Efflux transporters such as P-gp and BCRP, which are highly expressed at the blood-brain barrier (BBB), are the reason why many drug molecules (e.g., chemotherapeutic drugs) cannot cross the BBB to enter the brain. Therefore, compound molecules that are substrates of these efflux transporters need to be eliminated in early-stage drug screening.
Currently, in preclinical research, the main efflux transporters evaluated are P-gp and BCRP, and their corresponding cell models are primarily MDCK-MDR1 and MDCK-BCRP.
