Protein Information

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

Compound Information

Name deltamethrin
CAS

Reference List

PubMed Abstract RScore(About this table)
1315545 Enan E, Matsumura F: Specific inhibition of calcineurin by type II synthetic pyrethroid insecticides. Biochem Pharmacol. 1992 Apr 15;43(8):1777-84.

It was found that all insecticidal Type II pyrethroids (cypermethrin, deltamethrin and fenvalerate) are potent inhibitors of isolated calcineurin from bovine brain.
85(1,1,1,5) Details
12242407 Allen GJ, Sanders D: Calcineurin, a Type 2B Protein Phosphatase, Modulates the Ca2+-Permeable Slow Vacuolar Ion Channel of Stomatal Guard Cells. Plant Cell. 1995 Sep;7(9):1473-1483.

The inhibitory effect of calcineurin could be blocked by the pyrethroid deltamethrin, indicating inhibition of SV channels by calcineurin via dephosphorylation.
84(1,1,1,4) Details
17551263 Martin C, Jacobi JS, Nava G, Jeziorski MC, Clapp C, Martinez de la Escalera G: GABA inhibition of cyclic AMP production in immortalized GnRH neurons is mediated by calcineurin-dependent dephosphorylation of adenylyl cyclase 9. Neuroendocrinology. 2007;85(4):257-66. Epub 2007 Jun 4.

Furthermore, blocking calcineurin with deltamethrin, FK-506 or cyclosporin A blocked the inhibitory effect of GABA on [cAMP] i, supporting the involvement of AC9 in this effect.
83(1,1,1,3) Details
16678970 Wu ZZ, Chen SR, Pan HL: Signaling mechanisms of down-regulation of voltage-activated Ca2+ channels by transient receptor potential vanilloid type 1 stimulation with olvanil in primary sensory neurons. Neuroscience. 2006 Aug 11;141(1):407-19. Epub 2006 May 6.

Furthermore, calcineurin (protein phosphatase 2B) inhibitors (deltamethrin and FK-506) eliminated the effect of olvanil on voltage-activated Ca (2+) channel current.
82(1,1,1,2) Details
9379408 Traynelis SF, Wahl P: Control of rat GluR6 glutamate receptor open probability by protein kinase A and calcineurin. J Physiol. 1997 Sep 15;503 ( Pt 3):513-31.

The calcineurin-stimulated decrease of Po,peak in cells co-transfected with C alpha-PKA is blocked by 800 nM deltamethrin, a calcineurin inhibitor.
36(0,1,1,6) Details
15337272 Choi JS, Soderlund DM: Cyclosporin A and deltamethrin block the downregulation of Nav1.8 sodium channels expressed in Xenopus oocytes. Neurosci Lett. 2004 Sep 9;367(3):389-93.

Perfusion of oocytes with either cyclosporin A or deltamethrin, considered to be diagnostic inhibitors of the protein phosphatase calcineurin, at 10 microM blocked spontaneous downregulation.
82(1,1,1,2) Details
9714322 Fakata KL, Swanson SA, Vorce RL, Stemmer PM: Pyrethroid insecticides as phosphatase inhibitors. . Biochem Pharmacol. 1998 Jun 15;55(12):2017-22.

The type II pyrethroid insecticides cis-cypermethrin (c-Cyp), trans-cypermethrin, deltamethrin (Delt), and fenvalerate A alpha (Fen), as well as the type I pyrethroid insecticides cis- and trans-permethrin and S-bioallethrin, were unable to inhibit the phosphatase activity of purified calcineurin under conditions of maximal activation by Ca2+ and calmodulin.
82(1,1,1,2) Details
10794729 Bandyopadhyay A, Shin DW, Kim DH: Regulation of ATP-induced calcium release in COS-7 cells by calcineurin. . Biochem J. 2000 May 15;348 Pt 1:173-81.

Measurement of calcineurin-specific phosphatase activity in vitro demonstrated a high level of endogenous calcineurin activities in COS-7 cells, which was effectively inhibited by the addition of deltamethrin or CsA.
39(0,1,1,9) Details
10995774 Hoy M, Bokvist K, Xiao-Gang W, Hansen J, Juhl K, Berggren PO, Buschard K, Gromada J: Phentolamine inhibits exocytosis of glucagon by Gi2 protein-dependent activation of calcineurin in rat pancreatic alpha -cells. J Biol Chem. 2001 Jan 12;276(2):924-30.

The inhibitory effect of phentolamine on exocytosis resulted from activation of the protein phosphatase calcineurin and was abolished by cyclosporin A and deltamethrin.
33(0,1,1,3) Details
11533141 Gromada J, Hoy M, Buschard K, Salehi A, Rorsman P: Somatostatin inhibits exocytosis in rat pancreatic alpha-cells by G (i2)-dependent activation of calcineurin and depriming of secretory granules. J Physiol. 2001 Sep 1;535(Pt 2):519-32.

