Low molecular weight non-peptide mimics of omega-conotoxin GVIA

Duggan, P. J., Lewis, R. J., Lok, Y. P., Lumsden, N. G., Tuck, K. L. and Yang, A. J. (2009) Low molecular weight non-peptide mimics of omega-conotoxin GVIA. Bioorganic and Medicinal Chemistry Letters, 19 10: 2763-2765. doi:10.1016/j.bmcl.2009.03.130


Author Duggan, P. J.
Lewis, R. J.
Lok, Y. P.
Lumsden, N. G.
Tuck, K. L.
Yang, A. J.
Title Low molecular weight non-peptide mimics of omega-conotoxin GVIA
Formatted title
Low molecular weight non-peptide mimics of ω-conotoxin GVIA
Journal name Bioorganic and Medicinal Chemistry Letters   Check publisher's open access policy
ISSN 1464-3405
0960-894X
Publication date 2009-05
Year available 2009
Sub-type Article (original research)
DOI 10.1016/j.bmcl.2009.03.130
Volume 19
Issue 10
Start page 2763
End page 2765
Total pages 3
Place of publication Oxford, UK
Publisher Elsevier
Collection year 2010
Language eng
Subject C1
8608 Human Pharmaceutical Products
860899 Human Pharmaceutical Products not elsewhere classified
111501 Basic Pharmacology
Abstract We report the synthesis and biological activity of a low molecular weight non-peptidic mimic of the analgesic peptide ω-conotoxin GVIA. The molecular weight of this compound presents a reduction by 193 g/mol compared to a previously reported lead. This compound exhibits an EC50 of 5.8 μM and is accessible in only six synthetic steps compared to the original lead (13 steps). We also report several improvements to the original synthetic route.
Keyword Conotoxin
GVIA
Peptidomimetic
Calcium channel blocker
Pain
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: 2010 Higher Education Research Data Collection
Institute for Molecular Bioscience - Publications
 
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Citation counts: TR Web of Science Citation Count  Cited 16 times in Thomson Reuters Web of Science Article | Citations
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Created: Thu, 03 Sep 2009, 08:14:46 EST by Mr Andrew Martlew on behalf of Institute for Molecular Bioscience