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Chemical Compound Review

Premarin     (8S,9S,13S,14S)-13-methyl-17- oxo-3...

Synonyms: Conestoral, SureCN22846, AC1MHDJ1, CHEMBL494753, CCRIS 9319, ...
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High impact information on Estrone hydrogen sulfate

  • Clones of each variant were created by site-directed mutagenesis, expressed in HEK-293 cells, and tested for function using the model substrates, estrone sulfate (ES) and cimetidine (CIM) [1].
  • GA stimulation of ES transport by oocytes coexpressing rabbit Na(+)-dicarboxylate cotransporter 1 and rat Oat3 was significantly inhibited when the preloading medium contained Li(+) or methylsuccinate (MS) or when Na(+) was absent [2].
  • Importantly, functional expression of Oat1, Oat3, and Oct2 transport as measured by kinetics (J(max) and K(t)) of PAH, ES, and TEA uptake was similar between adult male and female rabbits, and correlated with rbOat1, rbOat3, and rbOct2 protein expression [3].
  • These results suggest that probenecid, KW-3902, and betamipron could inhibit hOAT4-mediated ES uptake in vitro, whereas probenecid alone could inhibit the hOAT2-mediated PGF(2alpha) uptake [4].
  • MTX and E3S showed a preferential basolateral-toapical (B-to-A) transport across Caco-2 cell monolayers [5].

Biological context of Estrone hydrogen sulfate


Gene context of Estrone hydrogen sulfate

  • Both BCRP inhibitors Ko143 and GF120918 increased the apical-to-basolateral (A-to-B) transport but decreased the B-to-A transport of MTX and E3S [5].


  1. The human organic anion transporter 3 (OAT3; SLC22A8): genetic variation and functional genomics. Erdman, A.R., Mangravite, L.M., Urban, T.J., Lagpacan, L.L., Castro, R.A., de la Cruz, M., Chan, W., Huang, C.C., Johns, S.J., Kawamoto, M., Stryke, D., Taylor, T.R., Carlson, E.J., Ferrin, T.E., Brett, C.M., Burchard, E.G., Giacomini, K.M. Am. J. Physiol. Renal Physiol. (2006) [Pubmed]
  2. Organic anion transporter 3 (Slc22a8) is a dicarboxylate exchanger indirectly coupled to the Na+ gradient. Sweet, D.H., Chan, L.M., Walden, R., Yang, X.P., Miller, D.S., Pritchard, J.B. Am. J. Physiol. Renal Physiol. (2003) [Pubmed]
  3. Sex differences in the mRNA, protein, and functional expression of organic anion transporter (Oat) 1, Oat3, and organic cation transporter (Oct) 2 in rabbit renal proximal tubules. Groves, C.E., Suhre, W.B., Cherrington, N.J., Wright, S.H. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  4. Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. Enomoto, A., Takeda, M., Shimoda, M., Narikawa, S., Kobayashi, Y., Kobayashi, Y., Yamamoto, T., Sekine, T., Cha, S.H., Niwa, T., Endou, H. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  5. Expression, localization, and functional characteristics of breast cancer resistance protein in Caco-2 cells. Xia, C.Q., Liu, N., Yang, D., Miwa, G., Gan, L.S. Drug Metab. Dispos. (2005) [Pubmed]
  6. Boronic acids as inhibitors of steroid sulfatase. Ahmed, V., Liu, Y., Silvestro, C., Taylor, S.D. Bioorg. Med. Chem. (2006) [Pubmed]
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