Cyclisation of disulfide-rich conotoxins in drug design applications

Wu, Xiaosa, Huang, Yen-Hua, Kaas, Quentin and Craik, David J. (2016) Cyclisation of disulfide-rich conotoxins in drug design applications. European Journal of Organic Chemistry, 2016 21: 3462-3472. doi:10.1002/ejoc.201600402


Author Wu, Xiaosa
Huang, Yen-Hua
Kaas, Quentin
Craik, David J.
Title Cyclisation of disulfide-rich conotoxins in drug design applications
Journal name European Journal of Organic Chemistry   Check publisher's open access policy
ISSN 1099-0690
1434-193X
Publication date 2016-07-01
Year available 2016
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1002/ejoc.201600402
Open Access Status Not yet assessed
Volume 2016
Issue 21
Start page 3462
End page 3472
Total pages 11
Place of publication Weinheim, Germany
Publisher Wiley - V C H Verlag GmbH & Co. KGaA
Language eng
Formatted abstract
Conotoxins are disulfide-rich peptides found in the venoms of marine snails of the genus Conus. They have attracted great attention from the pharmaceutical industry because of their potential uses as drug leads, but like most peptides, conotoxins are susceptible to proteolysis and typically are not orally bioavailable. Here we discuss approaches that have been used to stabilise conotoxins to improve their potential pharmaceutical use. Specifically, we focus on the use of backbone cyclisation to improve their stability in biological fluids. The Microreview provides an introduction to the various classes of conotoxins, including their frameworks (cysteine patterns) and a background on the receptors that they interact with, as well as an analysis of the binding interactions between conotoxins and their receptors.
Keyword Conotoxins
Cyclization
Disulfides
Drug design
Stability
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: HERDC Pre-Audit
Institute for Molecular Bioscience - Publications
 
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