Overview
- Craig A.G. et al. (1999) J. Biol. Chem. 274, 13752.
Alomone Labs Contulakin-G increases intracellular Ca2+ concentration in HT-29 cells.Cells were loaded with Fluo-3 AM. Changes in intracellular Ca2+ were detected via changes in Fluo-3 emission following Contulakin-G (#GPC-100) application. A. Normalized fluorescence before and after application (at 20 seconds, see arrow) of 0-3.3 μM Contulakin-G (as indicated). B. Normalized fluorescence plotted against Contulakin-G concentrations (n = 2, standard deviation indicated by error bars).
- Craig A.G. et al. (1999) J. Biol. Chem. 274, 13752.
- Craig, A.G. et al. (2001) Toxicon 39, 809.
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)1.
Contulakin-G is a peptide initially isolated and purified from the marine snail Conus geographus venom based on its ability to induce sluggishness in mice2.
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 receptors1. 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 concentrations1,2.
Contulakin-G (#GPC-100) is a highly pure, synthetic, and biologically active peptide toxin.
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