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Identification
NameStreptomycin
Accession NumberDB01082  (APRD00412)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

Streptomycin is an aminoglycoside antibiotic produced by the soil actinomycete Streptomyces griseus. It acts by binding to the 30S ribosomal subunit of susceptible organisms and disrupting the initiation and elongation steps in protein synthesis. It is bactericidal due to effects that are not fully understood.

Structure
Thumb
Synonyms
[2-Deoxy-2-(dimethylamino)-alpha-L-glucopyranosyl]-(1->2)-[5-deoxy-3-C-formyl-alpha-L-lyxofuranosyl]-(1->4)-{n',n'''-[(1,3,5/2,4,6)-2,4,5,6-tetrahydroxycyclohexane-1,3-diyl]diguanidine}
2,4-Diguanidino-3,5,6-trihydroxycyclohexyl 5-deoxy-2-O-(2-deoxy-2-methylamino-alpha-L-glucopyranosyl)-3-C-formyl-beta-L-lyxopentanofuranoside
Kantrex
SM
STREPTOMYCIN
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Streptomycin for Injection USPpowder for solution1 gintramuscularSterimax Inc2001-10-15Not applicableCanada
Streptomycin Sulfate Injection USP 1g/2.5mlliquid1 gintramuscular; refer (see dosage form)Pfizer Canada Inc1993-12-312000-07-26Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Streptomycininjection, powder, lyophilized, for solution1 g/1intramuscularX Gen Pharmaceuticals, Inc.1998-06-30Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Streptomycin Sulfate
Thumb
  • InChI Key: CFCMMYICHMLDCC-QXQFOYBSSA-N
  • Monoisotopic Mass: 679.233048989
  • Average Mass: 679.653
DBSALT000422
Categories
UNIIY45QSO73OB
CAS number57-92-1
WeightAverage: 581.5741
Monoisotopic: 581.265669747
Chemical FormulaC21H39N7O12
InChI KeyInChIKey=UCSJYZPVAKXKNQ-HZYVHMACSA-N
InChI
InChI=1S/C21H39N7O12/c1-5-21(36,4-30)16(40-17-9(26-2)13(34)10(31)6(3-29)38-17)18(37-5)39-15-8(28-20(24)25)11(32)7(27-19(22)23)12(33)14(15)35/h4-18,26,29,31-36H,3H2,1-2H3,(H4,22,23,27)(H4,24,25,28)/t5-,6-,7+,8-,9-,10-,11+,12-,13-,14+,15+,16-,17-,18-,21+/m0/s1
IUPAC Name
1-[(1R,2R,3S,4R,5R,6S)-3-carbamimidamido-4-{[(2R,3R,4R,5S)-3-{[(2S,3S,4S,5R,6S)-4,5-dihydroxy-6-(hydroxymethyl)-3-(methylamino)oxan-2-yl]oxy}-4-formyl-4-hydroxy-5-methyloxolan-2-yl]oxy}-2,5,6-trihydroxycyclohexyl]guanidine
SMILES
CN[[email protected]]1[[email protected]](O)[C@@H](O)[[email protected]](CO)O[[email protected]]1O[[email protected]]1[[email protected]](O[[email protected]]2[[email protected]](O)[C@@H](O)[[email protected]](NC(N)=N)[C@@H](O)[C@@H]2NC(N)=N)O[C@@H](C)[C@]1(O)C=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as aminocyclitol glycosides. These are organic compounds containing an amicocyclitol moiety glycosidically linked to a carbohydrate moiety. There are two major classes of aminoglycosides containing a 2-streptamine core. They are called 4,5- and 4,6-disubstituted 2-deoxystreptamines.
