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Table 2 Peptides and proteins inhibiting calcineurin-NFATc signalling

From: Novel inhibitors of the calcineurin/NFATc hub - alternatives to CsA and FK506?

Inhibitor peptide Mode of action IC50/Kd*/Ki** References
CaN457-482-AID   10 μMa Perrino BA 1999 [167]
mask the active centre of CaN    
CaN424-521-AID   2.5 μMa Sagoo JK 1996 [164]
mNFATc2106-121 - SPRIEIT   12 μMi Aramburu J 1998 [21]
block CaN-NFATc interaction    
VIVIT peptide   0.5 μM* k < 1 μMl Roehrl MH 2004 [114] Aramburu J 1999 [171]
AKAP79330-357 blocks CaN-NFATc interaction 1.5 μMa Dell'Acqua ML 2002 [173]
RCAN1   60 nM* k Chan B 2005 [177]
RCAN1-4141-197 - exon7 block CaN-NFATc interaction 70 nM* k Chan B 2005 [177]
RCAN1-4143-163 - CIC peptide   1.25 μM* k Mulero MC 2009 [111]
LxVPc1 peptide blocks CaN-NFATc interaction and modulates enzymatic activity of CaN ~3 μMa Rodriguez A 2009 [24]
RCAN1-495-118 - SP repeat peptide masks the active centre of CaN 91.5 μM** a Vega RB 2002 [185]
VacA inhibits translocation of NFATc N.D. Gebert B 2003 [187]
A238L   N.D. Miskin JE 1998 [190]
block CaN-NFATc interaction    
A238L200-213   0.6 μMk Miskin JE 2000 [194]
  1. N.D.: not determined
  2. Indicated methods for IC50/Kd/Ki determination: a - phosphatase assay on RII phosphopeptide; b - phosphatase assay on pNPP; c - NFAT dependent reporter gene expression; d - IL-2 promoter dependent reporter gene expression; e - phosphatase assay on 4-methylumbelliferyl phosphate; f - displacement of VIVIT peptide; g - IL-2 secretion assay; h - EMSA for NFATc; i - interference with CaN-NFATc binding assay; k - binding assay to CaN; l - phosphatase assay on NFATc; m - cell proliferation assay