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Chemical Compound Review

AC1LABND     [(2S,5R)-5-[2-amino-6-[(4...

Synonyms: AG-J-85320, CTK7J7120
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Disease relevance of AIDS-106810


Psychiatry related information on AIDS-106810

  • In the present study, we measured the binding of nitrobenzylthioinosine (NBMPR), an ENT1 transporter inhibitor, and the ENT1 transporter mRNA after prolonged wakefulness and recovery sleep [6].

High impact information on AIDS-106810

  • However, in contrast to nucleoside transport in wild-type cells, residual nucleoside transport in AE1 cells was resistant to inhibition by nitrobenzylthioinosine [7].
  • Liver parenchymal cells show low and negligible mRNA levels for rENT1 and rENT2 transporters, respectively, although most of the equilibrative transport activity found in hepatocytes is NBTI-resistant [8].
  • Nitrobenzylthioinosine, another nucleoside membrane transport inhibitor, did not enhance DDP cytotoxicity or uptake at concentrations that produced equivalent degrees of inhibition of [3H]uridine uptake [9].
  • Cytidine, uridine, and nitrobenzylthioinosine all strongly repressed the anabolic phosphorylation of CPEC when added to Molt-4 cells along with the drug.(ABSTRACT TRUNCATED AT 400 WORDS)[10]
  • Transport and metabolism of 9-beta-D-arabinofuranosylguanine in a human T-lymphoblastoid cell line: nitrobenzylthioinosine-sensitive and -insensitive influx [11].

Chemical compound and disease context of AIDS-106810


Biological context of AIDS-106810

  • We have used enzymic cleavage by trypsin in conjunction with glycosidase digestion to probe the transmembrane topologies and molecular structures of mammalian equilibrative, nitrobenzylthioinosine (NBMPR)-sensitive, nucleoside transport systems [15].
  • L1210 mouse leukemia cells exhibit two distinct types of nucleoside transport activity that have similar kinetic properties and substrate specificity, but differ markedly in their sensitivity to the inhibitor nitrobenzylthioinosine (NBMPR) (Belt, J. A. (1983) Mol. Pharmacol. 24, 479-484) [16].
  • Mammalian nitrobenzylthioinosine-sensitive nucleoside transport proteins. Immunological evidence that transporters differing in size and inhibitor specificity share sequence homology [17].
  • Two distinct high-affinity synaptosomal membrane-associated [3H]dipyridamole binding sites, with different sensitivities to inhibition by nitrobenzylthioinosine, were characterized in the presence of 3-[(3-cholamidopropyl) dimethylammonio]-1-propanesulfonate (CHAPS, 0.01%) to prevent [3H]dipyridamole binding to glass tubes and filters [18].
  • The dose-response curve for the inhibition of uridine transport by nitrobenzylthioinosine (NBMPR) was biphasic: approx. 40% of the transport activity was inhibited with an IC50 (concentration causing half-maximal inhibition) value of 0.5 nM, but the remaining activity was insensitive to concentrations as high as 1 microM [19].

Anatomical context of AIDS-106810


Associations of AIDS-106810 with other chemical compounds


Gene context of AIDS-106810

  • The human (h) and rat (r) equilibrative (Na(+)-independent) nucleoside transporters (ENTs) hENT1, rENT1, hENT2, and rENT2 belong to a family of integral membrane proteins with 11 transmembrane domains (TMs) and are distinguished functionally by differences in sensitivity to inhibition by nitrobenzylthioinosine and coronary vasoactive drugs [27].
  • Molecular cloning and functional characterization of nitrobenzylthioinosine (NBMPR)-sensitive (es) and NBMPR-insensitive (ei) equilibrative nucleoside transporter proteins (rENT1 and rENT2) from rat tissues [28].
  • Influx of paracrinally generated cADPR into clonogenic HP was mediated by a concentrative, nitrobenzylthioinosine- and dipyridamole-inhibitable nucleoside transporter, this providing a possible explanation to the effectiveness of the hormone-like concentrations of the cyclic nucleotide measured in the medium conditioned by BST-1(+) feeders [29].
  • Mammalian cells express at least two subtypes of equilibrative nucleoside transporters, i.e. ENT1 and ENT2, which can be distinguished functionally by their sensitivity and resistance respectively to inhibition by nitrobenzylthioinosine [30].
  • Two subtypes of equilibrative transporters have been defined by their differential sensitivities to inhibition by nitrobenzylthioinosine (NBMPR; es/ENT1, sensitive; ei/ENT2, insensitive) [31].

