Tariquidar Research Paper
A8208
Description:
Kd :5.1 nM in CHrB30 cell line
Tariquidar is a P-glycoprotein inhibitor.
Resistance to chemotherapy is a major impediment of successful systemic treatment of breast cancer. One of the best-characterized mechanisms of multidrug resistance is overexpression of P-glycoprotein (P-gp). P-gp is an ATP-dependent drug efflux pump expeling several structurally and functionally unrelated antitumor drugs from cells.
In vitro: The selectivity as an inhibitor and a substrate of tariquidar for the human P-gp, breast cancer resistance protein (BCRP) and multidrug resistance protein 1 (MRP1) were examined. The results showed that at low concentrations, tariquidar acted selectively as an inhibitor of P-gp and also as a substrate of BCRP.
Description:
Kd :5.1 nM in CHrB30 cell line
Tariquidar is a P-glycoprotein inhibitor.
Resistance to chemotherapy is a major impediment of successful systemic treatment of breast cancer. One of the best-characterized mechanisms of multidrug resistance is overexpression of P-glycoprotein (P-gp). P-gp is an ATP-dependent drug efflux pump expeling several structurally and functionally unrelated antitumor drugs from cells.
In vitro: The selectivity as an inhibitor and a substrate of tariquidar for the human P-gp, breast cancer resistance protein (BCRP) and multidrug resistance protein 1 (MRP1) were examined. The results showed that at low concentrations, tariquidar acted selectively as an inhibitor of P-gp and also as a substrate of BCRP.