Method of screening candidate compounds for susceptibility to biliary excretion

作者: Kim L. Brouwer , Peijin Zhang , Xianbin Tian

DOI:

关键词:

摘要: A method of screening a candidate compound for susceptibility to biliary excretion by hepatocyte transport protein. The includes the steps providing culture hepatocytes comprising protein, having at least one bile canaliculus; exposing culture; and determining an amount in canaliculus, canaliculus indicating In some embodiments comprises inhibiting expression measuring comparing amounts canalicules with without inhibition difference indicates embodiment, protein is inhibited through introduction RNA sequence corresponding coding strand gene encoding into hepatocyte. Optionally, long-term sandwich configuration. particularly applicable multiple compounds single effort.

参考文章(41)
Xingrong Liu, Kim L. R. Brouwer, Liang‐Sheng L. Gan, Kenneth R. Brouwer, Bruno Stieger, Peter J. Meier, Kenneth L. Audus, Edward L. LeCluyse, Partial maintenance of taurocholate uptake by adult rat hepatocytes cultured in a collagen sandwich configuration. Pharmaceutical Research. ,vol. 15, pp. 1533- 1539 ,(1998) , 10.1023/A:1011994831139
Ronald T. Borchardt, Glynn Wilson, Philip L. Smith, Models for Assessing Drug Absorption and Metabolism ,(1996)
Aaron Herman Heifetz, John Melvin Frazier, Linda Mary Arterburn, Joanne Zurlo, James Donald Yager, Hepatocyte test kit ,(1995)
Kim L. R. Brouwer, Peijin Zhang, Xianbin Tian, Method for inhibiting expression of a protein in a hepatocyte ,(2009)
C J Chen, D Clark, K Ueda, I Pastan, M M Gottesman, I B Roninson, Genomic organization of the human multidrug resistance (MDR1) gene and origin of P-glycoproteins. Journal of Biological Chemistry. ,vol. 265, pp. 506- 514 ,(1990) , 10.1016/S0021-9258(19)40260-3
Bruno HAGENBUCH, Bruce F. SCHARSCHMIDT, Peter J. MEIER, Effect of antisense oligonucleotides on the expression of hepatocellular bile acid and organic anion uptake systems in Xenopus laevis oocytes Biochemical Journal. ,vol. 316, pp. 901- 904 ,(1996) , 10.1042/BJ3160901