Compound class:
Peptide or derivative
Comment: Octpep-1 is a 12 amino acid peptide that's derived from an octopus venom molecule. It disrupts PI3K/AKT pathway signalling in melanoma cells and produces a cytotoxic effect that is selective for these cells compared to normal fibroblasts [2]. Octpep-1 can induce an antiproliferative effect against aggressive and hard-to-treat melanoma cells that are driven by the BRAFV600E mutation [1]. Although Octpep-1 appears to exhibit (very) weak agonist activity at tachykinin NK1 receptors, it's antiproliferative activity is independent of NK1R expression [1].
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Bioactivity Comments |
Agonist potency at all three tachykinin receptors is ~200 μM measuring intracellular Ca2+ responses in receptor-expressing COS-1 cells [1]. |