NDLI: Structural Basis for Molecular Recognition at Serotonin Receptors

Content Provider	PubMed Central
Author	Wang, Chong Jiang, Yi Ma, Jinming Huixian, Wu Wacker, Daniel Katritch, Vsevolod Han, Gye Won Liu, Wei Huang, Xi-ping Vardy, Eyal Mccorvy, John D. Gao, Xiang Zhou, Edward X. Melcher, Karsten Zhang, Chenghai Bai, Fang Yang, Huaiyu Yang, Linlin Jiang, Hualiang Roth, Bryan L. Vadim, Cherezov Stevens, Raymond C. Xu, H. Eric
Abstract	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-HT1B G protein-coupled receptor bound to the agonist anti-migraine 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 to the accompanying structure of the 5-HT2B receptor, the 5-HT1B 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.
Related Links	http://dx.doi.org/10.1126/science.1232807
Ending Page	614
Page Count	5
Starting Page	610
File Format	PDF
ISSN	10959203
e-ISSN	10959203
Journal	Science (New York, N.Y.)
Issue Number	6132
Volume Number	340
Language	English
Publisher Date	2013-05-03
Access Restriction	Open
Subject Keyword	Medical Sciences Research in Higher Education
Content Type	Text
Resource Type	Article
Subject	History and Philosophy of Science

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

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