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Open AccessArticle

Engineering of an Anti-Inflammatory Peptide Based on the Disulfide-Rich Linaclotide Scaffold

Centre for Biodiscovery and Molecular Development of Therapeutics, AITHM, James Cook University, Cairns 4870, Australia
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Biomedicines 2018, 6(4), 97; https://doi.org/10.3390/biomedicines6040097
Received: 1 July 2018 / Revised: 11 September 2018 / Accepted: 21 September 2018 / Published: 6 October 2018
(This article belongs to the Special Issue Discovery and Development of Constrained Peptide Ligands)
Inflammatory bowel diseases are a set of complex and debilitating diseases, for which there is no satisfactory treatment. Peptides as small as three amino acids have been shown to have anti-inflammatory activity in mouse models of colitis, but they are likely to be unstable, limiting their development as drug leads. Here, we have grafted a tripeptide from the annexin A1 protein into linaclotide, a 14-amino-acid peptide with three disulfide bonds, which is currently in clinical use for patients with chronic constipation or irritable bowel syndrome. This engineered disulfide-rich peptide maintained the overall fold of the original synthetic guanylate cyclase C agonist peptide, and reduced inflammation in a mouse model of acute colitis. This is the first study to show that this disulfide-rich peptide can be used as a scaffold to confer a new bioactivity. View Full-Text
Keywords: anti-inflammatory peptides; disulfide-rich peptides; inflammatory bowel disease anti-inflammatory peptides; disulfide-rich peptides; inflammatory bowel disease
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MDPI and ACS Style

Cobos, C.; Bansal, P.S.; Jones, L.; Wangchuk, P.; Wilson, D.; Loukas, A.; Daly, N.L. Engineering of an Anti-Inflammatory Peptide Based on the Disulfide-Rich Linaclotide Scaffold. Biomedicines 2018, 6, 97.

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