Structure-based Discovery of Conformationally Selective Inhibitors of the Serotonin Transporter
I. Singh, A. Seth, C. B. Billesbolle, J. Braz, R. M. Rodriguiz, K. Roy, B. Bekele, V. Craik, X.-P. Huang, D. Boytsov, P. Lak, H. R. O'Donnell, W. R. Sandtner, B. L. Roth, A. Basbaum, , G. Rudnick
The paper identifies two novel inhibitors of the serotonin transporter that selectively target the inward-open conformation, showing improved potency and reduced off-target effects compared to existing drugs.
bioRxiv · Jun 13, 2022Biochemistry