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Crystal Structure of an LSD-Bound Human Serotonin Receptor.

Cell. 2017; 
Wacker Daniel,Wang Sheng,McCorvy John D,Betz Robin M,Venkatakrishnan A J,Levit Anat,Lansu Katherine,Schools Zachary L,Che Tao,Nichols David E,Shoichet Brian K,Dror Ron O,Roth Bry
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摘要

The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the crystal structure?of LSD in complex with the human serotonin receptor 5-HT. The complex reveals conformational rearrangements to accommodate LSD, providing a structural explanation for the conformational selectivity of LSD's key diethylamide moiety. LSD dissociates exceptionally slow from both 5-HTR and 5-HTR-a major target for its psychoactivity. Molecular dynamics (MD) simulations suggest that LSD's slow binding kinetics may be due to a "lid" formed by extracellular loop 2 (EL2) at the entrance to the binding pocket. A mutation predicted to increase the mobility of this lid greatly accelerates LSD's binding kinetics a... More

关键词

GPCR,crystallography,hallucinogens,serotonin receptor,structure-func