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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
Author to whom correspondence should be addressed.
Biomedicines 2018, 6(4), 97;
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)
PDF [2130 KB, uploaded 6 October 2018]


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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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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