Asset Details

MbrlCatalogueTitleDetail

Do you wish to reserve the book?

Structural Basis for Molecular Recognition at Serotonin Receptors

by Zhang, Chenghai , Cherezov, Vadim , Wacker, Daniel , Liu, Wei , McCorvy, John D. , Gao, Xiang , Zhou, X. Edward , Han, Gye Won , Melcher, Karsten , Xu, H. Eric , Jiang, Yi , Bai, Fang , Vardy, Eyal , Huang, Xi-Ping , Wu, Huixian , Yang, Huaiyu , Stevens, Raymond C. , Roth, Bryan L. , Wang, Chong , Ma, Jinming , Katritch, Vsevolod , Yang, Linlin , Jiang, Hualiang

in Agonists / Amino Acid Sequence / Binding Sites / crystal structure / Crystallography, X-Ray / Dihydroergotamine - chemistry / Dihydroergotamine - metabolism / drugs / Ergotamine - chemistry / Ergotamine - metabolism / Grants / headache / Humans / Hydrogen Bonding / Hydrogen bonds / Hydrophobic and Hydrophilic Interactions / Indoles / Ligands / LSD / Lysergic Acid Diethylamide - chemistry / Lysergic Acid Diethylamide - metabolism / migraine / Models, Molecular / Molecular biology / Molecular Docking Simulation / Molecular Sequence Data / Mutagenesis / Narcotics / Neurons / Norfenfluramine - chemistry / Norfenfluramine - metabolism / Obesity / Pindolol - analogs & derivatives / Pindolol - chemistry / Pindolol - metabolism / Propranolol - chemistry / Propranolol - metabolism / Protein Conformation / Protein Folding / Protein Structure, Secondary / Receptor, Serotonin, 5-HT1B - chemistry / Receptor, Serotonin, 5-HT1B - genetics / Receptor, Serotonin, 5-HT1B - metabolism / Receptors / Sand sheets / Serotonin / Serotonin 5-HT1 Receptor Agonists - chemistry / Serotonin 5-HT1 Receptor Agonists - metabolism / Serotonin receptors / Tryptamines - chemistry / Tryptamines - metabolism

2013

Yes Please

Hey, we have placed the reservation for you!

By the way, why not check out events that you can attend while you pick your title.

Oops! Something went wrong.

Looks like we were not able to place the reservation. Kindly try again later.

Are you sure you want to remove the book from the shelf?

Structural Basis for Molecular Recognition at Serotonin Receptors

2013

Confirm

Do you wish to request the book?

Structural Basis for Molecular Recognition at Serotonin Receptors

2013

Please be aware that the book you have requested cannot be checked out. If you would like to checkout this book, you can reserve another copy

How would you like to get it?

Submit

We have requested the book for you!

Your request is successful and it will be processed during the Library working hours. Please check the status of your request in My Requests.

Oops! Something went wrong.

Looks like we were not able to place your request. Kindly try again later.

Journal Article

Structural Basis for Molecular Recognition at Serotonin Receptors

Zhang, Chenghai,

Cherezov, Vadim,

Wacker, Daniel,

Liu, Wei,

McCorvy, John D.,

Gao, Xiang,

Zhou, X. Edward,

Han, Gye Won,

Melcher, Karsten,

Xu, H. Eric,

Jiang, Yi,

Bai, Fang,

Vardy, Eyal,

Huang, Xi-Ping,

Wu, Huixian,

Yang, Huaiyu,

Stevens, Raymond C.,

Roth, Bryan L.,

Wang, Chong,

Ma, Jinming,

Katritch, Vsevolod,

Yang, Linlin,

Jiang, Hualiang

2013

Overview

Serotonin or 5-hydroxytryptamine (5-HT) regulates a wide spectrum of human physiology through the 5-HT receptor family. We report the crystal structures of the human 5-HT 1B G protein–coupled receptor bound to the agonist antimigraine medications ergotamine and dihydroergotamine. The structures reveal similar binding modes for these ligands, which occupy the orthosteric pocket and an extended binding pocket close to the extracellular loops. The orthosteric pocket is formed by residues conserved in the 5-HT receptor family, clarifying the family-wide agonist activity of 5-HT. Compared with the structure of the 5-HT 2B receptor, the 5-HT 1B receptor displays a 3 angstrom outward shift at the extracellular end of helix V, resulting in a more open extended pocket that explains subtype selectivity. Together with docking and mutagenesis studies, these structures provide a comprehensive structural basis for understanding receptor-ligand interactions and designing subtype-selective serotonergic drugs.

Share this book

Add to My Shelf

Publisher

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

Subject

Agonists

/ Amino Acid Sequence

/ Binding Sites

/ crystal structure

/ Crystallography, X-Ray

/ Dihydroergotamine - chemistry

/ Dihydroergotamine - metabolism