Identification
NameATP
Accession NumberDB00171  (NUTR00017, EXPT00007)
TypeSmall Molecule
GroupsNutraceutical
Description

An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.

Structure
Thumb
Synonyms
Adenosine 5'-triphosphate
Adenosine triphosphate
Adenosine-5'-triphosphate
ATP
External IDs Not Available
Product Ingredients
IngredientUNIICASInChI KeyDetails
Adenosine triphosphate disodium5L51B4DR1G 987-65-5TTWYZDPBDWHJOR-IDIVVRGQSA-LDetails
Adenosine triphosphate disodium trihydrate7ZRM409FOZ 51963-61-2MWEQTWJABOLLOS-AZGWGOJFSA-LDetails
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AtriphosBiochimica
StriadyneAuclair
Brand mixturesNot Available
Categories
UNII8L70Q75FXE
CAS number56-65-5
WeightAverage: 507.181
Monoisotopic: 506.995745159
Chemical FormulaC10H16N5O13P3
InChI KeyZKHQWZAMYRWXGA-KQYNXXCUSA-N
InChI
InChI=1S/C10H16N5O13P3/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(17)6(16)4(26-10)1-25-30(21,22)28-31(23,24)27-29(18,19)20/h2-4,6-7,10,16-17H,1H2,(H,21,22)(H,23,24)(H2,11,12,13)(H2,18,19,20)/t4-,6-,7-,10-/m1/s1
IUPAC Name
({[({[(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy](hydroxy)phosphoryl}oxy)phosphonic acid
SMILES
NC1=NC=NC2=C1N=CN2[C@@H]1O[[email protected]](COP(O)(=O)OP(O)(=O)OP(O)(O)=O)[C@@H](O)[[email protected]]1O
Pharmacology
Indication

For nutritional supplementation, also for treating dietary shortage or imbalance

Structured Indications Not Available
Pharmacodynamics

Adenosine triphosphate (ATP) is the nucleotide known in biochemistry as the "molecular currency" of intracellular energy transfer; that is, ATP is able to store and transport chemical energy within cells. ATP also plays an important role in the synthesis of nucleic acids. The total quantity of ATP in the human body is about 0.1 mole. The energy used by human cells requires the hydrolysis of 200 to 300 moles of ATP daily. This means that each ATP molecule is recycled 2000 to 3000 times during a single day. ATP cannot be stored, hence its consumption must closely follow its synthesis.

Mechanism of action

ATP is able to store and transport chemical energy within cells. ATP also plays an important role in the synthesis of nucleic acids. ATP can be produced by various cellular processes, most typically in mitochondria by oxidative phosphorylation under the catalytic influence of ATP synthase. The total quantity of ATP in the human body is about 0.1 mole. The energy used by human cells requires the hydrolysis of 200 to 300 moles of ATP daily. This means that each ATP molecule is recycled 2000 to 3000 times during a single day. ATP cannot be stored, hence its consumption must closely follow its synthesis.

TargetKindPharmacological actionActionsOrganismUniProt ID
Abelson tyrosine-protein kinase 2Proteinunknown
inhibitor
HumanP42684 details
ATP-binding cassette sub-family A member 1ProteinunknownNot AvailableHumanO95477 details
Acetyl-coenzyme A synthetase, cytoplasmicProteinunknownNot AvailableHumanQ9NR19 details
ALK tyrosine kinase receptorProteinunknownNot AvailableHumanQ9UM73 details
NEDD8-activating enzyme E1 regulatory subunitProteinunknownNot AvailableHumanQ13564 details
5'-AMP-activated protein kinase catalytic subunit alpha-1ProteinunknownNot AvailableHumanQ13131 details
Serine/threonine-protein kinase A-RafProteinunknownNot AvailableHumanP10398 details
Serine/threonine-protein kinase receptor R3ProteinunknownNot AvailableHumanP37023 details
Long-chain-fatty-acid--CoA ligase 1ProteinunknownNot AvailableHumanP33121 details
Cytosolic purine 5'-nucleotidaseProteinunknownNot AvailableHumanP49902 details
ATPase ASNA1ProteinunknownNot AvailableHumanO43681 details
ATP-binding cassette sub-family C member 9ProteinunknownNot AvailableHumanO60706 details
RAC-alpha serine/threonine-protein kinaseProteinunknownNot AvailableHumanP31749 details
Beta-adrenergic receptor kinase 1ProteinunknownNot AvailableHumanP25098 details
Apoptotic protease-activating factor 1ProteinunknownNot AvailableHumanO14727 details
