Title : Characterization of binding properties to human P-glycoprotein: development of a [3H]verapamil radioligand-binding assay.

Pub. Date : 1999 Jan

PMID : 9862789






4 Functional Relationships(s)
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1 Because of the reversible and competitive interaction of numerous substrates with P-gp, a radioligand-binding assay was developed by taking [3H]verapamil and [3H]vinblastine as radioligands and the human intestinal Caco-2 cells, overexpressed with P-gp by culturing in the presence of vinblastine or transfecting with multidrug resistance gene MDR-1 as receptor preparation. Vinblastine ATP binding cassette subfamily B member 1 Homo sapiens
2 Because of the reversible and competitive interaction of numerous substrates with P-gp, a radioligand-binding assay was developed by taking [3H]verapamil and [3H]vinblastine as radioligands and the human intestinal Caco-2 cells, overexpressed with P-gp by culturing in the presence of vinblastine or transfecting with multidrug resistance gene MDR-1 as receptor preparation. Vinblastine ATP binding cassette subfamily B member 1 Homo sapiens
3 A clear induction of the expression of P-gp was demonstrated in the Caco-2 cells grown in the presence of vinblastine, as well as in the transfected cells, although to a lesser extent. Vinblastine ATP binding cassette subfamily B member 1 Homo sapiens
4 The binding properties of [3H]verapamil and [3H]vinblastine to a P-gp preparation derived from induced Caco-2 cells are described. Vinblastine ATP binding cassette subfamily B member 1 Homo sapiens