Table 2 |
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Peptides and proteins inhibiting calcineurin-NFATc signalling |
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|
Inhibitor peptide |
Mode of action |
IC50/Kd*/Ki** |
References |
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|
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CaN457-482-AID |
10 μMa |
Perrino BA 1999 [167] |
|
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|
mask the active centre of CaN |
|
|
|
CaN424-521-AID |
2.5 μMa |
Sagoo JK 1996 [164] |
|
|
|
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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] |
|
|
|
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|
AKAP79330-357 |
blocks CaN-NFATc interaction |
1.5 μMa |
Dell'Acqua ML 2002 [173] |
|
|
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|
RCAN1 |
60 nM* k |
Chan B 2005 [177] |
|
|
|
|
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|
RCAN1-4141-197 - exon7 |
block CaN-NFATc interaction |
70 nM* k |
Chan B 2005 [177] |
|
|
|
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|
RCAN1-4143-163 - CIC peptide |
1.25 μM* k |
Mulero MC 2009 [111] |
|
|
|
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|
LxVPc1 peptide |
blocks CaN-NFATc interaction and modulates enzymatic activity of CaN |
~3 μMa |
Rodriguez A 2009 [24] |
|
|
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RCAN1-495-118 - SP repeat peptide |
masks the active centre of CaN |
91.5 μM** a |
Vega RB 2002 [185] |
|
|
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VacA |
inhibits translocation of NFATc |
N.D. |
Gebert B 2003 [187] |
|
|
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A238L |
N.D. |
Miskin JE 1998 [190] |
|
|
|
block CaN-NFATc interaction |
|
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|
A238L200-213 |
0.6 μMk |
Miskin JE 2000 [194] |
|
|
|
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N.D.: not determined 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 |
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Sieber and Baumgrass Cell Communication and Signaling 2009 7:25 doi:10.1186/1478-811X-7-25 |
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