Acetyl-coenzyme A synthetase 2-like, mitochondrialProteinunknownNot AvailableHumanQ9NUB1 details
Activin receptor type-1BProteinunknownNot AvailableHumanP36896 details
Activin receptor type-1ProteinunknownNot AvailableHumanQ04771 details
Bile salt export pumpProteinunknownNot AvailableHumanO95342 details
Asparagine synthetase [glutamine-hydrolyzing]ProteinunknownNot AvailableHumanP08243 details
Cyclin-dependent kinase 15ProteinunknownNot AvailableHumanQ96Q40 details
ADP/ATP translocase 1ProteinunknownNot AvailableHumanP12235 details
ATP-binding cassette sub-family C member 8ProteinunknownNot AvailableHumanQ09428 details
Argininosuccinate synthaseProteinunknownNot AvailableHumanP00966 details
AFG3-like protein 2ProteinunknownNot AvailableHumanQ9Y4W6 details
Beta-adrenergic receptor kinase 2ProteinunknownNot AvailableHumanP35626 details
Anti-Muellerian hormone type-2 receptorProteinunknownNot AvailableHumanQ16671 details
Activated CDC42 kinase 1ProteinunknownNot AvailableHumanQ07912 details
Tyrosine-protein kinase ABL1Proteinunknown
inhibitor
HumanP00519 details
Adenylate cyclase type 1ProteinunknownNot AvailableHumanQ08828 details
Multidrug resistance protein 1ProteinunknownNot AvailableHumanP08183 details
ATP-binding cassette sub-family G member 1ProteinunknownNot AvailableHumanP45844 details
Canalicular multispecific organic anion transporter 1ProteinunknownNot AvailableHumanQ92887 details
Multidrug resistance-associated protein 6ProteinunknownNot AvailableHumanO95255 details
Multidrug resistance-associated protein 4ProteinunknownNot AvailableHumanO15439 details
Multidrug resistance-associated protein 1ProteinunknownNot AvailableHumanP33527 details
Cystic fibrosis transmembrane conductance regulatorProteinunknown
cofactor
HumanP13569 details
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformProteinunknownNot AvailableHumanP42336 details
Casein kinase II subunit alphaProteinunknownNot AvailableHumanP68400 details
Casein kinase II subunit betaProteinunknownNot AvailableHumanP67870 details
P2Y purinoceptor 11ProteinunknownNot AvailableHumanQ96G91 details
Serine/threonine-protein phosphatase 5ProteinunknownNot AvailableHumanP53041 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
Toxicity

Oral LD50 in rats is > 2 g/kg.

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Nucleotide Sugars MetabolismMetabolicSMP00010
Glycerolipid MetabolismMetabolicSMP00039
Sulfate/Sulfite MetabolismMetabolicSMP00041
Galactose MetabolismMetabolicSMP00043
Pyrimidine MetabolismMetabolicSMP00046
Tryptophan MetabolismMetabolicSMP00063
Fructose and Mannose DegradationMetabolicSMP00064
Butyrate MetabolismMetabolicSMP00073
Alendronate Action PathwayDrug actionSMP00095
Zoledronate Action PathwayDrug actionSMP00107
Phenylacetate MetabolismMetabolicSMP00126
GluconeogenesisMetabolicSMP00128
3-Methylglutaconic Aciduria Type IIIDiseaseSMP00140
Adenylosuccinate Lyase DeficiencyDiseaseSMP00167
HistidinemiaDiseaseSMP00191
HypoacetylaspartiaDiseaseSMP00192
Methylmalonic AciduriaDiseaseSMP00200
Molybdenum Cofactor DeficiencyDiseaseSMP00203
Purine Nucleoside Phosphorylase DeficiencyDiseaseSMP00210
Pyruvate Dehydrogenase Complex DeficiencyDiseaseSMP00212
S-Adenosylhomocysteine (SAH) Hydrolase DeficiencyDiseaseSMP00214
Glycine N-methyltransferase DeficiencyDiseaseSMP00222
Non Ketotic HyperglycinemiaDiseaseSMP00223
Omeprazole Action PathwayDrug actionSMP00226
Ranitidine Action PathwayDrug actionSMP00230
Cimetidine Action PathwayDrug actionSMP00232
Nizatidine Action PathwayDrug actionSMP00233
Isovaleric AciduriaDiseaseSMP00238
Salla Disease/Infantile Sialic Acid Storage DiseaseDiseaseSMP00240
Pirenzepine Action PathwayDrug actionSMP00246
Pharmacogenomic Effects/ADRs Not Available
Interactions
Drug Interactions Not Available
Food InteractionsNot Available
References
Synthesis Reference

George M. Whitesides, Patricia E. Garrett, Merrell G. Siegel, "Method for preparing adenosine triphosphate." U.S. Patent US4164444, issued April, 1975.

