Table 2 Peptides and proteins inhibiting calcineurin-NFATc signalling

Inhibitor peptide	Mode of action	IC₅₀/K_d/K_i*	References
CaN_457-482-AID		10 μM^a	Perrino BA 1999 [167]
mask the active centre of CaN
CaN_424-521-AID		2.5 μM^a	Sagoo JK 1996 [164]
mNFATc2_106-121 - SPRIEIT		12 μMⁱ	Aramburu J 1998 [21]
block CaN-NFATc interaction
VIVIT peptide		0.5 μM* ^k < 1 μM^l	Roehrl MH 2004 [114] Aramburu J 1999 [171]
AKAP79_330-357	blocks CaN-NFATc interaction	1.5 μM^a	Dell'Acqua ML 2002 [173]
RCAN1		60 nM* ^k	Chan B 2005 [177]
RCAN1-4_141-197 - exon7	block CaN-NFATc interaction	70 nM* ^k	Chan B 2005 [177]
RCAN1-4_143-163 - CIC peptide		1.25 μM* ^k	Mulero MC 2009 [111]
LxVPc1 peptide	blocks CaN-NFATc interaction and modulates enzymatic activity of CaN	~3 μM^a	Rodriguez A 2009 [24]
RCAN1-4_95-118 - 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
A238L_200-213		0.6 μM^k	Miskin JE 2000 [194]

N.D.: not determined
Indicated methods for IC₅₀/K_d/K_i determination: a - phosphatase assay on R_II 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

ISSN: 1478-811X