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Cyclisation of Disulfide‐Rich Conotoxins in Drug Design Applications
Author(s) -
Wu Xiaosa,
Huang YenHua,
Kaas Quentin,
Craik David J.
Publication year - 2016
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201600402
Subject(s) - conotoxin , chemistry , conus , disulfide bond , computational biology , combinatorial chemistry , biochemistry , venom , biology , anatomy
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.