US4164444
General References
  1. Gajewski E, Steckler DK, Goldberg RN: Thermodynamics of the hydrolysis of adenosine 5'-triphosphate to adenosine 5'-diphosphate. J Biol Chem. 1986 Sep 25;261(27):12733-7. [PubMed:3528161 ]
  2. Storer AC, Cornish-Bowden A: Concentration of MgATP2- and other ions in solution. Calculation of the true concentrations of species present in mixtures of associating ions. Biochem J. 1976 Oct 1;159(1):1-5. [PubMed:11772 ]
  3. Wilson JE, Chin A: Chelation of divalent cations by ATP, studied by titration calorimetry. Anal Biochem. 1991 Feb 15;193(1):16-9. [PubMed:1645933 ]
  4. Garfinkel L, Altschuld RA, Garfinkel D: Magnesium in cardiac energy metabolism. J Mol Cell Cardiol. 1986 Oct;18(10):1003-13. [PubMed:3537318 ]
  5. Parsons M: Glycosomes: parasites and the divergence of peroxisomal purpose. Mol Microbiol. 2004 Aug;53(3):717-24. [PubMed:15255886 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSDownload (72.6 KB)
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedSupportive CareCachexia / Unspecified Adult Solid Tumor, Protocol Specific1
2CompletedOtherAlzheimer's Disease (AD)1
3CompletedTreatmentCancers / Palliative Care / Quality of Life / Survival1
Not AvailableRecruitingTreatmentNonvalvular Atrial Fibrillation1
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point (°C)176 °CNot Available
water solubility1E+006 mg/LMERCK INDEX (1996); freely soluble
logP-5.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.49 mg/mLALOGPS
logP-0.84ALOGPS
logP-6ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)0.9ChemAxon
pKa (Strongest Basic)5ChemAxon
Physiological Charge-3ChemAxon
Hydrogen Acceptor Count14ChemAxon
Hydrogen Donor Count7ChemAxon
Polar Surface Area279.13 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity95.81 m3·mol-1ChemAxon
Polarizability38.92 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8672
Blood Brain Barrier+0.9035
Caco-2 permeable-0.7475
P-glycoprotein substrateNon-substrate0.6692
P-glycoprotein inhibitor INon-inhibitor0.8983
P-glycoprotein inhibitor IINon-inhibitor0.9763
Renal organic cation transporterNon-inhibitor0.9571
CYP450 2C9 substrateNon-substrate0.8379
CYP450 2D6 substrateNon-substrate0.8363
CYP450 3A4 substrateNon-substrate0.5673
CYP450 1A2 substrateNon-inhibitor0.8908
CYP450 2C9 inhibitorNon-inhibitor0.9403
CYP450 2D6 inhibitorNon-inhibitor0.9005
CYP450 2C19 inhibitorNon-inhibitor0.9352
CYP450 3A4 inhibitorNon-inhibitor0.9375
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.976
Ames testNon AMES toxic0.8933
CarcinogenicityNon-carcinogens0.9165
BiodegradationNot ready biodegradable0.9645
Rat acute toxicity2.5022 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9727
hERG inhibition (predictor II)Non-inhibitor0.8159
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT (LTQ Orbitrap XL, Thermo Scientific ) , Negativesplash10-0a4i-0131190000-316dbdca27f38ad8ee57View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT (LTQ Orbitrap XL, Thermo Scientific ) , Negativesplash10-004i-0000900000-f5ffc4694dfd302fd52dView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-ITFT (LTQ Orbitrap XL, Thermo Scientific ) , Negativesplash10-0a4i-0000900000-e9a09b9360491c310280View in MoNA
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
1D NMR13C NMR SpectrumNot Available
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
Taxonomy
DescriptionThis compound belongs to the class of chemical entities known as purine ribonucleoside triphosphates. These are purine ribobucleotides with a triphosphate group linked to the ribose moiety.
KingdomChemical entities
Super ClassOrganic compounds
ClassNucleosides, nucleotides, and analogues
Sub ClassPurine nucleotides
Direct ParentPurine ribonucleoside triphosphates
Alternative ParentsPurine ribonucleoside monophosphates / Pentose phosphates / Glycosylamines / 6-aminopurines / Monosaccharide phosphates / Monoalkyl phosphates / Aminopyrimidines and derivatives / N-substituted imidazoles / Imidolactams / Primary aromatic amines
SubstituentsPurine ribonucleoside triphosphate / Purine ribonucleoside monophosphate / Pentose phosphate / Pentose-5-phosphate / Glycosyl compound / N-glycosyl compound / 6-aminopurine / Monosaccharide phosphate / Pentose monosaccharide / Imidazopyrimidine
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptorsadenosine 5'-phosphate, purine ribonucleoside 5'-triphosphate (CHEBI:15422 ) / Ribonucleotides, Coenzymes (C00002 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Receptor binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays an ABL1-overlapping role in key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion and receptor endocytosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like MYH10 (involved in movement); CTTN (...
Gene Name:
ABL2
Uniprot ID:
P42684
Uniprot Name:
Abelson tyrosine-protein kinase 2
Molecular Weight:
128341.935 Da
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Syntaxin binding
Specific Function:
cAMP-dependent and sulfonylurea-sensitive anion transporter. Key gatekeeper influencing intracellular cholesterol transport.
Gene Name:
ABCA1
Uniprot ID:
O95477
Uniprot Name:
ATP-binding cassette sub-family A member 1
Molecular Weight:
254299.89 Da
References
  1. Porchay I, Pean F, Bellili N, Royer B, Cogneau J, Chesnier MC, Caradec A, Tichet J, Balkau B, Marre M, Fumeron F: ABCA1 single nucleotide polymorphisms on high-density lipoprotein-cholesterol and overweight: the D.E.S.I.R. study. Obesity (Silver Spring). 2006 Nov;14(11):1874-9. [PubMed:17135600 ]
  2. Badeau R, Jauhiainen M, Metso J, Nikander E, Tikkanen MJ, Ylikorkala O, Mikkola TS: Effect of isolated isoflavone supplementation on ABCA1-dependent cholesterol efflux potential in postmenopausal women. Menopause. 2007 Mar-Apr;14(2):293-9. [PubMed:17224860 ]
  3. Zarubica A, Trompier D, Chimini G: ABCA1, from pathology to membrane function. Pflugers Arch. 2007 Feb;453(5):569-79. Epub 2006 Jul 21. [PubMed:16858612 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Atp binding
Specific Function:
Activates acetate so that it can be used for lipid synthesis or for energy generation.
