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. Attached Files Name Description MIMEType Size Downloads tranberg-wconotoxingvia-2012.pdf Published version application/pdf 899.70KB 107 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 Persistent URL http://hdl.handle.net/10536/DRO/DU:30051588 Document type: Journal Article Collections: Faculty of Science, Engineering and Built Environment School of Life and Environmental Sciences Open Access Collection Related Links Link Description Connect to published version Go to link with your DU access privileges     Unless expressly stated otherwise, the copyright for items in DRO is owned by the author, with all rights reserved. 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. Versions Version Filter Type Thu, 21 Mar 2013, 09:35:27 EST Thu, 21 Mar 2013, 10:17:36 EST Mon, 17 Jun 2013, 18:16:14 EST Fri, 05 May 2017, 16:54:29 EST Mon, 08 May 2017, 09:35:06 EST Fri, 07 Sep 2018, 12:33:07 EST Filtered Full Citation counts:   Cited 17 times in TR Web of Science Cited 17 times in Scopus Search Google Scholar Access Statistics: 280 Abstract Views, 107 File Downloads  -  Detailed Statistics Created: Thu, 21 Mar 2013, 09:35:27 EST

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