西亚试剂：Structural Features for Functional Selectivity at Serotonin

Structural Features for Functional Selectivity at Serotonin Receptors

Daniel Wacker1, Chong Wang1, Vsevolod Katritch1, Gye Won Han1, Xi-Ping Huang2, Eyal Vardy2, John D. McCorvy2, Yi Jiang1,3, Meihua Chu1, Fai Yiu Siu1, Wei Liu1, H. Eric Xu3,4, Vadim Cherezov1, Bryan L. Roth2,*, Raymond C. Stevens1,*

Drugs active at G protein–coupled receptors (GPCRs) can differentially modulate either canonical or noncanonical signaling pathways via a phenomenon known as functional selectivity or biased signaling. We report biochemical studies that show that the hallucinogen lysergic acid diethylamide (LSD), its precursor ergotamine (ERG), and related ergolines display strong functional selectivity for β-arrestin signaling at the 5-hydroxytryptamine (5-HT) receptor 5-HT2B, while being relatively unbiased at the 5-HT1B receptor. To investigate the structural basis for biased signaling, we determined the crystal structure of the human 5-HT2B receptor bound to ERG, and compared it with the 5-HT1B/ERG structure. Given the relatively poor understanding of GPCR structure-function to date, insight into different GPCR signaling pathways is important to better understand both adverse and favorable therapeutic activities.

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