gene Name
ATP7B
Uniprot ID
P35670
Uniprot Name
Copper-transporting ATPase 2
Molecular Weight
157261.34 Da
References
  1. Rabik CA, Maryon EB, Kasza K, Shafer JT, Bartnik CM, Dolan ME: Role of copper transporters in resistance to platinating agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):133-42. doi: 10.1007/s00280-008-0860-1. Epub 2008 Nov 8. [PubMed:18998134]
  2. Mangala LS, Zuzel V, Schmandt R, Leshane ES, Halder JB, Armaiz-Pena GN, Spannuth WA, Tanaka T, Shahzad MM, Lin YG, Nick AM, Danes CG, Lee JW, Jennings NB, Vivas-Mejia PE, Wolf JK, Coleman RL, Siddik ZH, Lopez-Berestein G, Lutsenko S, Sood AK: Therapeutic Targeting of ATP7B in Ovarian Carcinoma. Clin Cancer Res. 2009 Jun 1;15(11):3770-80. doi: 10.1158/1078-0432.CCR-08-2306. Epub 2009 May 26. [PubMed:19470734]
  3. Furukawa T, Komatsu M, Ikeda R, Tsujikawa K, Akiyama S: Copper transport systems are involved in multidrug resistance and drug transport. Curr Med Chem. 2008;15(30):3268-78. [PubMed:19075668]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Superoxide dismutase copper chaperone activity
Specific Function
May supply copper to copper-requiring proteins within the secretory pathway, when localized in the trans-Golgi network. Under conditions of elevated extracellular copper, it relocalized to the plas...
Gene Name
ATP7A
Uniprot ID
Q04656
Uniprot Name
Copper-transporting ATPase 1
Molecular Weight
163372.275 Da
References
  1. Rabik CA, Maryon EB, Kasza K, Shafer JT, Bartnik CM, Dolan ME: Role of copper transporters in resistance to platinating agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):133-42. doi: 10.1007/s00280-008-0860-1. Epub 2008 Nov 8. [PubMed:18998134]
  2. Furukawa T, Komatsu M, Ikeda R, Tsujikawa K, Akiyama S: Copper transport systems are involved in multidrug resistance and drug transport. Curr Med Chem. 2008;15(30):3268-78. [PubMed:19075668]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Ceckova M, Vackova Z, Radilova H, Libra A, Buncek M, Staud F: Effect of ABCG2 on cytotoxicity of platinum drugs: interference of EGFP. Toxicol In Vitro. 2008 Dec;22(8):1846-52. doi: 10.1016/j.tiv.2008.09.001. Epub 2008 Sep 9. [PubMed:18801423]

Drug created on June 13, 2005 07:24 / Updated on October 25, 2020 09:16

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates