Functional evidence that transmembrane 12 and the loop between transmembrane 11 and 12 form part of the drug-binding domain in P-glycoprotein encoded by MDR1.

Abstract excerpt

Human MDR1 encodes an ATP-binding cassette transporter, P-glycoprotein, that mediates multiple drug resistance (MDR) to antitumor agents. It has been previously shown that photoaffinity drug-labeling sites reside within, or near, the last transmembrane loop of each cassette within P-glycoprotein (transmembrane domains (TM) 5-6 and 11-12). A genetic approach was used to determine if the drug-labeling site in the...

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