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Structural Features for Functional Selectivity at Serotonin Receptors

by Cherezov, Vadim , Wacker, Daniel , McCorvy, John D. , Liu, Wei , Han, Gye Won , Xu, H. Eric , Jiang, Yi , Vardy, Eyal , Huang, Xi-Ping , Siu, Fai Yiu , Stevens, Raymond C. , Roth, Bryan L. , Wang, Chong , Katritch, Vsevolod , Chu, Meihua

in Agonists / Amino Acid Motifs / Amino Acid Sequence / Arrestin - metabolism / Arrestins - metabolism / beta-Arrestins / Binding Sites / Biochemistry / Crystal structure / Crystallography, X-Ray / drugs / Ergolines - chemistry / Ergolines - metabolism / Ergotamine - chemistry / Ergotamine - metabolism / Grants / headache / HEK293 Cells / Humans / Hydrogen bonds / Ligands / Lysergic Acid Diethylamide / Lysergic Acid Diethylamide - chemistry / Lysergic Acid Diethylamide - metabolism / migraine / Models, Molecular / Molecular Sequence Data / Narcotics / Neurons / Obesity / Pharmacology / Protein Conformation / Protein Structure, Secondary / Receptor, Serotonin, 5-HT1B - chemistry / Receptor, Serotonin, 5-HT1B - metabolism / Receptor, Serotonin, 5-HT2B - chemistry / Receptor, Serotonin, 5-HT2B - metabolism / Receptors / Receptors, Serotonin - chemistry / Receptors, Serotonin - metabolism / Sand sheets / Serotonin / Serotonin receptors / Signal Transduction

2013

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Structural Features for Functional Selectivity at Serotonin Receptors

2013

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2013

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Journal Article

Structural Features for Functional Selectivity at Serotonin Receptors

Cherezov, Vadim,

Wacker, Daniel,

McCorvy, John D.,

Liu, Wei,

Han, Gye Won,

Xu, H. Eric,

Jiang, Yi,

Vardy, Eyal,

Huang, Xi-Ping,

Siu, Fai Yiu,

Stevens, Raymond C.,

Roth, Bryan L.,

Wang, Chong,

Katritch, Vsevolod,

Chu, Meihua

2013

Overview

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-HT 2B 5-hydroxytryptamine (5-HT) receptor, whereas they are relatively unbiased at the 5-HT 1B receptor. To investigate the structural basis for biased signaling, we determined the crystal structure of the human 5-HT 2B receptor bound to ERG and compared it with the 5-HT 1B /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.

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Publisher

American Association for the Advancement of Science,The American Association for the Advancement of Science

Subject

Agonists

/ Amino Acid Motifs

/ Amino Acid Sequence

/ Arrestin - metabolism

/ Arrestins - metabolism

/ beta-Arrestins

/ Binding Sites