The inhibitory effect of somatostatin on exocytosis was mediated by activation of the serine/threonine protein phosphatase calcineurin and was prevented by pretreatment with cyclosporin A and deltamethrin or intracellularly applied calcineurin autoinhibitory peptide.
33(0,1,1,3) Details
7531976 Richter A, Davies DE, Alexander P: Growth inhibitory effects of FK506 and cyclosporin A independent of inhibition of calcineurin. Biochem Pharmacol. 1995 Jan 31;49(3):367-73.

The role of calcineurin in CyA- or FK506-induced growth inhibition was investigated using the synthetic pyrethroid insecticides: cypermethrin, deltamethrin and fenvalerate, which are known calcineurin inhibitors.
32(0,1,1,2) Details
10575025 Liu Q, Berg DK: Actin filaments and the opposing actions of CaM kinase II and calcineurin in regulating alpha7-containing nicotinic receptors on chick ciliary ganglion neurons. J Neurosci. 1999 Dec 1;19(23):10280-8.

Blockade of calmodulin by calmidazolium or blockade of CaM kinase II with either KN93 or autocamtide-2-related inhibitory peptide each prevents the rundown; blockade of the phosphatase calcineurin with either cyclosporin A or deltamethrin increases the rundown.
32(0,1,1,2) Details
8661777 Vayro S, Simmons NL: An effect of Ca2+ on the Intrinsic Cl (-)-conductance of rat kidney cortex brush border membrane vesicles. J Membr Biol. 1996 Mar;150(2):163-73.

In addition, inhibitors of protein phosphatase 2B, deltamethrin (50 nM) and trifluoperazine (10 microM), caused partial reversal of Ca2 (+)-dependent inhibition of D-glucose uptake.
31(0,1,1,1) Details
10535451 Poulsen CR, Bokvist K, Olsen HL, Hoy M, Capito K, Gilon P, Gromada J: Multiple sites of purinergic control of insulin secretion in mouse pancreatic beta-cells. Diabetes. 1999 Nov;48(11):2171-81.

Inhibition of exocytosis by ATP resulted from G-protein-dependent activation of the serine/threonine protein phosphatase calcineurin and was abolished by cyclosporin A and deltamethrin.
31(0,1,1,1) Details
18611438 Ranta F, Dufer M, Stork B, Wesselborg S, Drews G, Haring HU, Lang F, Ullrich S: Regulation of calcineurin activity in insulin-secreting cells: stimulation by Hsp90 during glucocorticoid-induced apoptosis. Cell Signal. 2008 Oct;20(10):1780-6. Epub 2008 Jun 18.

Previously, we described that apoptotic cell death induced by the synthetic glucocorticoid dexamethasone (dex) is inhibited by calcineurin inhibitors, FK506 and deltamethrin, in insulin-secreting cells.
6(0,0,0,6) Details
11062058 Bandyopadhyay A, Shin DW, Ahn JO, Kim DH: Calcineurin regulates ryanodine receptor/Ca (2+)-release channels in rat heart. Biochem J. 2000 Nov 15;352 Pt 1:61-70.

Treatment of neonatal cardiomyocytes with 20 microM deltamethrin, 10 microM cyclosporin A (CsA), or 10 mciroM FK506 led to Ca (2+) oscillations in originally quiescent cardiomyocytes.
6(0,0,0,6) Details
9572286 Matsuda T, Takuma K, Asano S, Kishida Y, Nakamura H, Mori K, Maeda S, Baba A: Involvement of calcineurin in Ca2+ paradox-like injury of cultured rat astrocytes. J Neurochem. 1998 May;70(5):2004-11.

Deltamethrin (20 nM), another calcineurin inhibitor, had a similar protective effect, whereas okadaic acid did not.
6(0,0,0,6) Details
8985861 Hardwick JC, Parsons RL: Activation of the protein phosphatase calcineurin during carbachol exposure decreases the extent of recovery from end-plate desensitization. J Neurophysiol. 1996 Dec;76(6):3609-16.

This staurosporine-induced decrease in ACh sensitivity could be prevented by pretreatment with the protein phosphatase 2B (calcineurin) inhibitor deltamethrin (0.5 microM), whereas okadaic acid (5 microM) and calyculin A (0.5 microM), inhibitors of protein phosphatases 1 and 2A, had no effect. 3.
3(0,0,0,3) Details
9539223 Amico C, Cupello A, Fossati C, Robello M: Involvement of phosphatase activities in the run-down of GABA (A) receptor function in rat cerebellar granule cells in culture. Neuroscience. 1998 May;84(2):529-35.

This event could be prevented, even in the absence of ATP, by using the perforated-patch technique or by adding to the pipette medium either a blocker of protein tyrosine phosphatase, sodium vanadate, or deltamethrin, a blocker of the protein serine/threonine phosphatase calcineurin.
This event could be prevented, even in the absence of ATP, by using the perforated-patch technique or by adding to the pipette medium either a blocker of protein tyrosine phosphatase, sodium vanadate, or deltamethrin, a blocker of the protein serine/threonine phosphatase calcineurin.
1(0,0,0,1) Details
9037753 Robello M, Amico C, Cupello A: A dual mechanism for impairment of GABAA receptor activity by NMDA receptor activation in rat cerebellum granule cells. Eur Biophys J. 1997;25(3):181-7.

