The inhibitory activity of glycine transporter 2 targeting bioactive lipid analgesics are influenced by formation of a deep lipid cavity
K. A. Wilson, S. N. Mostyn, Z. J. Frangos, S. Shimmon, T. Rawling, R. J. Vandenberg, M. L. O'Mara
This study investigates how N-acyl amino acids inhibit GlyT2 by binding to an allosteric site, showing that stereochemistry, tail length, and double bond position enhance inhibition through deep penetration into the binding pocket.
bioRxiv · Sep 10, 2020 · PreprintBiochemistry