Crystal Structure of an LSD-Bound Human Serotonin Receptor

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• 作者：Daniel Wacker¹ ; ⁹ ; ^{dwacker@email.unc.edu} ; Sheng Wang¹ ; ⁹ ; John D. McCorvy¹ ; ⁹ ; Robin M. Betz² ; ³ ; ⁴ ; ⁵ ; A.J. Venkatakrishnan² ; ³ ; ⁴ ; Anat Levit⁶ ; Katherine Lansu¹ ; Zachary L. Schools¹ ; Tao Che¹ ; David E. Nichols⁷ ; Brian K. Shoichet⁶ ; Ron O. Dror² ; ³ ; ⁴ ; ⁵ ; ^{ron.dror@stanford.edu} ; Bryan L. Roth¹ ; ⁷ ; ⁸ ; ¹⁰ ; ^{bryan_roth@med.unc.edu}
• 关键词：GPCR ; serotonin receptor ; crystallography ; structure-function ; hallucinogens
• 刊名：Cell
• 出版年：2017
• 出版时间：26 January 2017
• 年：2017
• 卷：168
• 期：3
• 页码：377-389.e12
• 全文大小：5292 K
• 卷排序：168

文摘

Crystal structure of the human 5-HT2B receptor bound to LSD is determined LSD shows unexpected binding configuration in the orthosteric site LSD has extremely slow on and off rate at 5-HT2B and 5-HT2A receptors Accelerated LSD kinetics selectively reduce arrestin signaling at 5-HT2B and 5-HT2A