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Structural features for functional selectivity at serotonin receptors

Academic Article
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Overview

related to degree

  • Wang, Chong, Ph.D. in Chemistry, Scripps Research , transferred from UCSD 2011 - 2014
  • Wacker, Daniel, Ph.D. in Biology, Scripps Research 2009 - 2013

authors

  • Wacker, Daniel
  • Wang, Chong
  • Katritch, Vsevolod
  • Han, G. W.
  • Huang, X. P.
  • Vardy, E.
  • McCorvy, J. D.
  • Jiang, Y.
  • Chu, M.
  • Siu, F. Y.
  • Liu, W.
  • Xu, H. E.
  • Cherezov, Vadim
  • Roth, B. L.
  • Stevens, Raymond

publication date

  • May 2013

journal

  • Science  Journal

abstract

  • 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 showing that the hallucinogen lysergic acid diethylamide, its precursor ergotamine (ERG), and related ergolines display strong functional selectivity for β-arrestin signaling at the 5-HT2B 5-hydroxytryptamine (5-HT) receptor, whereas they are 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 and function to date, insight into different GPCR signaling pathways is important to better understand both adverse and favorable therapeutic activities.

subject areas

  • Amino Acid Motifs
  • Amino Acid Sequence
  • Arrestin
  • Arrestins
  • Binding Sites
  • Crystallography, X-Ray
  • Ergolines
  • Ergotamine
  • HEK293 Cells
  • Humans
  • Ligands
  • Lysergic Acid Diethylamide
  • Models, Molecular
  • Molecular Sequence Data
  • Protein Conformation
  • Protein Structure, Secondary
  • Receptor, Serotonin, 5-HT1B
  • Receptor, Serotonin, 5-HT2B
  • Receptors, Serotonin
  • Signal Transduction
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Identity

PubMed Central ID

  • PMC3644390

International Standard Serial Number (ISSN)

  • 1095-9203 (Electronic) 0036-8075 (Linking)

Digital Object Identifier (DOI)

  • 10.1126/science.1232808

PubMed ID

  • 23519215
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Additional Document Info

start page

  • 615

end page

  • 619

volume

  • 340

issue

  • 6132

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