MDR1 human

The MDR1 protein is involved in cancer drug resistance and in the transport of hydrophobic drugs and xenobiotics in the bowel, kidney, liver, and the blood-brain barrier. Drugs interacting with this protein may be useful for the reversal of cancer drug resistance or increasing the absorption or brain entry of various pharmacological agents.

Detection of ATPase activity of the MDR1 protein is a measure of transporter activity. The assay is performed using purified membrane vesicles from Sf9 (Spodoptera frugiperda) cells, expressing high levels of MDR1 protein. The ABC transporters pump substrates out of the cell by using hydrolysis of ATP as an energy source. ATP hydrolysis yields inorganic phosphate (P_i), which can be detected by a simple colorimetric reaction. The amount of P_i liberated is proportional to the activity of the transporter.

Supplied as isolated Sf9 cell membranes containing human MDR1 (Pgp) suspended in TMEP solution.

Membrane preparations containing ABC transporters show a baseline ATPase activity that varies for different transporters. Transported substrates increase this baseline ATPase activity, while inhibitors or slowly transported compounds inhibit the baseline ATPase activity and/or the ATPase activity measured in the presence of a stimulating agent. Both activation and inhibition studies can be performed.

Distributed for SOLVO Biotechnology, Inc.