KingdomOrganic compounds
Super ClassOrganooxygen compounds
ClassCarbohydrates and carbohydrate conjugates
Sub ClassAminosaccharides
Direct ParentAminocyclitol glycosides
Alternative Parents
Substituents
  • Amino cyclitol glycoside
  • Streptamine aminoglycoside
  • Glucosamine
  • Amino sugar
  • O-glycosyl compound
  • Glycosyl compound
  • Aminocyclitol derivative
  • Cyclitol derivative
  • Cyclohexylamine
  • Cyclohexanol
  • Oxane
  • Monosaccharide
  • Tertiary alcohol
  • Oxolane
  • Cyclic alcohol
  • Secondary alcohol
  • Polyol
  • Guanidine
  • 1,2-diol
  • 1,2-aminoalcohol
  • Oxacycle
  • Organoheterocyclic compound
  • Carboximidamide
  • Secondary amine
  • Secondary aliphatic amine
  • Acetal
  • Hydrocarbon derivative
  • Primary alcohol
  • Organonitrogen compound
  • Imine
  • Carbonyl group
  • Amine
  • Aldehyde
  • Alcohol
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of tuberculosis. May also be used in combination with other drugs to treat tularemia (Francisella tularensis), plague (Yersia pestis), severe M. avium complex, brucellosis, and enterococcal endocarditis (e.g. E. faecalis, E. faecium).
PharmacodynamicsStreptomycin is an aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses.
Mechanism of actionAminoglycosides like Streptomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Streptomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.
Related Articles
AbsorptionRapidly absorbed after intramuscular injection with peak serum concentrations attained after 1 - 2 hours. Not absorbed in the GI tract.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationSmall amounts are excreted in milk, saliva, and sweat. Streptomycin is excreted by glomerular filtration.
Half life5 - 6 hours in adults with normal renal function
ClearanceNot Available
ToxicityNephrotoxic and ototoxic potential. Nephrotoxicity is caused by accumulation of the drug in proximal renal tubular cells, which results in cellular damage. Tubular cells may regenerate despite continued exposure and nephrotoxicity is usually mild and reversible. Streptomycin is the least nephrotoxic of the aminoglycosides owing to the small number of cationic amino groups in its structure. Otoxocity occurs via drug accumulation in the endolymph and perilymph of the inner ear. Accumulation causes irreversible damage to hair cells of the cochlea or summit of the ampullar cristae of the vestibular complex. High frequency hearing loss precedes low frequency hearing loss. Further toxicity may result in retrograde degeneration of the auditory nerve. Vestibular toxicity may result in vertigo, nausea and vomiting, dizziness and loss of balance. LD50=430 mg/kg (Orally in rats with Streptomycin Sulfate); Side effects include nausea, vomiting, and vertigo, paresthesia of face, rash, fever, urticaria, angioneurotic edema, and eosinophilia.
Affected organisms
  • Enteric bacteria and other eubacteria
  • Mycobacteria
  • Mycobacterium tuberculosis
  • Yersinia pestis
  • Francisella tularensis
  • Staphylococcus aureus
  • Enterococcus faecalis
Pathways
PathwayCategorySMPDB ID
Streptomycin Action PathwayDrug actionSMP00259
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8824
Blood Brain Barrier-0.9712
Caco-2 permeable-0.6968
P-glycoprotein substrateSubstrate0.5531
P-glycoprotein inhibitor INon-inhibitor0.7577
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterNon-inhibitor0.7782
CYP450 2C9 substrateNon-substrate0.7053
CYP450 2D6 substrateNon-substrate0.8177
CYP450 3A4 substrateNon-substrate0.5275
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9072
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8867
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8818
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.9528
BiodegradationNot ready biodegradable0.9821
Rat acute toxicity1.8409 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9924
hERG inhibition (predictor II)Non-inhibitor0.9009
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintramuscular1 g/1
Powder for solutionintramuscular1 g
Liquidintramuscular; refer (see dosage form)1 g
Prices
Unit descriptionCostUnit
Streptomycin sulf 1 gm vial14.65USD vial
Streptomycin sulfate powder0.82USD g
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP-6.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility12.8 mg/mLALOGPS
logP-2.6ALOGPS
logP-7.7ChemAxon
logS-1.7ALOGPS
pKa (Strongest Acidic)10.88ChemAxon
pKa (Strongest Basic)11.9ChemAxon
Physiological Charge3ChemAxon
Hydrogen Acceptor Count19ChemAxon
Hydrogen Donor Count14ChemAxon
Polar Surface Area331.43 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity149.47 m3·mol-1ChemAxon
Polarizability55.76 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
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
References
Synthesis Reference

Arnold L. Demain, Kozo Nagaoka, “Derivatives of streptomycin and method of producing streptomycin derivatives by mutational biosynthesis.” U.S. Patent US3993544, issued November 23, 1976.

