Multidrug resistance proteins (MDRPs) are a group of membrane transporters that play a crucial role in the removal of foreign substances, including drugs and toxins, from cells. They are found in various organisms, including bacteria, fungi, plants, and animals, and are particularly important in providing defense mechanisms against the toxic effects of certain chemicals.
MDRPs function by using energy from ATP hydrolysis to actively transport a wide range of substrates out of cells, thus preventing their accumulation to toxic levels. They are often expressed at high levels in tissues such as the liver, kidneys, intestines, and blood-brain barrier, where their detoxification functions are particularly crucial.
These transport proteins are known for their ability to confer resistance to multiple drugs, by actively pumping them out of cells, thereby reducing their therapeutic efficacy. This phenomenon poses a significant challenge in the treatment of various diseases, including cancer, as MDRPs can confer resistance to chemotherapeutic agents, making them less effective in killing cancer cells.
The identification and study of MDRPs have allowed researchers to gain insights into drug resistance mechanisms and develop strategies to overcome them. Modulating MDRP activity or developing inhibitors to prevent drug efflux has been proposed as a potential approach to counteract multidrug resistance in clinical settings. Understanding the structure, function, and regulation of multidrug resistance proteins is of great importance in drug discovery and designing more effective therapeutic interventions.