On the one hand Ca+2 influx across NMDA channels activates calcineurin and dephosphorylates the GABAA receptor complex directly or dephosphorylates proteins critical for the function of the receptor.
The NMDA effect was reduced by including adenosine-5'-O-3-thiophosphate (ATP-gamma-S) in the internal solution and there was a reduction in the NMDA effect caused by deltamethrin, a calcineurin inhibitor.
1(0,0,0,1) Details
8948591 Carrera A, Moos J, Ning XP, Gerton GL, Tesarik J, Kopf GS, Moss SB: Regulation of protein tyrosine phosphorylation in human sperm by a calcium/calmodulin-dependent mechanism: identification of A kinase anchor proteins as major substrates for tyrosine phosphorylation. Dev Biol. 1996 Nov 25;180(1):284-96.

This Ca2+-induced dephosphorylation was calmodulin-dependent, suggesting that calcineurin was involved.
In this regard, the calcineurin inhibitor deltamethrin inhibited the Ca2+ ionophore-induced dephosphorylation.
1(0,0,0,1) Details
10627609 Lautermilch NJ, Spitzer NC: Regulation of calcineurin by growth cone calcium waves controls neurite extension. J Neurosci. 2000 Jan 1;20(1):315-25.

Pharmacological blockers of CN (cyclosporin A and deltamethrin) and peptide inhibitors of CN [the Xenopus CN (xCN) autoinhibitory domain and African swine fever virus protein A238L] block the Ca (2+)-dependent reduction of neurite outgrowth in cultured neurons.
2(0,0,0,2) Details
16644695 Ranta F, Avram D, Berchtold S, Dufer M, Drews G, Lang F, Ullrich S: Dexamethasone induces cell death in insulin-secreting cells, an effect reversed by exendin-4. Diabetes. 2006 May;55(5):1380-90.

Dexamethasone increased PP-2B (calcineurin) activity, an effect abrogated by FK506.
FK506 (0.1 micromol/l) and another calcineurin inhibitor, deltamethrin (1 micromol/l), attenuated dexamethasone-induced cell death.
2(0,0,0,2) Details
9594016 Fischer H, Illek B, Machen TE: Regulation of CFTR by protein phosphatase 2B and protein kinase C. . Pflugers Arch. 1998 Jul;436(2):175-81.

Treating CFTR-expressing 3T3 cells with either of the two specific PP2B blockers cyclosporin A (CsA, 1 microM) or deltamethrin (DM, 30 nM) caused rapid activation of CFTR in cell-attached patches.
2(0,0,0,2) Details
15746091 Wu ZZ, Chen SR, Pan HL: Transient receptor potential vanilloid type 1 activation down-regulates voltage-gated calcium channels through calcium-dependent calcineurin in sensory neurons. J Biol Chem. 2005 May 6;280(18):18142-51. Epub 2005 Mar 3.

Furthermore, intracellular dialysis of deltamethrin or cyclosporin A, the specific calcineurin (protein phosphatase 2B) inhibitors, but not okadaic acid (a selective protein phosphatase 1/protein phosphatase 2A inhibitor), abolished the effect of capsaicin on I (Ca).
2(0,0,0,2) Details
10844399 Kampermann J, Herbst M, Ullrich S: Effects of adrenaline and tolbutamide on insulin secretion in INS-1 cells under voltage control. Cell Physiol Biochem. 2000;10(1-2):81-90.


After incubation of the cells with deltamethrin, a calcineurin inhibitor, the stimulation of secretion was attenuated, but the adrenaline-induced inhibition was not affected.
0(0,0,0,0) Details
17200551 Swingle M, Ni L, Honkanen RE: Small-molecule inhibitors of ser/thr protein phosphatases: specificity, use and common forms of abuse. Methods Mol Biol. 2007;365:23-38.


Inhibitors of PP2B (calcineurin) will only be mentioned in passing, except to state that, in our hands, cypermethrin, deltamethrin, and fenvalerate, which are sold as potent inhibitors of PP2B, do not inhibit the catalytic activity of PP2B.
0(0,0,0,0) Details
11562451 Dufer M, Krippeit-Drews P, Lembert N, Idahl LA, Drews G: Diabetogenic effect of cyclosporin A is mediated by interference with mitochondrial function of pancreatic B-cells. Mol Pharmacol. 2001 Oct;60(4):873-9.


This effect is not due to an inhibition of calcineurin, which mediates the immunosuppressive effect of CsA, because other calcineurin inhibitors, deltamethrin and tacrolimus, did not affect the oscillations in [Ca (2+)](c) of the B-cells.
0(0,0,0,0) Details
10936494 Thompson TL, Moore CC, Smith B: Estrogen priming modulates autoreceptor-mediated potentiation of dopamine uptake. Eur J Pharmacol. 2000 Aug 11;401(3):357-63.


Pretreatment with protein phosphatase 2B (deltamethrin, cypermethrin) or protein phosphatase 1 (tautomycin) inhibitors attenuated basal and quinpirole-potentiated dopamine uptake in ovariectomized but not estrogen-primed tissue.
0(0,0,0,0) Details