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ω-Conotoxin GVIA mimetics that bind and inhibit neuronal Cav2.2 ion channels

Tranberg, Charlotte Elisabet, Yang, Aijun, Vetter, Irina, McArthur, Jeffrey R., Baell, Jonathan B., Lewis, Richard J., Tuck, Kellie L. and Duggan, Peter J. 2012, ω-Conotoxin GVIA mimetics that bind and inhibit neuronal Cav2.2 ion channels, Marine drugs, vol. 10, no. 10, pp. 2349-2368, doi: 10.3390/md10102349.

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Title ω-Conotoxin GVIA mimetics that bind and inhibit neuronal Cav2.2 ion channels
Formatted title ω-Conotoxin GVIA mimetics that bind and inhibit neuronal Cav2.2 ion channels
Author(s) Tranberg, Charlotte Elisabet
Yang, Aijun
Vetter, Irina
McArthur, Jeffrey R.
Baell, Jonathan B.
Lewis, Richard J.
Tuck, Kellie L.
Duggan, Peter J.
Journal name Marine drugs
Volume number 10
Issue number 10
Start page 2349
End page 2368
Total pages 20
Publisher MDPI AG
Place of publication Basel, Switzerland
Publication date 2012
ISSN 1660-3397
Keyword(s) Cav2.2
conotoxin
peptidomimetics
radioligand binding
Ca2+ fluorescence assay
patch clamp electrophysiology
Summary The neuronal voltage-gated N-type calcium channel (Cav2.2) is a validated target for the treatment of neuropathic pain. A small library of anthranilamide-derived ω-Conotoxin GVIA mimetics bearing the diphenylmethylpiperazine moiety were prepared and tested using three experimental measures of calcium channel blockade. These consisted of a 125I-ω-conotoxin GVIA displacement assay, a fluorescence-based calcium response assay with SH-SY5Y neuroblastoma cells, and a whole-cell patch clamp electrophysiology assay with HEK293 cells stably expressing human Cav2.2 channels. A subset of compounds were active in all three assays. This is the first time that compounds designed to be mimics of ω-conotoxin GVIA and found to be active in the 125I-ω-conotoxin GVIA displacement assay have also been shown to block functional ion channels in a dose-dependent manner.
Language eng
DOI 10.3390/md10102349
Field of Research 059999 Environmental Sciences not elsewhere classified
Socio Economic Objective 970105 Expanding Knowledge in the Environmental Sciences
HERDC Research category C1.1 Refereed article in a scholarly journal
Copyright notice ©2012, The Authors
Free to Read? Yes
Use Rights Creative Commons Attribution licence
Persistent URL http://hdl.handle.net/10536/DRO/DU:30051588

Document type: Journal Article
Collections: School of Life and Environmental Sciences
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Every reasonable effort has been made to ensure that permission has been obtained for items included in DRO. If you believe that your rights have been infringed by this repository, please contact drosupport@deakin.edu.au.