Publication highlights

Publication highlights

Qin Y, Dongchun N, Kowal J, Manolaridis I, Scott MJ, Stahlberg H and Locher K,Structures of ABCG2 under turnover conditions reveal a key step in the drug transport mechanism, Nature Commun. 2021, 12:4376.

ABCG2 is a multidrug transporter that affects drug pharmacokinetics and contributes to multidrug resistance of cancer cells. In this paper, the authors presented cryo-EM structures of ABCG2 under turnover conditions containing either the endogenous substrate estrone-3-sulfate or the exogenous substrate topotecan. The study revealed key conformational changes that are essential for substrate recognition and translocation, and allow ABCG2 to distinguish substrates from inhibitors.


Bosshart PD, Kalbermatter D, Bonetti S, Fotiadis D, The making of a potent L-lactate transport inhibitor, Commun. Chem. 2021, 4:128

L-lactate is an important metabolite, energy source, and signalling molecule in health and disease. In this study, the authors reported the rational, structure-guided identification of potent, nanomolar affinity inhibitors acting on an L-lactate-specific SLC16 homologue from the bacterium Syntrophobacter fumaroxidans. In addition, they solved the high-resolution crystal structures of SfMCT with bound inhibitors, which provided important insights into the binding mechanism of these molecules on an atomic level.