Gene Name:
ACSS2
Uniprot ID:
Q9NR19
Uniprot Name:
Acetyl-coenzyme A synthetase, cytoplasmic
Molecular Weight:
78579.11 Da
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. Starai VJ, Celic I, Cole RN, Boeke JD, Escalante-Semerena JC: Sir2-dependent activation of acetyl-CoA synthetase by deacetylation of active lysine. Science. 2002 Dec 20;298(5602):2390-2. [PubMed:12493915 ]
  4. Schuler AJ, Jenkins D: Enhanced biological phosphorus removal from wastewater by biomass with different phosphorus contents, Part II: Anaerobic adenosine triphosphate utilization and acetate uptake rates. Water Environ Res. 2003 Nov-Dec;75(6):499-511. [PubMed:14704009 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane receptor protein tyrosine kinase activity
Specific Function:
Neuronal orphan receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis and differentiation of the nervous system. Transduces signals from ligands at the cell surface, through specific activation of the mitogen-activated protein kinase (MAPK) pathway. Phosphorylates almost...
Gene Name:
ALK
Uniprot ID:
Q9UM73
Uniprot Name:
ALK tyrosine kinase receptor
Molecular Weight:
176440.535 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Ubiquitin protein ligase binding
Specific Function:
Regulatory subunit of the dimeric UBA3-NAE1 E1 enzyme. E1 activates NEDD8 by first adenylating its C-terminal glycine residue with ATP, thereafter linking this residue to the side chain of the catalytic cysteine, yielding a NEDD8-UBA3 thioester and free AMP. E1 finally transfers NEDD8 to the catalytic cysteine of UBE2M. Necessary for cell cycle progression through the S-M checkpoint. Overexpres...
Gene Name:
NAE1
Uniprot ID:
Q13564
Uniprot Name:
NEDD8-activating enzyme E1 regulatory subunit
Molecular Weight:
60245.795 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Tau-protein kinase activity
Specific Function:
Catalytic subunit of AMP-activated protein kinase (AMPK), an energy sensor protein kinase that plays a key role in regulating cellular energy metabolism. In response to reduction of intracellular ATP levels, AMPK activates energy-producing pathways and inhibits energy-consuming processes: inhibits protein, carbohydrate and lipid biosynthesis, as well as cell growth and proliferation. AMPK acts ...
Gene Name:
PRKAA1
Uniprot ID:
Q13131
Uniprot Name:
5'-AMP-activated protein kinase catalytic subunit alpha-1
Molecular Weight:
64008.64 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor signaling protein activity
Specific Function:
Involved in the transduction of mitogenic signals from the cell membrane to the nucleus. May also regulate the TOR signaling cascade.Isoform 2: Serves as a positive regulator of myogenic differentiation by inducing cell cycle arrest, the expression of myogenin and other muscle-specific proteins, and myotube formation.
Gene Name:
ARAF
Uniprot ID:
P10398
Uniprot Name:
Serine/threonine-protein kinase A-Raf
Molecular Weight:
67584.825 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane receptor protein serine/threonine kinase activity
Specific Function:
Type I receptor for TGF-beta family ligands BMP9/GDF2 and BMP10 and important regulator of normal blood vessel development. On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. May b...
Gene Name:
ACVRL1
Uniprot ID:
P37023
Uniprot Name:
Serine/threonine-protein kinase receptor R3
Molecular Weight:
56124.03 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Long-chain fatty acid-coa ligase activity
Specific Function:
Activation of long-chain fatty acids for both synthesis of cellular lipids, and degradation via beta-oxidation. Preferentially uses palmitoleate, oleate and linoleate.
Gene Name:
ACSL1
Uniprot ID:
P33121
Uniprot Name:
Long-chain-fatty-acid--CoA ligase 1
Molecular Weight:
77942.685 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Nucleotide binding
Specific Function:
May have a critical role in the maintenance of a constant composition of intracellular purine/pyrimidine nucleotides in cooperation with other nucleotidases. Preferentially hydrolyzes inosine 5'-monophosphate (IMP) and other purine nucleotides.
Gene Name:
NT5C2
Uniprot ID:
P49902
Uniprot Name:
Cytosolic purine 5'-nucleotidase
Molecular Weight:
64969.2 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transporter activity
Specific Function:
ATPase required for the post-translational delivery of tail-anchored (TA) proteins to the endoplasmic reticulum. Recognizes and selectively binds the transmembrane domain of TA proteins in the cytosol. This complex then targets to the endoplasmic reticulum by membrane-bound receptors, where the tail-anchored protein is released for insertion. This process is regulated by ATP binding and hydroly...
Gene Name:
ASNA1
Uniprot ID:
O43681
Uniprot Name:
ATPase ASNA1
Molecular Weight:
38792.445 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transporter activity
Specific Function:
Subunit of ATP-sensitive potassium channels (KATP). Can form cardiac and smooth muscle-type KATP channels with KCNJ11. KCNJ11 forms the channel pore while ABCC9 is required for activation and regulation.
Gene Name:
ABCC9
Uniprot ID:
O60706
Uniprot Name:
ATP-binding cassette sub-family C member 9
Molecular Weight:
174221.7 Da
References
  1. Zhao JL, Yang YJ, You SJ, Jing ZC, Wu YJ, Cheng JL, Gao RL: Pretreatment with fosinopril or valsartan reduces myocardial no-reflow after acute myocardial infarction and reperfusion. Coron Artery Dis. 2006 Aug;17(5):463-9. [PubMed:16845255 ]
  2. Yang YJ, Zhao JL, You SJ, Wu YJ, Jing ZC, Gao RL, Chen ZJ: Post-infarction treatment with simvastatin reduces myocardial no-reflow by opening of the KATP channel. Eur J Heart Fail. 2007 Jan;9(1):30-6. Epub 2006 Jul 7. [PubMed:16829188 ]
  3. Bryan J, Munoz A, Zhang X, Dufer M, Drews G, Krippeit-Drews P, Aguilar-Bryan L: ABCC8 and ABCC9: ABC transporters that regulate K+ channels. Pflugers Arch. 2007 Feb;453(5):703-18. Epub 2006 Aug 8. [PubMed:16897043 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein serine/threonine/tyrosine kinase activity
Specific Function:
AKT1 is one of 3 closely related serine/threonine-protein kinases (AKT1, AKT2 and AKT3) called the AKT kinase, and which regulate many processes including metabolism, proliferation, cell survival, growth and angiogenesis. This is mediated through serine and/or threonine phosphorylation of a range of downstream substrates. Over 100 substrate candidates have been reported so far, but for most of ...
