CALP3 TFA

CALP3, a Ca2+-like peptide, is a potent Ca2+ channel blocker that activates EF hand motifs of Ca2+-binding proteins. CALP3 can functionally mimic increased [Ca2+]i by modulating the activity of Calmodulin (CaM), Ca2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia[1][2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Cancer

Research Areas >> Neurological Disease

Ca2+

CALP3 (50, 100, 150, 200 μM) inhibits glutamate caused a large sustained increase in [Ca2+]i in a dose-dependent manner (IC50=37.25 μM) in Fura-2-loaded neuronal cultures[1]. CALP3 (50, 100, 150, 200 μM) inhibits glutamate-induced cytotoxicity in a dose-dependent manner (IC50=50.97 μM) in cultured rat neocortical neurons. CALP3 causes dose-dependent inhibition of apoptosis (IC50=33.41 μM)[1]. CALP3 (100 μM) inhibits apoptosis induced by HIV gp120 and SAg in Human T cells[1]. CALP3 (100 μM; 15 min pretreatment) reduces gossypol-induced necrosis and increases the fraction of live cells[2]. Cyclic-CALP3 is synthesized starting from Fmoc-Asp(PEG-PS)-OAl. Cyclic CALP3 is unable to inhibit Ca21 influx, and this peptide served as a negative control. Cyclic CALP3 does not inhibit the effect of glutamate[1].

[1]. Manion MK, et al. A new type of Ca(2+) channel blocker that targets Ca(2+) sensors and prevents Ca(2+)-mediated apoptosis. FASEB J. 2000 Jul;14(10):1297-306.

[2]. Ferdek PE, et al. BH3 mimetic-elicited Ca2+ signals in pancreatic acinar cells are dependent on Bax and can be reduced by Ca²⁺-like peptides. Cell Death Dis. 2017 Mar 2;8(3):e2640.