Contulakin-G. Neurotensin Receptor Ligand.
Contulakin-G acts as an agonist of neurotensin receptors. It binds to human neurotensin type 1 receptor (NTSR1), rat neurotensin types 1 and 2 receptors (NTSR1/NTSR2) and mouse neurotensin type 3 receptor (SORT1).
Contulakin-G is a peptide initially isolated and purified from the marine snail Conus geographus venom based on its ability to induce sluggishness in mice.
O-linked glycosylation at Threonine residue at position 10 appears to be a highly unusual strategy for increasing the efficacy of toxins directed against neurotransmitter receptors. Although the binding affinity of Contulakin-G for cloned neurotensin receptors in vitro proved to be significantly lower than neurotensin, Contulakin-G was shown to be a neurotensin receptor agonist at physiologically relevant concentrations.
G-Protein Coupled Receptor Ligands; Neurotensin Receptor Ligands