Gene Name:
AKT1
Uniprot ID:
P31749
Uniprot Name:
RAC-alpha serine/threonine-protein kinase
Molecular Weight:
55686.035 Da
References
  1. Van Meter TE, Broaddus WC, Cash D, Fillmore H: Cotreatment with a novel phosphoinositide analogue inhibitor and carmustine enhances chemotherapeutic efficacy by attenuating AKT activity in gliomas. Cancer. 2006 Nov 15;107(10):2446-54. [PubMed:17041888 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein kinase activity
Specific Function:
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner.
Gene Name:
ADRBK1
Uniprot ID:
P25098
Uniprot Name:
Beta-adrenergic receptor kinase 1
Molecular Weight:
79572.96 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Nucleotide binding
Specific Function:
Oligomeric Apaf-1 mediates the cytochrome c-dependent autocatalytic activation of pro-caspase-9 (Apaf-3), leading to the activation of caspase-3 and apoptosis. This activation requires ATP. Isoform 6 is less effective in inducing apoptosis.
Gene Name:
APAF1
Uniprot ID:
O14727
Uniprot Name:
Apoptotic protease-activating factor 1
Molecular Weight:
141838.815 Da
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. Chinnaiyan AM: The apoptosome: heart and soul of the cell death machine. Neoplasia. 1999 Apr;1(1):5-15. [PubMed:10935465 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Atp binding
Specific Function:
Important for maintaining normal body temperature during fasting and for energy homeostasis. Essential for energy expenditure under ketogenic conditions (By similarity). Converts acetate to acetyl-CoA so that it can be used for oxidation through the tricarboxylic cycle to produce ATP and CO(2).
Gene Name:
ACSS1
Uniprot ID:
Q9NUB1
Uniprot Name:
Acetyl-coenzyme A synthetase 2-like, mitochondrial
Molecular Weight:
74856.1 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Ubiquitin protein ligase binding
Specific Function:
Transmembrane serine/threonine kinase activin type-1 receptor forming an activin receptor complex with activin receptor type-2 (ACVR2A or ACVR2B). Transduces the activin signal from the cell surface to the cytoplasm and is thus regulating a many physiological and pathological processes including neuronal differentiation and neuronal survival, hair follicle development and cycling, FSH productio...
Gene Name:
ACVR1B
Uniprot ID:
P36896
Uniprot Name:
Activin receptor type-1B
Molecular Weight:
56806.05 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transmembrane receptor protein serine/threonine kinase activity
Specific Function:
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for activin. May be involved for left-right pattern formation during embryogenesis (By similarity).
Gene Name:
ACVR1
Uniprot ID:
Q04771
Uniprot Name:
Activin receptor type-1
Molecular Weight:
57152.41 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transporter activity
Specific Function:
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name:
ABCB11
Uniprot ID:
O95342
Uniprot Name:
Bile salt export pump
Molecular Weight:
146405.83 Da
References
  1. Snow KL, Moseley RH: Effect of thiazolidinediones on bile acid transport in rat liver. Life Sci. 2007 Jan 30;80(8):732-40. Epub 2006 Nov 10. [PubMed:17126857 ]
  2. Suchy FJ, Ananthanarayanan M: Bile salt excretory pump: biology and pathobiology. J Pediatr Gastroenterol Nutr. 2006 Jul;43 Suppl 1:S10-6. [PubMed:16819395 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein homodimerization activity
Specific Function:
Not Available
Gene Name:
ASNS
Uniprot ID:
P08243
Uniprot Name:
Asparagine synthetase [glutamine-hydrolyzing]
Molecular Weight:
64369.39 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein serine/threonine kinase activity
Specific Function:
Serine/threonine-protein kinase that acts like an antiapoptotic protein that counters TRAIL/TNFSF10-induced apoptosis by inducing phosphorylation of BIRC5 at 'Thr-34'.
Gene Name:
CDK15
Uniprot ID:
Q96Q40
Uniprot Name:
Cyclin-dependent kinase 15
Molecular Weight:
49022.64 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Adenine transmembrane transporter activity
Specific Function:
Catalyzes the exchange of cytoplasmic ADP with mitochondrial ATP across the mitochondrial inner membrane.
