Target Information

Target General Infomation
Target ID
T13491
Former ID
TTDS00430
Target Name
Equilibrative nucleoside transporter 1
Gene Name
SLC29A1
Synonyms
ENT1; Equilibrative NBMPR-sensitive nucleoside transporter; Equilibrative nitrobenzylmercaptopurine riboside-sensitive nucleoside transporter; Nucleoside transporter 1; Nucleoside transporter, es-type; Solute carrier family 29 member 1; SLC29A1
Target Type
Successful
Disease Angina pectoris [ICD9: 413; ICD10: I20]
Function
Mediates 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.
BioChemical Class
Transmembrane protein
Target Validation
T13491
UniProt ID
Q99808
Sequence
MTTSHQPQDRYKAVWLIFFMLGLGTLLPWNFFMTATQYFTNRLDMSQNVSLVTAELSKDA
QASAAPAAPLPERNSLSAIFNNVMTLCAMLPLLLFTYLNSFLHQRIPQSVRILGSLVAIL
LVFLITAILVKVQLDALPFFVITMIKIVLINSFGAILQGSLFGLAGLLPASYTAPIMSGQ
GLAGFFASVAMICAIASGSELSESAFGYFITACAVIILTIICYLGLPRLEFYRYYQQLKL
EGPGEQETKLDLISKGEEPRAGKEESGVSVSNSQPTNESHSIKAILKNISVLAFSVCFIF
TITIGMFPAVTVEVKSSIAGSSTWERYFIPVSCFLTFNIFDWLGRSLTAVFMWPGKDSRW
LPSLVLARLVFVPLLLLCNIKPRRYLTVVFEHDAWFIFFMAAFAFSNGYLASLCMCFGPK
KVKPAEAETAGAIMAFFLCLGLALGAVFSFLFRAIV
Drugs and Mode of Action
Drug(s) LIDOFLAZINE Drug Info Approved Angina pectoris [1]
Inhibitor 6-(4-Nitro-benzylsulfanyl)-9-phenethyl-9H-purine Drug Info [2]
9-Benzyl-6-(4-nitro-benzylsulfanyl)-9H-purine Drug Info [2]
Dilazep Drug Info [3]
KF24345 Drug Info [4]
LIDOFLAZINE Drug Info [5]
N6-CYCLOPENTYLADENOSINE Drug Info [6]
NBTGR Drug Info [7]
Nitrobenzylthioinosine Drug Info [8]
S6-nitrobenzyl mercaptopurine riboside Drug Info [9]
Modulator [3H]nitrobenzylmercaptopurine ribonucleoside Drug Info [7]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
DRM DRM Info
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2J 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.
REF 3Residues 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.
REF 4Interaction of the novel adenosine uptake inhibitor 3-[1-(6,7-diethoxy-2-morpholinoquinazolin-4-yl)piperidin-4-yl]-1,6-dimethyl-2,4(1H,3H)-quinazolinedione hydrochloride (KF24345) with the es and ei subtypes of equilibrative nucleoside transporters. J Pharmacol Exp Ther. 2004 Mar;308(3):1083-93. Epub 2003 Nov 21.
REF 5J 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.
REF 6J Med Chem. 2005 Jan 13;48(1):321-9.Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines.
REF 7(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1117).
REF 8The role of human nucleoside transporters in uptake of 3'-deoxy-3'-fluorothymidine. Mol Pharmacol. 2008 Nov;74(5):1372-80. Epub 2008 Jul 31.
REF 9Bioorg 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.

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