Cell-permeable calmodulin (CaM)
agonist that binds to the EF-hand/Ca2+-binding site; produces
CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites
on other Ca2+ channels, including NMDAand HIV-1 gp120-activated channels,
inhibiting Ca2+-mediated cytotoxicity and apoptosis (IC50
= 52 μM). Inhibits VLA-5-mediated adhesion of mast cells to fibronectin in
vitro and attenuates inflammatory cell influx in guinea pig lung in vivo.
Villainet al (2000) De novo design of peptides targeted to
the EF hands of calmodulin. J.Biol.Chem. 274 2676. Manion
et al (2000) A new type of Ca2+ channel blocker that targets Ca2+
sensors and prevents Ca2+-mediated apoptosis. FASEB J. 14
1297. Houtman et al (2001) Attenuation of very late
antigen-5-mediated adhesion of bone marrow-derived mast cells to fibronectin by
peptides with inverted hydropathy to EF-hands. J.Immunol. 166
861. Ten Broeke et al (2003) Ca2+ sensors modulate
asthmatic symptoms in an allergic model for asthma. Eur.J.Pharmacol. 476
151.
