Background: Rifampin is a representative inducer of P-gp, and the only known mechanism is binding between rifampin and PXR. Results: Rifampin directly activates CK2, which phosphorylates Hsp90. Consequently, PXR increases, and P-gp expression is induced. Conclusion: A mechanism for inducing P-gp expression by rifampin exposure is newly identified. Significance: A strategy for overcoming P-gp-derived drug resistance is suggested.
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