Cryogenic-electron microscopy (Cryo-EM) structures of a human ABCG2 mutant transporter protein
The transporter protein ABCG2 belongs to the ATP-binding-cassette (ABC) family. The protein is expressed in the plasma membranes of cells within a variety of tissues and tissue barriers, including the blood-brain, blood-testes and maternal-fetal barrier. The protein can be powered by ATP to translocate endogenous substrates, affect the pharmacokinetics of many drugs and protect against a variety of xenobiotics including anticancer drugs, notably in breast cancer. ABCG2 is often referred to as the breast cancer resistance protein, where previous studies have revealed the ABCG2 architecture and structural basis of ABCG2 inhibition with small molecules and antibodies. The mechanism of substrate recognition by ABCG2 alongside its ATP-driven transport capability remains yet to be determined.