Article
Methanethiosulfonate derivatives of rhodamine and verapamil activate human P-glycoprotein at different sites.
The Journal of biological chemistry - 12 Dec 2003
Loo Tip W, Bartlett M Claire, Clarke David M
Abstract excerpt
The human multidrug resistance P-glycoprotein (P-gp, ABCB1) actively extrudes a broad range of potentially cytotoxic compounds out of the cell. Key steps in understanding the transport process are binding of drug substrates in the transmembrane domains, initiation of ATPase activity, and subsequent drug efflux. We used cysteine-scanning mutagenesis of the transmembrane segment residues and reaction with the...
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