Analytical, diagnostic and therapeutic context of AIDS-106810


  1. Combination therapy of schistosomiasis by tubercidin and nitrobenzylthioinosine 5'-monophosphate. el Kouni, M.H., Diop, D., Cha, S. Proc. Natl. Acad. Sci. U.S.A. (1983) [Pubmed]
  2. Sensitivity of acute leukemia cells to cytarabine is a correlate of cellular es nucleoside transporter site content measured by flow cytometry with SAENTA-fluorescein. Gati, W.P., Paterson, A.R., Larratt, L.M., Turner, A.R., Belch, A.R. Blood (1997) [Pubmed]
  3. Therapy of mouse leukemia L1210 with combinations of nebularine and nitrobenzylthioinosine 5'-monophosphate. Lynch, T.P., Paran, J.H., Paterson, A.R. Cancer Res. (1981) [Pubmed]
  4. Transport and metabolism of 1-beta-D-arabinofuranosylcytosine in human ovarian adenocarcinoma cells. Jamieson, G.P., Snook, M.B., Bradley, T.R., Bertoncello, I., Wiley, J.S. Cancer Res. (1989) [Pubmed]
  5. Mitochondrial expression of the human equilibrative nucleoside transporter 1 (hENT1) results in enhanced mitochondrial toxicity of antiviral drugs. Lai, Y., Tse, C.M., Unadkat, J.D. J. Biol. Chem. (2004) [Pubmed]
  6. Nitrobenzylthioinosine (NBMPR) binding and nucleoside transporter ENT1 mRNA expression after prolonged wakefulness and recovery sleep in the cortex and basal forebrain of rat. Alanko, L., Stenberg, D., Porkka-Heiskanen, T. Journal of sleep research. (2003) [Pubmed]
  7. Residual nitrobenzylthioinosine-resistant nucleoside transport in a transport mutant (AE1) of S49 murine T-lymphoma cells. Plagemann, P.G., Woffendin, C. Mol. Cell. Biol. (1987) [Pubmed]
  8. Differential expression and regulation of nucleoside transport systems in rat liver parenchymal and hepatoma cells. del Santo, B., Valdés, R., Mata, J., Felipe, A., Casado, F.J., Pastor-Anglada, M. Hepatology (1998) [Pubmed]
  9. Synergism between dipyridamole and cisplatin in human ovarian carcinoma cells in vitro. Jekunen, A., Vick, J., Sanga, R., Chan, T.C., Howell, S.B. Cancer Res. (1992) [Pubmed]
  10. Cellular pharmacology of cyclopentenyl cytosine in Molt-4 lymphoblasts. Ford, H., Cooney, D.A., Ahluwalia, G.S., Hao, Z., Rommel, M.E., Hicks, L., Dobyns, K.A., Tomaszewski, J.E., Johns, D.G. Cancer Res. (1991) [Pubmed]
  11. Transport and metabolism of 9-beta-D-arabinofuranosylguanine in a human T-lymphoblastoid cell line: nitrobenzylthioinosine-sensitive and -insensitive influx. Prus, K.L., Averett, D.R., Zimmerman, T.P. Cancer Res. (1990) [Pubmed]
  12. Combination therapy of mouse leukemia L1210 by 1-beta-D-arabinofuranosylcytosine and 6-[(4-nitrobenzyl)thio]-9-beta-D-ribofuranosylpurine. Cass, C.E., Muzik, H., Paterson, A.R. Cancer Res. (1975) [Pubmed]
  13. Effects of nitrobenzylthioinosine on neuronal injury, adenosine levels, and adenosine receptor activity in rat forebrain ischemia. Parkinson, F.E., Zhang, Y.W., Shepel, P.N., Greenway, S.C., Peeling, J., Geiger, J.D. J. Neurochem. (2000) [Pubmed]
  14. Tamoxifen inhibits nitrobenzylthioinosine-sensitive equilibrative uridine transport in human MCF-7 breast cancer cells. Cai, J., Lee, C.W. Biochem. J. (1996) [Pubmed]
  15. Enzymic cleavage as a probe of the molecular structures of mammalian equilibrative nucleoside transporters. Kwong, F.Y., Wu, J.S., Shi, M.M., Fincham, H.E., Davies, A., Henderson, P.J., Baldwin, S.A., Young, J.D. J. Biol. Chem. (1993) [Pubmed]
  16. Isolation and characterization of a mutant of L1210 murine leukemia deficient in nitrobenzylthioinosine-insensitive nucleoside transport. Belt, J.A., Noel, L.D. J. Biol. Chem. (1988) [Pubmed]
  17. Mammalian nitrobenzylthioinosine-sensitive nucleoside transport proteins. Immunological evidence that transporters differing in size and inhibitor specificity share sequence homology. Kwong, F.Y., Fincham, H.E., Davies, A., Beaumont, N., Henderson, P.J., Young, J.D., Baldwin, S.A. J. Biol. Chem. (1992) [Pubmed]
  18. Heterogeneity of [3H]dipyridamole binding to CNS membranes: correlation with [3H]nitrobenzylthioinosine binding and [3H]uridine influx studies. Jones, K.W., Hammond, J.R. J. Neurochem. (1992) [Pubmed]
  19. Nucleoside transport in rat cerebral-cortical synaptosomes. Evidence for two types of nucleoside transporters. Lee, C.W., Jarvis, S.M. Biochem. J. (1988) [Pubmed]
