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Literature summary for 3.1.3.16 extracted from

  • Yamaguchi, H.; Durell, S.R.; Feng, H.; Bai, Y.; Anderson, C.W.; Appella, E.
    Development of a substrate-based cyclic phosphopeptide inhibitor of protein phosphatase 2Cdelta, Wip1 (2006), Biochemistry, 45, 13193-13202.
    View publication on PubMed
Search for more literature for 3.1.3.16

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21(DE3) cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
K238D not inhibited by c(MpSIpYVA) Homo sapiens
K238Q not inhibited by c(MpSIpYVA) Homo sapiens
R110E inhibited by c(MpSIpYVA) similar to the wild type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
c(M-L-2-amino-4-phosphono-4,4-difluorobutanoate-IpYVA)
-
 Homo sapiens
cyclic phosphopeptide c(M-L-2-amino-4-phosphono-4,4-difluorobutanoate-IpYVA) inhibits only Wip1 Homo sapiens
cyclic phosphopeptide c(MpSIpY)
-
 Homo sapiens
cyclic phosphopeptide c(MpSIpYV)
-
 Homo sapiens
cyclic phosphopeptide c(MpSIpYVA) inhibits only Wip1 Homo sapiens
cyclic phosphopeptide c(MpSIpYVAT)
-
 Homo sapiens
cyclic phosphopeptide c(TDDEMpSIpYVAT)
-
 Homo sapiens
additional information phosphoserine-containing diphosphorylated peptides with the sequence pSXpY inhibit Wip1 phosphatase activity; PP2A and PP2Calpha are not significantly inhibited by the cyclic phosphopeptides c(MpSIpYVA) and c(M-L-2-amino-4-phosphono-4,4-difluorobutanoate-IpYVA) Homo sapiens
phosphopeptide TDDEMpS-cyclohexylalanine-pYVAT 40% inhibition at 0.1 mM Homo sapiens
phosphopeptide TDDEMpS-D-pYVAT 32% inhibition at 0.1 mM Homo sapiens
phosphopeptide TDDEMpS-I-pYVAT 54% inhibition at 0.1 mM Homo sapiens
phosphopeptide TDDEMpS-P-pYVAT 26% inhibition at 0.1 mM Homo sapiens
phosphopeptide TDDEMpS-V-pYVAT 51% inhibition at 0.1 mM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information phosphothreonine-containing peptides with the sequence pTXpY are physiological substrates Homo sapiens ?
-
 ?
p38 MAP kinase phosphoprotein
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
PP2A
-
 Homo sapiens
PP2CR
-
 Homo sapiens
PPM1D
-
 Homo sapiens
protein phosphatase 2Cdelta
-
 Homo sapiens
serine/threonine phosphatase
-
 Homo sapiens
Wip1
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0009
-
 cyclic phosphopeptide c(MpSIpYVA) at 30°C and pH 7.5 Homo sapiens
0.0029
-
 cyclic phosphopeptide c(MpSIpYV) at 30°C and pH 7.5 Homo sapiens
0.0074
-
 cyclic phosphopeptide c(MpSIpY) at 30°C and pH 7.5 Homo sapiens
0.0252
-
 cyclic phosphopeptide c(MpSIpYVAT) at 30°CC and pH 7.5 Homo sapiens
0.035
-
 cyclic phosphopeptide c(TDDEMpSIpYVAT) at 30°C and pH 7.5 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0037
-
 at 30°C and pH 7.5 Homo sapiens cyclic phosphopeptide c(MpSIpYVA)
0.0116
-
 at 30°C and pH 7.5 Homo sapiens cyclic phosphopeptide c(MpSIpYV)
0.0165
-
 at 30°C and pH 7.5 Homo sapiens c(M-L-2-amino-4-phosphono-4,4-difluorobutanoate-IpYVA)
0.0294
-
 at 30?C and pH 7.5 Homo sapiens cyclic phosphopeptide c(MpSIpY)
0.0999
-
 at 30°C and pH 7.5 Homo sapiens cyclic phosphopeptide c(MpSIpYVAT)
0.1384
-
 at 30°C and pH 7.5 Homo sapiens cyclic phosphopeptide c(TDDEMpSIpYVAT)