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

Analgesic action

Conotoxins and spider toxins that block voltage-sensitive calcium chanels are potent analgesics

  • Neurotoxin Tx3-6 from brazilian armed spider displayed higher efficacy and long-lasting analgesia in a thermal model of pain, when compared with omega-conotoxin MVIIA. Tx3-6 was also more effective to reverse previously installed persistent chemical and neuropathic pain. It is suggested that Tx3-6 might be useful in the control of persistent pathological pain [Souza et al., 2008].
  • The tarantula spider toxin GsMTx4 was shown to reduce mechanical and neuropathic pain . However, GsMTx4 did not affect response to thermal stimuli [Park et al., 2008].
  • Omega-conotoxin MVIIA (Ziconotide) is a potent analgesic and has been approved for the treatment of severe chronic pain [Wallace 2006].