  20. Fluctuations in nucleoside uptake and binding of the inhibitor of nucleoside transport, nitrobenzylthioinosine, during the replication cycle of HeLa cells. Cass, C.E., Dahlig, E., Lau, E.Y., Lynch, T.P., Paterson, A.R. Cancer Res. (1979) [Pubmed]
  21. Treatment of mouse neoplasms with high doses of tubercidin. Lynch, T.P., Jakobs, E.S., Paran, J.H., Paterson, A.R. Cancer Res. (1981) [Pubmed]
  22. Photoaffinity labeling of the human erythrocyte nucleoside transporter by N6-(p-Azidobenzyl)adenosine and nitrobenzylthioinosine. Evidence that the transporter is a band 4.5 polypeptide. Young, J.D., Jarvis, S.M., Robins, M.J., Paterson, A.R. J. Biol. Chem. (1983) [Pubmed]
  23. Chimeric constructs between human and rat equilibrative nucleoside transporters (hENT1 and rENT1) reveal hENT1 structural domains interacting with coronary vasoactive drugs. Sundaram, M., Yao, S.Y., Ng, A.M., Griffiths, M., Cass, C.E., Baldwin, S.A., Young, J.D. J. Biol. Chem. (1998) [Pubmed]
  24. Defective facilitated diffusion of nucleosides, a primary mechanism of resistance to 5-fluoro-2'-deoxyuridine in the HCT-8 human carcinoma line. Sobrero, A.F., Moir, R.D., Bertino, J.R., Handschumacher, R.E. Cancer Res. (1985) [Pubmed]
  25. Topology of a human equilibrative, nitrobenzylthioinosine (NBMPR)-sensitive nucleoside transporter (hENT1) implicated in the cellular uptake of adenosine and anti-cancer drugs. Sundaram, M., Yao, S.Y., Ingram, J.C., Berry, Z.A., Abidi, F., Cass, C.E., Baldwin, S.A., Young, J.D. J. Biol. Chem. (2001) [Pubmed]
  26. Inhibition of thymidine uptake in asynchronous HeLa cells by nitrobenzylthioinosine. Cass, C.E., Paterson, A.R. Exp. Cell Res. (1977) [Pubmed]
  27. Functional and molecular characterization of nucleobase transport by recombinant human and rat equilibrative nucleoside transporters 1 and 2. Chimeric constructs reveal a role for the ENT2 helix 5-6 region in nucleobase translocation. Yao, S.Y., Ng, A.M., Vickers, M.F., Sundaram, M., Cass, C.E., Baldwin, S.A., Young, J.D. J. Biol. Chem. (2002) [Pubmed]
  28. Molecular cloning and functional characterization of nitrobenzylthioinosine (NBMPR)-sensitive (es) and NBMPR-insensitive (ei) equilibrative nucleoside transporter proteins (rENT1 and rENT2) from rat tissues. Yao, S.Y., Ng, A.M., Muzyka, W.R., Griffiths, M., Cass, C.E., Baldwin, S.A., Young, J.D. J. Biol. Chem. (1997) [Pubmed]
  29. Concentrative uptake of cyclic ADP-ribose generated by BST-1+ stroma stimulates proliferation of human hematopoietic progenitors. Podestà, M., Benvenuto, F., Pitto, A., Figari, O., Bacigalupo, A., Bruzzone, S., Guida, L., Franco, L., Paleari, L., Bodrato, N., Usai, C., De Flora, A., Zocchi, E. J. Biol. Chem. (2005) [Pubmed]
  30. Molecular cloning and functional characterization of inhibitor-sensitive (mENT1) and inhibitor-resistant (mENT2) equilibrative nucleoside transporters from mouse brain. Kiss, A., Farah, K., Kim, J., Garriock, R.J., Drysdale, T.A., Hammond, J.R. Biochem. J. (2000) [Pubmed]
  31. Interaction of a series of draflazine analogues with equilibrative nucleoside transporters: species differences and transporter subtype selectivity. Hammond, J.R. Naunyn Schmiedebergs Arch. Pharmacol. (2000) [Pubmed]
  32. 5'-S-(2-aminoethyl)-N6-(4-nitrobenzyl)-5'-thioadenosine (SAENTA), a novel ligand with high affinity for polypeptides associated with nucleoside transport. Partial purification of the nitrobenzylthioinosine-binding protein of pig erythrocytes by affinity chromatography. Agbanyo, F.R., Vijayalakshmi, D., Craik, J.D., Gati, W.P., McAdam, D.P., Asakura, J., Robins, M.J., Paterson, A.R., Cass, C.E. Biochem. J. (1990) [Pubmed]
  33. Modification by nitrobenzylthioinosine-5'-monophosphate of pseudoisocytidine pharmacokinetics in mice and rats through inhibition of membrane transport. Kolassa, N., Paterson, A.R., Chou, T.C. Cancer treatment reports. (1983) [Pubmed]
  34. Nucleoside transport in erythrocytes from bottle-nosed dolphin (Tursiops truncatus). Craik, J.D., Young, J.D., Cheeseman, C.I. Comp. Biochem. Physiol. A Physiol. (1997) [Pubmed]
  35. Separation of nitrobenzylthioinosine from high affinity binding sites on human erythrocytes by gel chromatography. Paterson, A.R., Almeida, A.F., Dahlig-Harley, E., Miller, J.P., Cass, C.E. Can. J. Biochem. Cell Biol. (1984) [Pubmed]
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