Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone

K. Ueda, N. Okamura, M. Hirai, Y. Tanigawara, T. Saeki, N. Kioka, T. Komano, R. Hori

研究成果: Article

608 引用 (Scopus)

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We expressed human MDR1 cDNA isolated from the human adrenal gland in porcine LLC-PK1 cells. A highly polarized epithelium formed by LLC-GA5- COL300 cells that expressed human P-glycoprotein specifically on the apical surface showed a multidrug-resistant phenotype and had 8.3-, 3.4-, and 6.5- fold higher net basal to apical transport of 3H-labeled cortisol, aldosterone, and dexamethasone, respectively, compared with host cells. But progesterone was not transported, although it inhibited azidopine photoaffinity labeling of human P-glycoprotein and increased the sensitivity of multidrug-resistant cells to vinblastine. An excess of progesterone inhibited the transepithelial transport of cortisol by P-glycoprotein. These results suggest that cortisol and aldosterone are physiological substrates for P-glycoprotein in the human adrenal cortex and that substances that efficiently bind to P-glycoprotein are not necessarily transported by P- glycoprotein.

元の言語English
ページ(範囲)24248-24252
ページ数5
ジャーナルJournal of Biological Chemistry
267
発行部数34
出版物ステータスPublished - 1992 1 1
外部発表Yes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology

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    Ueda, K., Okamura, N., Hirai, M., Tanigawara, Y., Saeki, T., Kioka, N., Komano, T., & Hori, R. (1992). Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone. Journal of Biological Chemistry, 267(34), 24248-24252.