A mechanism of uncompetitive inhibition of the serotonin transporter
S. Bhat, A. Elkasaby, A. Kasture, D. Boytsov, J. B. Reichelt, T. Hummel, S. Sucic, C. Pifl, M. Freissmuth, W. Sandtner
This paper identifies ECSI#6 as an uncompetitive inhibitor of the serotonin transporter, showing it preferentially binds to the K+-bound inward-facing conformation and acts as a pharmacochaperone for misfolded variants.
bioRxiv · Aug 11, 2022Pharmacology & Toxicology