Protein Information

Name protein phosphatase 2B (protein family or complex)
Synonyms Calcineurin; Calcineurins; Protein phosphatase 2B

Compound Information

Name 4-aminopyridine
CAS 4-pyridinamine

Reference List

PubMed Abstract RScore(About this table)
11588168 Jovanovic JN, Sihra TS, Nairn AC, Hemmings HC Jr, Greengard P, Czernik AJ: Opposing changes in phosphorylation of specific sites in synapsin I during Ca2+-dependent glutamate release in isolated nerve terminals. J Neurosci. 2001 Oct 15;21(20):7944-53.


We demonstrate that, in vitro, phosphorylation sites 1, 2, and 3 of synapsin I (P-site 1 phosphorylated by cAMP-dependent protein kinase; P-sites 2 and 3 phosphorylated by Ca (2+)-calmodulin-dependent protein kinase II) were excellent substrates for protein phosphatase 2A, whereas P-sites 4, 5, and 6 (phosphorylated by mitogen-activated protein kinase) were efficiently dephosphorylated only by Ca (2+)-calmodulin-dependent protein phosphatase 2B-calcineurin.
2(0,0,0,2) Details
11222925 Storchak LG, Kravchuk MV, Himmelreich NH: Okadaic acid and cyclosporin A modulate [(3) H] GABA release from rat brain synaptosomes. Neurochem Int. 2001 Apr;38(5):445-51.

Rat brain synaptosomes were used to investigate the effect of okadaic acid, an inhibitor of protein phosphatase 1 and 2A, and cyclosporin A, an inhibitor of protein phosphatase 2B (calcineurin), on [(3) H] GABA release.
Release of [(3) H] GABA was evoked by 4-aminopyridine in the presence of calcium and by alpha-latrotoxin in the presence and absence of calcium.
1(0,0,0,1) Details
14976250 Bush E, Fielitz J, Melvin L, Martinez-Arnold M, McKinsey TA, Plichta R, Olson EN: A small molecular activator of cardiac hypertrophy uncovered in a chemical screen for modifiers of the calcineurin signaling pathway. Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):2870-5. Epub 2004 Feb 19.

In a high-throughput screen for small molecules capable of regulating MCIP1 expression in muscle cells, we identified a unique 4-aminopyridine derivative exhibiting an embedded partial structural motif of serotonin (5-hydroxytryptamine, 5-HT).
4(0,0,0,4) Details
10854899 Sistiaga A, Sanchez-Prieto J: Protein phosphatase 2B inhibitors mimic the action of arachidonic acid and prolong the facilitation of glutamate release by group I mGlu receptors. Neuropharmacology. 2000 Jul 10;39(9):1544-53.

The activation of these receptors with the specific agonist 3,5-dihydroxyphenylglycine (DHPG) failed to enhance the cumulative Ca (2+)-dependent release of glutamate evoked by a 5 min depolarization with 4-aminopyridine, in the absence but not in the presence of arachidonic acid.
2(0,0,0,2) Details
20051248 Jin H, Hadri L, Palomeque J, Morel C, Karakikes I, Kaprielian R, Hajjar R, Lebeche D: KChIP2 attenuates cardiac hypertrophy through regulation of I (to) and intracellular calcium signaling. J Mol Cell Cardiol. 2010 Jan 4.

It also significantly decreased calcineurin expression, NFATc1 expression and nuclear translocation and its downstream target, MCiP1.4.
Interestingly, blocking I (to) with 4-aminopyridine in KChIP2-overexpressing adult cardiomyocytes significantly increased the Ca (2+) transients to control levels.
2(0,0,0,2) Details