title: Chemical activators of protein phosphatase-1 induce calcium release inside intact cells.
abstract: Protein phosphatase-1 (PP1) is a major Ser/Thr phosphatase that is involved in numerous cellular processes. PP1-disrupting peptides (PDPs) are selective chemical tools used to study PP1. They generate catalytically active PP1 inside cells but do not bind to the closely related PP2A. Here, we show that PDPs also do not act directly on PP2B, thus demonstrating the selectivity of PDPs toward PP1. We present PDPs with different properties, enabling reversible versus permanent activation of PP1. We also show that Ca(2+) spiking is an acute effect caused by PDP-induced activation of PP1. The Ca(2+) is released from internal stores. Our data show that PDPs can be used as selective chemical genetics tools to study acute and long-term effects of PP1 activation in intact cells, and PDPs will therefore be valuable tools to study PP1 biology.
authors: Cell Biology and Biophysics Unit, European Molecular Biology Laboratory (EMBL), 69117 Heidelberg, Germany.
authors: Gregor
authors: G
authors: Reither
authors: Jayanta
authors: J
authors: Chatterjee
authors: Monique
authors: M
authors: Beullens
authors: Mathieu
authors: M
authors: Bollen
authors: Carsten
authors: C
authors: Schultz
authors: Maja
authors: M
authors: Köhn
mesh_terms: D000595:Amino Acid Sequence; D019703:Calcineurin / Q000737:chemistry / Q000378:metabolism; D002118:Calcium / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D008969:Molecular Sequence Data; D010455:Peptides / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D054645:Protein Phosphatase 1 / Q000737:chemistry / Q000378:metabolism*; D054648:Protein Phosphatase 2 / Q000737:chemistry / Q000378:metabolism
chemical_list: D010455:Peptides; D019703:Calcineurin; D054645:Protein Phosphatase 1; D054648:Protein Phosphatase 2; D002118:Calcium