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Gene Review

OCT1  -  organic cation transporter 1

Sus scrofa

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Disease relevance of OCT1

  • However, the finding of an active basolateral organic cation transporter, together with the presence of gamma GT, dipeptidase and beta-lyase, makes this system especially interesting for testing all compounds that use this transporter or these enzymes in order to elicit toxicity [1].

High impact information on OCT1


Anatomical context of OCT1

  • The Xenopus oocyte system provides a functional approach to further characterize the OCT [4].
  • Using [14C]tetraethylammonium bromide ([14C]TEA) as a substrate, we tested several renal cell lines for a nucleoside-sensitive OCT. American opossum kidney proximal tubule cells (OK) express a cimetidine-sensitive and metabolic-dependent ability to efflux TEA [7].

Associations of OCT1 with chemical compounds

  • Previous work (J. A. Nelson, J. F. Kuttesch, Jr., and B. H. Herbert. Biochemical Pharmacology 32: 2323-2327, 1983) indicated a role for the classic organic cation transporter (OCT) in the secretion of the dAdo analog, 2'-deoxytubercidin, by mouse kidney [7].

Other interactions of OCT1

  • Previously we cloned membrane associated (M(r) 62000-67000) polypeptides from pig (pRS1), rabbit (rbRS1) and man (hRS1) which modified transport activities that were expressed in Xenopus laevis oocytes by the Na(+)-D-glucose cotransporter SGLT1 and/or the organic cation transporter OCT2 [8].


  1. Differential toxicity as a result of apical and basolateral treatment of LLC-PK1 monolayers with S-(1,2,3,4,4-pentachlorobutadienyl)glutathione and N-acetyl-S-(1,2,3,4,4-pentachlorobutadienyl)-L-cysteine. Mertens, J.J., Weijnen, J.G., van Doorn, W.J., Spenkelink, B., Temmink, J.H., van Bladeren, P.J. Chem. Biol. Interact. (1988) [Pubmed]
  2. Primary structure and functional expression of the apical organic cation transporter from kidney epithelial LLC-PK1 cells. Gründemann, D., Babin-Ebell, J., Martel, F., Ording, N., Schmidt, A., Schömig, E. J. Biol. Chem. (1997) [Pubmed]
  3. Gentamicin-induced increases in cytosolic calcium in pig kidney cells (LLC-PK1). Holohan, P.D., Sokol, P.P., Ross, C.R., Coulson, R., Trimble, M.E., Laska, D.A., Williams, P.D. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  4. Functional expression of the renal organic cation transporter and P-glycoprotein in Xenopus laevis oocytes. Nelson, J.A., Dutt, A., Allen, L.H., Wright, D.A. Cancer Chemother. Pharmacol. (1995) [Pubmed]
  5. The characterisation and uptake of paraquat in cultured baboon kidney proximal tubule cells (bPTC). Machaalani, R., Lazzaro, V., Duggin, G.G. Human & experimental toxicology. (2001) [Pubmed]
  6. Transcellular transport of creatinine in renal tubular epithelial cell line LLC-PK1. Urakami, Y., Kimura, N., Okuda, M., Masuda, S., Katsura, T., Inui, K. Drug Metab. Pharmacokinet. (2005) [Pubmed]
  7. A nucleoside-sensitive organic cation transporter in opossum kidney cells. Chen, R., Pan, B.F., Sakurai, M., Nelson, J.A. Am. J. Physiol. (1999) [Pubmed]
  8. The transport modifier RS1 is localized at the inner side of the plasma membrane and changes membrane capacitance. Valentin, M., Kühlkamp, T., Wagner, K., Krohne, G., Arndt, P., Baumgarten, K., Weber, W., Segal, A., Veyhl, M., Koepsell, H. Biochim. Biophys. Acta (2000) [Pubmed]
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