Gene Name:
SLC25A4
Uniprot ID:
P12235
Uniprot Name:
ADP/ATP translocase 1
Molecular Weight:
33064.265 Da
References
  1. Walther T, Tschope C, Sterner-Kock A, Westermann D, Heringer-Walther S, Riad A, Nikolic A, Wang Y, Ebermann L, Siems WE, Bader M, Shakibaei M, Schultheiss HP, Dorner A: Accelerated mitochondrial adenosine diphosphate/adenosine triphosphate transport improves hypertension-induced heart disease. Circulation. 2007 Jan 23;115(3):333-44. Epub 2007 Jan 8. [PubMed:17210842 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sulfonylurea receptor activity
Specific Function:
Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
Gene Name:
ABCC8
Uniprot ID:
Q09428
Uniprot Name:
ATP-binding cassette sub-family C member 8
Molecular Weight:
176990.36 Da
References
  1. Nakamura A, Kawahito S, Kawano T, Nazari H, Takahashi A, Kitahata H, Nakaya Y, Oshita S: Differential effects of etomidate and midazolam on vascular adenosine triphosphate-sensitive potassium channels: isometric tension and patch clamp studies. Anesthesiology. 2007 Mar;106(3):515-22. [PubMed:17325510 ]
  2. Bienengraeber M, Warltier DC, Bosnjak ZJ, Stadnicka A: Mechanism of cardiac sarcolemmal adenosine triphosphate-sensitive potassium channel activation by isoflurane in a heterologous expression system. Anesthesiology. 2006 Sep;105(3):534-40. [PubMed:16931986 ]
  3. Bryan J, Munoz A, Zhang X, Dufer M, Drews G, Krippeit-Drews P, Aguilar-Bryan L: ABCC8 and ABCC9: ABC transporters that regulate K+ channels. Pflugers Arch. 2007 Feb;453(5):703-18. Epub 2006 Aug 8. [PubMed:16897043 ]
  4. Tanaka K, Kawano T, Nakamura A, Nazari H, Kawahito S, Oshita S, Takahashi A, Nakaya Y: Isoflurane activates sarcolemmal adenosine triphosphate-sensitive potassium channels in vascular smooth muscle cells: a role for protein kinase A. Anesthesiology. 2007 May;106(5):984-91. [PubMed:17457130 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Is indirectly involved in the control of blood pressure.
Gene Name:
ASS1
Uniprot ID:
P00966
Uniprot Name:
Argininosuccinate synthase
Molecular Weight:
46530.055 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Zinc ion binding
Specific Function:
ATP-dependent protease which is essential for axonal development.
Gene Name:
AFG3L2
Uniprot ID:
Q9Y4W6
Uniprot Name:
AFG3-like protein 2
Molecular Weight:
88583.03 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein kinase activity
Specific Function:
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.
Gene Name:
ADRBK2
Uniprot ID:
P35626
Uniprot Name:
Beta-adrenergic receptor kinase 2
Molecular Weight:
79709.085 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transforming growth factor beta receptor activity, type ii
Specific Function:
On ligand binding, forms a receptor complex consisting of two type II and two type I transmembrane serine/threonine kinases. Type II receptors phosphorylate and activate type I receptors which autophosphorylate, then bind and activate SMAD transcriptional regulators. Receptor for anti-Muellerian hormone.
Gene Name:
AMHR2
Uniprot ID:
Q16671
Uniprot Name:
Anti-Muellerian hormone type-2 receptor
Molecular Weight:
62749.02 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Ww domain binding
Specific Function:
Non-receptor tyrosine-protein and serine/threonine-protein kinase that is implicated in cell spreading and migration, cell survival, cell growth and proliferation. Transduces extracellular signals to cytosolic and nuclear effectors. Phosphorylates AKT1, AR, MCF2, WASL and WWOX. Implicated in trafficking and clathrin-mediated endocytosis through binding to epidermal growth factor receptor (EGFR)...
Gene Name:
TNK2
Uniprot ID:
Q07912
Uniprot Name:
Activated CDC42 kinase 1
Molecular Weight:
114567.605 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Syntaxin binding
Specific Function:
Non-receptor tyrosine-protein kinase that plays a role in many key processes linked to cell growth and survival such as cytoskeleton remodeling in response to extracellular stimuli, cell motility and adhesion, receptor endocytosis, autophagy, DNA damage response and apoptosis. Coordinates actin remodeling through tyrosine phosphorylation of proteins controlling cytoskeleton dynamics like WASF3 ...
Gene Name:
ABL1
Uniprot ID:
P00519
Uniprot Name:
Tyrosine-protein kinase ABL1
Molecular Weight:
122871.435 Da
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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Metal ion binding
Specific Function:
Catalyzes the formation of the signaling molecule cAMP in response to G-protein signaling. Mediates responses to increased cellular Ca(2+)/calmodulin levels (By similarity). May be involved in regulatory processes in the central nervous system. May play a role in memory and learning. Plays a role in the regulation of the circadian rhythm of daytime contrast sensitivity probably by modulating th...
