Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00430

Target Information
NameEquilibrative nucleoside transporter 1    
Type of targetSuccessful target    
SynonymsENT1    
Equilibrative NBMPR-sensitive nucleoside transporter    
Equilibrative nitrobenzylmercaptopurine riboside-sensitive nucleoside transporter    
Nucleoside transporter 1    
Nucleoside transporter, es-type    
Solute carrier family 29 member 1    
DiseaseMalaria
[ICD9: 084   ICD10: B50-B54]
[1][2][3][4]
BioChemical ClassTransmembrane protein    
UniProt IDQ99808
Q9NIH7
FunctionMediates both influx and efflux of nucleosides across the membrane (equilibrative transporter). It is sensitive to low concentrations of the inhibitor nitrobenzylmercaptopurine riboside (nbmpr) and is sodium-independent.    
SequenceMTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVSLVTAELSKDA QASAAPAAPLPERNSLSAIFNNVMTLCAMLPLLLFTYLNSFLHQRIPQSVRILGSLVAIL LVFLITAILVKVQLDALPFFVITMIKIVLINSFGAILQGSLFGLAGLLPASYTAPIMSGQ GLAGFFASVAMICAIASGSELSESAFGYFITACAVIILTIICYLGLPRLEFYRYYQQLKL EGPGEQETKLDLISKGEEPRAGKEESGVSVSNSQPTNESHSIKAILKNISVLAFSVCFIF TITIGMFPAVTVEVKSSIAGSSTWERYFIPVSCFLTFNIFDWLGRSLTAVFMWPGKDSRW LPSLVLARLVFVPLLLLCNIKPRRYLTVVFEHDAWFIFFMAAFAFSNGYLASLCMCFGPK KVKPAEAETAGAIMAFFLCLGLALGAVFSFLFRAIV
Target ValidationClick to Find Target Validation Information.    
Inhibitor6- (4-Nitro-benzylsulfanyl)-9-phenethyl-9H-purine[5]
9-Benzyl-6- (4-nitro-benzylsulfanyl)-9H-purine[5]
Dilazep[6]
Dipyridamole[6]
LIDOFLAZINE[7]
N6-CYCLOPENTYLADENOSINE[8]
Nitrobenzylthioinosine[9]
S6-nitrobenzyl mercaptopurine riboside[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Nucleoside transport as a potential target for chemotherapy in malaria. Curr Pharm Des. 2007;13(6):569-80. To Reference
Ref 2How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 3Transport of nucleosides across the Plasmodium falciparum parasite plasma membrane has characteristics of PfENT1. Mol Microbiol. 2006 May;60(3):738-48. To Reference
Ref 4Identification of a nucleoside/nucleobase transporter from Plasmodium falciparum, a novel target for anti-malarial chemotherapy. Biochem J. 2000 Jul 1;349(Pt 1):67-75. To Reference
Ref 5J Med Chem. 2004 Oct 21;47(22):5441-50.Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups. To Reference
Ref 6Residues Met89 and Ser160 in the human equilibrative nucleoside transporter 1 affect its affinity for adenosine, guanosine, S6-(4-nitrobenzyl)-mercaptopurine riboside, and dipyridamole. Mol Pharmacol. 2005 Mar;67(3):837-44. Epub 2004 Nov 19. To Reference
Ref 7J Med Chem. 2007 Aug 9;50(16):3906-20. Epub 2007 Jul 18.Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors. To Reference
Ref 8J Med Chem. 2005 Jan 13;48(1):321-9.Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines. To Reference
Ref 9The role of human nucleoside transporters in uptake of 3'-deoxy-3'-fluorothymidine. Mol Pharmacol. 2008 Nov;74(5):1372-80. Epub 2008 Jul 31. To Reference
Ref 10Bioorg Med Chem Lett. 2009 Feb 1;19(3):917-21. Epub 2008 Dec 6.Synthesis and biological evaluation of phloridzin analogs as human concentrative nucleoside transporter 3 (hCNT3) inhibitors. To Reference



 

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