Knottins display a variety of biological functions


  • ‣ Some knottins are thought to perform their action via interaction with a receptor.
  • ‣ This has led several authors to use the slightly restrictive name "Inhibitor Cystine Knot" (ICK)
  • ‣ Different activities are located on different parts of the molecules, and almost all Knottin loops have been implied in one ore more function.
  • ‣ The major known biological functions exerted by Knottins are briefly outlined below.
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Analgesics

Anthelmintic

Anti-ED

Antimalarial

Antimicrobials

Antitumors

Protease inhibitors

Toxins

Insecticids

Others

Antitumors

Antitumor activities have been shown for PCI and cyclotides

  • The Potato Carboxypeptidase inhibitor PCI is an antagonist of human EGF and inhibits tumor cell growth [Blanco-Aparicio et al., 1998 ]
  • The cyclotides varv A, varv F, and cycloviolacin O2 display cytotoxicity for several human tumor cell lines [Lindholm et al., 2002]. The activity profiles differed significantly from those of antitumor drugs in clinical use, suggesting a new mode of action for these cyclotides.
  • Cycloviolacin O2 Disrupts Lipid Membranes. Cytotoxic, antimicrobial, hemolytic, and insecticidal effects are likely all connected to membrane disruption. [Svangard et al., 2007 ].