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BIBW22 BS is a phenylpteridine analog that functions as a potent multidrug resistance (MDR)-reversing agent. It directly interacts with P-glycoprotein (P-gp), a protein found in tumor cells that contributes to the MDR phenotype by facilitating drug transport across cell membranes. Unlike some other P-gp inhibitors, BIBW22 BS is not effluxed from drug-resistant cells and instead accumulates within them, thereby inhibiting the photolabeling of P-gp.
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