Conopeptide p-tia defines a new allosteric site on the extracellular surface of the α1b-adrenoceptor

Ragnarsson, Lotten, Wang, Ching-I Anderson, Andersson, Asa, Fajarningsih, Dewi, Monks, Thea, Brust, Andreas, Rosengren, K. Johan and Lewis, Richard J. (2013) Conopeptide p-tia defines a new allosteric site on the extracellular surface of the α1b-adrenoceptor. Journal of Biological Chemistry, 288 3: 1814-1827. doi:10.1074/jbc.M112.430785


Author Ragnarsson, Lotten
Wang, Ching-I Anderson
Andersson, Asa
Fajarningsih, Dewi
Monks, Thea
Brust, Andreas
Rosengren, K. Johan
Lewis, Richard J.
Title Conopeptide p-tia defines a new allosteric site on the extracellular surface of the α1b-adrenoceptor
Formatted title
Conopeptide ρ-TIA defines a new allosteric site on the extracellular surface of the α1B-adrenoceptor
Journal name Journal of Biological Chemistry   Check publisher's open access policy
ISSN 0021-9258
Publication date 2013-01-01
Year available 2012
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1074/jbc.M112.430785
Open Access Status DOI
Volume 288
Issue 3
Start page 1814
End page 1827
Total pages 14
Place of publication Bethesda, MD, United States
Publisher American Society for Biochemistry and Molecular Biology
Language eng
Formatted abstract
Background: Mechanistic insight into allosteric modulation of GPCRs can facilitate antagonist design.

Results: Extracellular surface residues (ECS) of the 1B-adrenoceptor at the base of extracellular loop 3 interact with the allosteric antagonist TIA.

Conclusion: The identified ECS pharmacophore provides the first structural constraints for allosteric antagonist design at p1-adrenoceptors.

Significance: Binding to the ECS of a GPCR can allosterically inhibit agonist signaling.
Keyword Allosteric modulation of GPCRs
Extracellular surface residues (ECS)
Allosteric antagonist
Q-Index Code C1
Q-Index Status Confirmed Code
Grant ID 011246
Institutional Status UQ
Additional Notes First Published: 26 November 2012.

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2013 Collection
School of Biomedical Sciences Publications
Institute for Molecular Bioscience - Publications
 
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