Bosshart PD., Kalbermatter D., Bonetti S. et al., Mechanistic basis of L-lactate transport in the SLC16 solute carrier family. Nat Commun 10, 2649 (2019).
The crystal structures of an L-lactate transporter with two different bound ligands have been solved in the outward-open conformation by the group of D. Fotiadis. The results of this pharmacologically relevant study provide new, important insights into the molecular working mechanism of L-lactate transporters and transport of this metabolite in cancer cells.
Bartholomäus R., Nicolussi S., Baumann A., Rau M., Simão AC., Gertsch J., Altmann K.-H., Total Synthesis of the Endocannabinoid Uptake Inhibitor Guineensine and SAR Studies. ChemMedChem 2019 Sep 4;14(17):1590-1596.
The groups of K.-H. Altmann and J. Gertsch successfully established a highly efficient total synthesis and first structure-activity relationship study of guineensine. This unsaturated fatty-acid-derived natural product is a potent inhibitor of endocannabinoid cellular uptake. This represents a starting point for the design and synthesis of more advanced guineensine analogues and, in the long term, for the development of more drug-like structures.