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- Title
Cyclisation of Disulfide-Rich Conotoxins in Drug Design Applications.
- Authors
Wu, Xiaosa; Huang, Yen‐Hua; Kaas, Quentin; Craik, David J.
- 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.
- Subjects
RING formation (Chemistry); DISULFIDES; CONOTOXINS; CHEMICAL reactions; NEUROTOXIC agents; DRUG design; ORGANIC chemistry
- Publication
European Journal of Organic Chemistry, 2016, Vol 2016, Issue 21, p3462
- ISSN
1434-193X
- Publication type
Article
- DOI
10.1002/ejoc.201600402