The paper develops a NanoBRET assay to quantify intracellular GlyT1 target engagement in living cells, distinguishing intracellular from extracellular ligands and resolving structure-activity relationships.

bioRxiv · Oct 6, 2026 · PreprintMolecular Biology

Structural basis for selective inhibition of human GABA transporter GAT3

Jonas Sigurd Mortensen, Francesco Bavo, Malene Hall Jensen, Alexander Peder Smiszek Pedersen, Julian Philipp Storm, Tillmann Pape, Bente Frølund, Petrine Wellendorph, Azadeh Shahsavar

This study presents cryo-EM structures of human GAT3 bound to inhibitor, substrate GABA, or in substrate-free state, revealing molecular mechanisms of inhibition and substrate recognition.

Nature Communications · Jan 29, 2026Peer-reviewedMolecular Biology

Allosteric factors in the calcium/calmodulin-responsive kinase II hub domain determine selectivity of GHB ligands for CaMKIIa

Stine Juul Gauger, Line B. Palmelund, Yongsong Tian, Aleš Marek, Mathias RJ Namini, Nane Griem‐Krey, Madeline Y. Petersen, Stefanie Kickinger, Jonas Sigurd Mortensen, Bente Frølund, Petrine Wellendorph

This study identifies allosteric factors in the CaMKII hub domain that determine GHB ligand selectivity for CaMKIIa over other isozymes.

Journal of Biological Chemistry · Apr 24, 2025Peer-reviewedBiochemistry