US3993544
General ReferencesNot Available
External Links
ATC CodesJ01GA01J04AM01A07AA04A07AA54
AHFS Codes
  • 08:12.02
PDB Entries
FDA labelNot Available
MSDSDownload (73.7 KB)
Interactions
Drug Interactions
Drug
Alendronic acidStreptomycin may increase the activities of Alendronate.
AmdinocillinThe serum concentration of Streptomycin can be decreased when it is combined with Amdinocillin.
AmoxicillinThe serum concentration of Streptomycin can be decreased when it is combined with Amoxicillin.
Amphotericin BAmphotericin B may increase the nephrotoxic activities of Streptomycin.
AmpicillinThe serum concentration of Streptomycin can be decreased when it is combined with Ampicillin.
Atracurium besylateStreptomycin may increase the activities of Atracurium besylate.
AvibactamAvibactam may increase the nephrotoxic activities of Streptomycin.
AzidocillinThe serum concentration of Streptomycin can be decreased when it is combined with Azidocillin.
AzlocillinThe serum concentration of Streptomycin can be decreased when it is combined with Azlocillin.
BacampicillinThe serum concentration of Streptomycin can be decreased when it is combined with Bacampicillin.
BacitracinStreptomycin may increase the nephrotoxic activities of Bacitracin.
BenzylpenicillinThe serum concentration of Streptomycin can be decreased when it is combined with Benzylpenicillin.
Botulinum Toxin Type AStreptomycin may increase the neuromuscular blocking activities of Botulinum Toxin Type A.
Botulinum Toxin Type BStreptomycin may increase the neuromuscular blocking activities of Botulinum Toxin Type B.
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Streptomycin.
CapreomycinCapreomycin may increase the neuromuscular blocking activities of Streptomycin.
CarbenicillinThe serum concentration of Streptomycin can be decreased when it is combined with Carbenicillin.
CarboplatinStreptomycin may increase the ototoxic activities of Carboplatin.
CefaclorCefaclor may increase the nephrotoxic activities of Streptomycin.
CefdinirCefdinir may increase the nephrotoxic activities of Streptomycin.
CefepimeCefepime may increase the nephrotoxic activities of Streptomycin.
CefiximeCefixime may increase the nephrotoxic activities of Streptomycin.
CefmenoximeCefmenoxime may increase the nephrotoxic activities of Streptomycin.
CefotaximeCefotaxime may increase the nephrotoxic activities of Streptomycin.
CefotetanCefotetan may increase the nephrotoxic activities of Streptomycin.
CefoxitinCefoxitin may increase the nephrotoxic activities of Streptomycin.
CefpodoximeCefpodoxime may increase the nephrotoxic activities of Streptomycin.
CefprozilCefprozil may increase the nephrotoxic activities of Streptomycin.
CeftazidimeCeftazidime may increase the nephrotoxic activities of Streptomycin.
CeftibutenCeftibuten may increase the nephrotoxic activities of Streptomycin.
CeftriaxoneCeftriaxone may increase the nephrotoxic activities of Streptomycin.
CefuroximeCefuroxime may increase the nephrotoxic activities of Streptomycin.
CelecoxibCelecoxib may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
Cisatracurium besylateStreptomycin may increase the activities of Cisatracurium besylate.
CisplatinCisplatin may increase the nephrotoxic activities of Streptomycin.
ClavulanateThe serum concentration of Streptomycin can be decreased when it is combined with Clavulanate.
