CALP1 (TFA)

CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity[1][2][3][4].

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[1]R Houtman, et al. 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. 2001 Jan 15;166(2):861-7.|[2]R Ten Broeke, et al. Calcium sensors as new therapeutic targets for airway hyperresponsiveness and asthma. FASEB J. 2001 Aug;15(10):1831-3.|[3]M K Manion, 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.|[4]M Villain, et al. De novo design of peptides targeted to the EF hands of calmodulin. J Biol Chem. 2000 Jan 28;275(4):2676-85.