Gene Name:
ADCY1
Uniprot ID:
Q08828
Uniprot Name:
Adenylate cyclase type 1
Molecular Weight:
123438.85 Da
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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Lage H: MDR1/P-glycoprotein (ABCB1) as target for RNA interference-mediated reversal of multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):813-21. [PubMed:16842213 ]
  2. Gardner ER, Burger H, van Schaik RH, van Oosterom AT, de Bruijn EA, Guetens G, Prenen H, de Jong FA, Baker SD, Bates SE, Figg WD, Verweij J, Sparreboom A, Nooter K: Association of enzyme and transporter genotypes with the pharmacokinetics of imatinib. Clin Pharmacol Ther. 2006 Aug;80(2):192-201. [PubMed:16890580 ]
  3. Blume H, Donath F, Warnke A, Schug BS: Pharmacokinetic drug interaction profiles of proton pump inhibitors. Drug Saf. 2006;29(9):769-84. [PubMed:16944963 ]
  4. Gervasini G, Carrillo JA, Garcia M, San Jose C, Cabanillas A, Benitez J: Adenosine triphosphate-binding cassette B1 (ABCB1) (multidrug resistance 1) G2677T/A gene polymorphism is associated with high risk of lung cancer. Cancer. 2006 Dec 15;107(12):2850-7. [PubMed:17120199 ]
  5. Fukui N, Suzuki Y, Sawamura K, Sugai T, Watanabe J, Inoue Y, Someya T: Dose-dependent effects of the 3435 C>T genotype of ABCB1 gene on the steady-state plasma concentration of fluvoxamine in psychiatric patients. Ther Drug Monit. 2007 Apr;29(2):185-9. [PubMed:17417072 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxin transporter activity
Specific Function:
Transporter involved in macrophage lipid homeostasis. Is an active component of the macrophage lipid export complex. Could also be involved in intracellular lipid transport processes. The role in cellular lipid homeostasis may not be limited to macrophages.
Gene Name:
ABCG1
Uniprot ID:
P45844
Uniprot Name:
ATP-binding cassette sub-family G member 1
Molecular Weight:
75591.275 Da
References
  1. Lage H: MDR1/P-glycoprotein (ABCB1) as target for RNA interference-mediated reversal of multidrug resistance. Curr Drug Targets. 2006 Jul;7(7):813-21. [PubMed:16842213 ]
  2. Materna V, Stege A, Surowiak P, Priebsch A, Lage H: RNA interference-triggered reversal of ABCC2-dependent cisplatin resistance in human cancer cells. Biochem Biophys Res Commun. 2006 Sep 15;348(1):153-7. Epub 2006 Jul 14. [PubMed:16876126 ]
  3. Thomas AC, Cullup T, Norgett EE, Hill T, Barton S, Dale BA, Sprecher E, Sheridan E, Taylor AE, Wilroy RS, DeLozier C, Burrows N, Goodyear H, Fleckman P, Stephens KG, Mehta L, Watson RM, Graham R, Wolf R, Slavotinek A, Martin M, Bourn D, Mein CA, O'Toole EA, Kelsell DP: ABCA12 is the major harlequin ichthyosis gene. J Invest Dermatol. 2006 Nov;126(11):2408-13. Epub 2006 Aug 10. [PubMed:16902423 ]
  4. Girardin F: Membrane transporter proteins: a challenge for CNS drug development. Dialogues Clin Neurosci. 2006;8(3):311-21. [PubMed:17117613 ]
  5. Pinkett HW, Lee AT, Lum P, Locher KP, Rees DC: An inward-facing conformation of a putative metal-chelate-type ABC transporter. Science. 2007 Jan 19;315(5810):373-7. Epub 2006 Dec 7. [PubMed:17158291 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Materna V, Stege A, Surowiak P, Priebsch A, Lage H: RNA interference-triggered reversal of ABCC2-dependent cisplatin resistance in human cancer cells. Biochem Biophys Res Commun. 2006 Sep 15;348(1):153-7. Epub 2006 Jul 14. [PubMed:16876126 ]
  2. Rau T, Erney B, Gores R, Eschenhagen T, Beck J, Langer T: High-dose methotrexate in pediatric acute lymphoblastic leukemia: impact of ABCC2 polymorphisms on plasma concentrations. Clin Pharmacol Ther. 2006 Nov;80(5):468-76. [PubMed:17112803 ]
  3. Li GX, Pei QL, Gao Y, Liu KM, Nie JS, Han G, Qiu YL, Zhang WP: Protective effects of hepatocellular canalicular conjugate export pump (Mrp2) on sodium arsenite-induced hepatic dysfunction in rats. Exp Toxicol Pathol. 2007 Aug;58(6):447-53. Epub 2007 Apr 30. [PubMed:17467962 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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) and N-ethylmaleimide S-glutathione (NEM-GS).Isoform 2: Inhibits TNF-alpha-mediated apoptosis through blocking one or more caspases.
Gene Name:
ABCC6
Uniprot ID:
O95255
Uniprot Name:
Multidrug resistance-associated protein 6
Molecular Weight:
164904.81 Da
References
  1. Ilias A, Urban Z, Seidl TL, Le Saux O, Sinko E, Boyd CD, Sarkadi B, Varadi A: Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). J Biol Chem. 2002 May 10;277(19):16860-7. Epub 2002 Mar 5. [PubMed:11880368 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Uniprot Name:
Multidrug resistance-associated protein 4
Molecular Weight:
149525.33 Da
References
  1. Sauna ZE, Peng XH, Nandigama K, Tekle S, Ambudkar SV: The molecular basis of the action of disulfiram as a modulator of the multidrug resistance-linked ATP binding cassette transporters MDR1 (ABCB1) and MRP1 (ABCC1). Mol Pharmacol. 2004 Mar;65(3):675-84. [PubMed:14978246 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Uniprot Name:
Multidrug resistance-associated protein 1
Molecular Weight:
171589.5 Da
References
  1. Westlake CJ, Payen L, Gao M, Cole SP, Deeley RG: Identification and characterization of functionally important elements in the multidrug resistance protein 1 COOH-terminal region. J Biol Chem. 2004 Dec 17;279(51):53571-83. Epub 2004 Sep 30. [PubMed:15459206 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
cofactor
General Function:
Pdz domain binding
Specific Function:
Involved in the transport of chloride ions. May regulate bicarbonate secretion and salvage in epithelial cells by regulating the SLC4A7 transporter. Can inhibit the chloride channel activity of ANO1. Plays a role in the chloride and bicarbonate homeostasis during sperm epididymal maturation and capacitation.