ClodronateStreptomycin may increase the activities of Clodronate.
CloxacillinThe serum concentration of Streptomycin can be decreased when it is combined with Cloxacillin.
ColistimethateStreptomycin may increase the nephrotoxic activities of Colistimethate.
ColistinStreptomycin may increase the nephrotoxic activities of Colistin.
CyclacillinThe serum concentration of Streptomycin can be decreased when it is combined with Cyclacillin.
CyclosporineStreptomycin may increase the nephrotoxic activities of Cyclosporine.
DiclofenacDiclofenac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
DicloxacillinThe serum concentration of Streptomycin can be decreased when it is combined with Dicloxacillin.
DiflunisalDiflunisal may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
DigoxinThe serum concentration of Digoxin can be decreased when it is combined with Streptomycin.
Etacrynic acidThe risk or severity of adverse effects can be increased when Ethacrynic acid is combined with Streptomycin.
EtodolacEtodolac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
FenoprofenFenoprofen may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
FloctafenineFloctafenine may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
FlucloxacillinThe serum concentration of Streptomycin can be decreased when it is combined with Flucloxacillin.
FlurbiprofenFlurbiprofen may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
FoscarnetFoscarnet may increase the nephrotoxic activities of Streptomycin.
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Streptomycin.
HetacillinThe serum concentration of Streptomycin can be decreased when it is combined with Hetacillin.
IbandronateStreptomycin may increase the activities of Ibandronate.
IbuprofenIbuprofen may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
IndomethacinIndomethacin may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
InfliximabInfliximab may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
KetoprofenKetoprofen may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
KetorolacKetorolac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
MannitolMannitol may increase the nephrotoxic activities of Streptomycin.
MecamylamineStreptomycin may increase the neuromuscular blocking activities of Mecamylamine.
Mefenamic acidMefenamic acid may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
MeloxicamMeloxicam may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
MeticillinThe serum concentration of Streptomycin can be decreased when it is combined with Meticillin.
MezlocillinThe serum concentration of Streptomycin can be decreased when it is combined with Mezlocillin.
NabumetoneNabumetone may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
NafcillinThe serum concentration of Streptomycin can be decreased when it is combined with Nafcillin.
NaproxenNaproxen may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
OxacillinThe serum concentration of Streptomycin can be decreased when it is combined with Oxacillin.
OxaprozinOxaprozin may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
PamidronateStreptomycin may increase the activities of Pamidronate.
PancuroniumStreptomycin may increase the activities of Pancuronium.
PhenoxymethylpenicillinThe serum concentration of Streptomycin can be decreased when it is combined with Phenoxymethylpenicillin.
Picosulfuric acidThe therapeutic efficacy of Sodium picosulfate can be decreased when used in combination with Streptomycin.
PiperacillinThe serum concentration of Streptomycin can be decreased when it is combined with Piperacillin.
PiroxicamPiroxicam may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
PivampicillinThe serum concentration of Streptomycin can be decreased when it is combined with Pivampicillin.
PivmecillinamThe serum concentration of Streptomycin can be decreased when it is combined with Pivmecillinam.
RisedronateStreptomycin may increase the activities of Risedronate.
RocuroniumStreptomycin may increase the activities of Rocuronium.
SuccinylcholineStreptomycin may increase the activities of Succinylcholine.
SulindacSulindac may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
TenofovirThe serum concentration of Streptomycin can be increased when it is combined with Tenofovir.
Tiaprofenic acidTiaprofenic acid may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
TicarcillinThe serum concentration of Streptomycin can be decreased when it is combined with Ticarcillin.
TiludronateStreptomycin may increase the activities of Tiludronate.
TolmetinTolmetin may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Streptomycin.
VancomycinVancomycin may increase the nephrotoxic activities of Streptomycin.
VecuroniumStreptomycin may increase the activities of Vecuronium.
