Structure-based discovery of conformationally selective inhibitors of the serotonin transporter.
Cell May 11, 2023 Isha Singh, Anubha Seth, Christian B. Billesbølle et al. 97 citations
The serotonin transporter (SERT) removes synaptic serotonin and is the target of anti-depressant drugs. SERT adopts three conformations: outward-open, occluded, and inward-open. All known inhibitors target the outward-open state except ibogaine, which has unusual anti-depressant and substance-withdrawal effects, and stabilizes the inward-open conformation. Unfortunately, ibogaine's promiscuity...