An Evolutionarily Conserved Residue in ABCG2 Regulates the Transport Cycle and Inhibitor Activity.

ABCG2 is a medically significant ATP‐binding cassette (ABC) transporter restricting the cellular penetration of more than 200 toxins and drugs, as well as promoting physiological detoxification and multidrug resistance in cancers. Although ABCG2 cryo‐EM structural studies reveal an overlap between substrate and inhibitor binding sites in the ABCG2 binding pocket, it is unknown how much these substrate and inhibitor interactions will translate into functional knowledge that is exploitable in live cells.