Zoledronic acidStreptomycin may increase the activities of Zoledronate.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Escherichia coli (strain K12)
Pharmacological action
yes
Actions
inhibitor
General Function:
Trna binding
Specific Function:
With S4 and S5 plays an important role in translational accuracy.Interacts with and stabilizes bases of the 16S rRNA that are involved in tRNA selection in the A site and with the mRNA backbone. Located at the interface of the 30S and 50S subunits, it traverses the body of the 30S subunit contacting proteins on the other side and probably holding the rRNA structure together. The combined cluste...
Gene Name:
rpsL
Uniprot ID:
P0A7S3
Molecular Weight:
13736.995 Da
References
  1. Mieskes KT, Rusch-Gerdes S, Truffot-Pernot C, Feldmann K, Tortoli E, Casal M, Loscher T, Rinder H: Rapid, simple, and culture-independent detection of rpsL codon 43 mutations that are highly predictive of streptomycin resistance in Mycobacterium tuberculosis. Am J Trop Med Hyg. 2000 Jul-Aug;63(1-2):56-60. [PubMed:11357996 ]
  2. Kenney TJ, Churchward G: Cloning and sequence analysis of the rpsL and rpsG genes of Mycobacterium smegmatis and characterization of mutations causing resistance to streptomycin. J Bacteriol. 1994 Oct;176(19):6153-6. [PubMed:7928982 ]
  3. Fukuda M, Koga H, Ohno H, Ogawa K, Yang B, Miyamoto J, Tomono K, Kohno S: [Relationship between streptomycin susceptibility and rpsL mutations of Mycobacterium tuberculosis strains]. Kekkaku. 1997 Sep;72(9):507-13. [PubMed:9364810 ]
2. 16S rRNA
Kind
Nucleotide
Organism
Enteric bacteria and other eubacteria
Pharmacological action
yes
Actions
inhibitor
References
  1. Okamoto S, Tamaru A, Nakajima C, Nishimura K, Tanaka Y, Tokuyama S, Suzuki Y, Ochi K: Loss of a conserved 7-methylguanosine modification in 16S rRNA confers low-level streptomycin resistance in bacteria. Mol Microbiol. 2007 Feb;63(4):1096-106. [PubMed:17238915 ]
  2. Nishimura K, Hosaka T, Tokuyama S, Okamoto S, Ochi K: Mutations in rsmG, encoding a 16S rRNA methyltransferase, result in low-level streptomycin resistance and antibiotic overproduction in Streptomyces coelicolor A3(2). J Bacteriol. 2007 May;189(10):3876-83. Epub 2007 Mar 23. [PubMed:17384192 ]
  3. Vila-Sanjurjo A, Lu Y, Aragonez JL, Starkweather RE, Sasikumar M, O'Connor M: Modulation of 16S rRNA function by ribosomal protein S12. Biochim Biophys Acta. 2007 Jul-Aug;1769(7-8):462-71. Epub 2007 Apr 20. [PubMed:17512991 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Protein-arginine deiminase activity
Specific Function:
Catalyzes the citrullination/deimination of arginine residues of proteins such as histones, thereby playing a key role in histone code and regulation of stem cell maintenance. Citrullinates histone H1 at 'Arg-54' (to form H1R54ci), histone H3 at 'Arg-2', 'Arg-8', 'Arg-17' and/or 'Arg-26' (to form H3R2ci, H3R8ci, H3R17ci, H3R26ci, respectively) and histone H4 at 'Arg-3' (to form H4R3ci). Acts as...
Gene Name:
PADI4
Uniprot ID:
Q9UM07
Molecular Weight:
74078.65 Da
References
  1. Knuckley B, Luo Y, Thompson PR: Profiling Protein Arginine Deiminase 4 (PAD4): a novel screen to identify PAD4 inhibitors. Bioorg Med Chem. 2008 Jan 15;16(2):739-45. Epub 2007 Oct 13. [PubMed:17964793 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Jariyawat S, Sekine T, Takeda M, Apiwattanakul N, Kanai Y, Sophasan S, Endou H: The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1. J Pharmacol Exp Ther. 1999 Aug;290(2):672-7. [PubMed:10411577 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23