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
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
Collection year 2013
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
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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