How CryoEM has expanded our understanding of membrane transporters .

Abstract Over the past two decades, technological advances in membrane protein structural biology have provided insight into the molecular mechanisms that transporters use to move diverse substrates across the membrane. However, the plasticity of these proteins' ligand binding pockets, which allows them to bind a range of substrates, also poses a challenge for drug development. Here, we highlight the structure, function, and transport mechanism of ABC/SLC transporters that are related to several diseases and multidrug resistance: ABCB1, ABCC1, ABCG2, SLC19A1, and SLC29A1. Significance Statement The knowledge of transporter structure will provide insights into future drug development.