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Targeting of Protein Phosphatases PP2A and PP2B to the C-terminus of the L-type Calcium Channel Cav1.2
Journal article   Peer reviewed

Targeting of Protein Phosphatases PP2A and PP2B to the C-terminus of the L-type Calcium Channel Cav1.2

Hui Xu, Kenneth S Ginsburg, Duane D Hall, Maike Zimmermann, Ivar S Stein, Mingxu Zhang, Samvit Tandan, Joseph A Hill, Mary C Horne, Donald Bers, …
Biochemistry (Easton), Vol.49(48), pp.10298-10307
12/07/2010
DOI: 10.1021/bi101018c
PMCID: PMC3075818
PMID: 21053940

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Abstract

The L-type Ca 2+ channel Ca v 1.2 forms macromolecular signaling complexes that comprise the β 2 adrenergic receptor, trimeric G s protein, adenylyl cyclase, and cAMP-dependent protein kinase (PKA 1 ) for efficient signaling in heart and brain. The protein phosphatases PP2A and PP2B are part of this complex. PP2A counteracts increase in Ca v 1.2 channel activity by PKA and other protein kinases, whereas PP2B can either augment or decrease Ca v 1.2 currents in cardiomyocytes depending on the precise experimental conditions. We found that PP2A binds to two regions in the C-terminus of the central, pore-forming α 1 subunit of Ca v 1.2: one region spans residues 1795-1818 and the other residues 1965-1971. PP2B binds immediately downstream of residue 1971. Injection of a peptide that contained residues 1965-1971 and displaced PP2A but not PP2B from endogenous Ca v 1.2 increased basal and isoproterenol-stimulated L-type Ca 2+ currents in acutely isolated cardiomyocytes. Together with our biochemical data, these physiological results indicate that anchoring of PP2A at this site of Ca v 1.2 in the heart negatively regulates cardiac L-type currents, likely by counterbalancing basal and stimulated phosphorylation that is mediated by PKA and possibly other kinases.

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