Cyclotides: A patent review

Smith, Amanda B., Daly, Norelle L. and Craik, David J. (2011) Cyclotides: A patent review. Expert Opinion On Therapeutic Patents, 21 11: 1657-1672. doi:10.1517/13543776.2011.620606

Author Smith, Amanda B.
Daly, Norelle L.
Craik, David J.
Title Cyclotides: A patent review
Journal name Expert Opinion On Therapeutic Patents   Check publisher's open access policy
ISSN 1354-3776
Publication date 2011-11-01
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1517/13543776.2011.620606
Volume 21
Issue 11
Start page 1657
End page 1672
Total pages 16
Place of publication London, United Kingdom
Publisher Informa Healthcare
Language eng
Formatted abstract
Introduction: Cyclotides are bioactive mini-proteins from plants that have the unique topological feature of a head-to-tail cyclic backbone combined with a cystine knot. Because of this structure they are ultra-stable and have attracted interest as peptide-based templates for drug design applications. Cyclotide biosynthesis involves processing from a genetically encoded precursor protein but methods have been developed for their man-made synthesis using solid phase peptide synthesis as well as recombinant methods. Their natural function in plants is as insecticidal agents and thus they have potential applications in agriculture. However, they have a range of pharmaceutically relevant activities, including anti-HIV, antimicrobial and uterotonic activity. Their exceptional stability and facile synthesis lend them to uses as pharmaceutical templates into which bioactive peptide sequences can be grafted.
Areas covered: This article reviews the patent literature associated with cyclotides with a focus on therapeutic applications. These patents are primarily related to the use of cystine knot scaffolds for the production of peptide-based drug leads, molecular probes or diagnostic agents.
Expert opinion: Although no cyclotide-related peptide has yet reached clinical trials, proof-of-concept has been obtained that bioactive peptide sequences can be grafted onto a cyclotide framework, maintaining biological activity while becoming resistant to proteolysis. Thus, cyclotides are promising templates in drug development applications and there is increasing interest in them and related cystine knot scaffolds, as well as in the use of other disulfide-rich scaffolds, in drug design.
Keyword Circular proteins
Cyclic peptides
Cystine knot
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Official 2012 Collection
Institute for Molecular Bioscience - Publications
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Citation counts: TR Web of Science Citation Count  Cited 18 times in Thomson Reuters Web of Science Article | Citations
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