Gene Name:
CFTR
Uniprot ID:
P13569
Uniprot Name:
Cystic fibrosis transmembrane conductance regulator
Molecular Weight:
168139.895 Da
References
  1. Berger AL, Ikuma M, Welsh MJ: Normal gating of CFTR requires ATP binding to both nucleotide-binding domains and hydrolysis at the second nucleotide-binding domain. Proc Natl Acad Sci U S A. 2005 Jan 11;102(2):455-60. Epub 2004 Dec 27. [PubMed:15623556 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein serine/threonine kinase activity
Specific Function:
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in...
Gene Name:
PIK3CA
Uniprot ID:
P42336
Uniprot Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Molecular Weight:
124283.025 Da
References
  1. Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ: The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-t hieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d. [PubMed:18754654 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein serine/threonine kinase activity
Specific Function:
Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Regulates numerous cellular processes, such as cell cycle progression, apoptosis and transcription, as well as viral infection. May act as a regulatory node which integrates and coor...
Gene Name:
CSNK2A1
Uniprot ID:
P68400
Uniprot Name:
Casein kinase II subunit alpha
Molecular Weight:
45143.25 Da
References
  1. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM: Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21. [PubMed:21174434 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transcription factor binding
Specific Function:
Participates in Wnt signaling (By similarity). Plays a complex role in regulating the basal catalytic activity of the alpha subunit.
Gene Name:
CSNK2B
Uniprot ID:
P67870
Uniprot Name:
Casein kinase II subunit beta
Molecular Weight:
24942.25 Da
References
  1. Pierre F, Chua PC, O'Brien SE, Siddiqui-Jain A, Bourbon P, Haddach M, Michaux J, Nagasawa J, Schwaebe MK, Stefan E, Vialettes A, Whitten JP, Chen TK, Darjania L, Stansfield R, Anderes K, Bliesath J, Drygin D, Ho C, Omori M, Proffitt C, Streiner N, Trent K, Rice WG, Ryckman DM: Discovery and SAR of 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid (CX-4945), the first clinical stage inhibitor of protein kinase CK2 for the treatment of cancer. J Med Chem. 2011 Jan 27;54(2):635-54. doi: 10.1021/jm101251q. Epub 2010 Dec 21. [PubMed:21174434 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Receptor activity
Specific Function:
Receptor for ATP and ADP coupled to G-proteins that activate both phosphatidylinositol-calcium and adenylyl cyclase second messenger systems. Not activated by UTP or UDP.
Gene Name:
P2RY11
Uniprot ID:
Q96G91
Uniprot Name:
P2Y purinoceptor 11
Molecular Weight:
40344.755 Da
References
  1. Xiao Z, Yang M, Lv Q, Wang W, Deng M, Liu X, He Q, Chen X, Chen M, Fang L, Xie X, Hu J: P2Y11 impairs cell proliferation by induction of cell cycle arrest and sensitizes endothelial cells to cisplatin-induced cell death. J Cell Biochem. 2011 Sep;112(9):2257-65. doi: 10.1002/jcb.23144. [PubMed:21503959 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Signal transducer activity
Specific Function:
Serine/threonine-protein phosphatase that dephosphorylates a myriad of proteins involved in different signaling pathways including the kinases CSNK1E, ASK1/MAP3K5, PRKDC and RAF1, the nuclear receptors NR3C1, PPARG, ESR1 and ESR2, SMAD proteins and TAU/MAPT. Implicated in wide ranging cellular processes, including apoptosis, differentiation, DNA damage response, cell survival, regulation of ion...
Gene Name:
PPP5C
Uniprot ID:
P53041
Uniprot Name:
Serine/threonine-protein phosphatase 5
Molecular Weight:
56878.22 Da
References
  1. Hong TJ, Kim S, Wi AR, Lee P, Kang M, Jeong JH, Hahn JS: Dynamic nucleotide-dependent interactions of cysteine- and histidine-rich domain (CHORD)-containing Hsp90 cochaperones Chp-1 and melusin with cochaperones PP5 and Sgt1. J Biol Chem. 2013 Jan 4;288(1):215-22. doi: 10.1074/jbc.M112.398636. Epub 2012 Nov 26. [PubMed:23184943 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Poly(a) rna binding
Specific Function:
ATP dependent phosphorylation of adenosine and other related nucleoside analogs to monophosphate derivatives. Serves as a potential regulator of concentrations of extracellular adenosine and intracellular adenine nucleotides.
Gene Name:
ADK
Uniprot ID:
P55263
Uniprot Name:
Adenosine kinase
Molecular Weight:
40545.075 Da
References
  1. Park J, Gupta RS: Adenosine kinase and ribokinase--the RK family of proteins. Cell Mol Life Sci. 2008 Sep;65(18):2875-96. doi: 10.1007/s00018-008-8123-1. [PubMed:18560757 ]
  2. Leoncini R, Vannoni D, Santoro A, Giglioni S, Carli R, Marinello E: Adenosine kinase from rat liver: new biochemical properties. Nucleosides Nucleotides Nucleic Acids. 2006;25(9-11):1107-12. [PubMed:17065073 ]
Drug created on June 13, 2005 07:24 / Updated on August 02, 2017 16:20