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Literature summary for 3.1.3.16 extracted from

  • Gibbons, J.A.; Weiser, D.C.; Shenolikar, S.
    Importance of a surface hydrophobic pocket on protein phosphatase-1 catalytic subunit in recognizing cellular regulators (2005), J. Biol. Chem., 280, 15903-15911.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression of wild-type and mutant PP1alpha subunits in Escherichia coli strain BL21 Homo sapiens

Protein Variants

Protein Variants Comment Organism
C291R site-directed mutagenesis, mutation of a hydrophobic surface pocket residue of subunit PP1alpha, the mutant shows reduced activity and impaired binding to protein phosphatase inhibitor-1 and protein phosphatase inhibitor-2, as well as to the neuronal regulatory subunit neurabin-I, and GM, the skeletal muscle glycogen-targeting subunit Homo sapiens
L289R site-directed mutagenesis, mutation of a hydrophobic surface pocket residue of subunit PP1alpha, the mutant shows reduced activity and reduced sensitivity to protein phosphatase inhibitor-1 and protein phosphatase inhibitor-2, as well as to the neuronal regulatory subunit neurabin-I, and GM, the skeletal muscle glycogen-targeting subunit Homo sapiens
M290K site-directed mutagenesis, mutation of a hydrophobic surface pocket residue of subunit PP1alpha, the mutant shows reduced activity and reduced sensitivity to protein phosphatase inhibitor-1 and protein phosphatase inhibitor-2, as well as to the neuronal regulatory subunit neurabin-I, and GM, the skeletal muscle glycogen-targeting subunit Homo sapiens
additional information construction of a C-terminally truncated PP1alpha subunit and a chimeric PP1alpha subunit containing the C-terminus of PP2A Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information IC50 of inhibitors for mutant PP1alpha catalytic subunits, overview Homo sapiens
neurabin-I IC50 for the wild-type catalytic subunit PP1alpha is 1.75 nM Homo sapiens
okadaic acid IC50 for the wild-type catalytic subunit PP1alpha is 157 nM Homo sapiens
Protein phosphatase inhibitor-1 i.e. I-1, specific inhibition of PP1, contains a consensus RVxF motif sequence, IC50 for the wild-type catalytic subunit PP1alpha is 25 nM Homo sapiens
protein phosphatase inhibitor-2 i.e. I-2, specific inhibition of PP1, contains a consensus RVxF motif sequence, IC50 for the wild-type catalytic subunit PP1alpha is 2 nM Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mn2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens PP1 contains a surface hydrophobic pocket on the catalytic subunit which is important in recognizing cellular regulators via their consensus RVxF motifs, regulation of the enzyme, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
recombinant wild-type and mutant PP1alpha subunits from Escherichia coli strain BL21 performing multiple chromatographic steps including affinity chromatography on MLCR- and heparin-resins Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
neuron
-
Homo sapiens
-
skeletal muscle
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information PP1 contains a surface hydrophobic pocket on the catalytic subunit which is important in recognizing cellular regulators via their consensus RVxF motifs, regulation of the enzyme, overview Homo sapiens ?
-
?
phosphorylated myelin basic protein + H2O
-
Homo sapiens myelin basic protein + phosphate
-
?
phosphorylated phosphorylase a + H2O
-
Homo sapiens phosphorylase a + phosphate
-
?

Subunits

Subunits Comment Organism
More association of catalytic subunit PP1alpha with regulatory subunits, e.g. the neuronal regulatory subunit neurabin-I, or GM, the skeletal muscle glycogen-targeting subunit, overview Homo sapiens

Synonyms

Synonyms Comment Organism
More EC 3.1.3.53, myosin-light-chain-phosphatase Homo sapiens
PP1
-
Homo sapiens
PP2A
-
Homo sapiens
protein phosphatase-1
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000175
-
IC50 for the wild-type catalytic subunit PP1alpha is 1.75 nM Homo sapiens neurabin-I
0.000002
-
i.e. I-2, specific inhibition of PP1, contains a consensus RVxF motif sequence, IC50 for the wild-type catalytic subunit PP1alpha is 2 nM Homo sapiens protein phosphatase inhibitor-2
0.000025
-
i.e. I-1, specific inhibition of PP1, contains a consensus RVxF motif sequence, IC50 for the wild-type catalytic subunit PP1alpha is 25 nM Homo sapiens Protein phosphatase inhibitor-1
0.000157
-
IC50 for the wild-type catalytic subunit PP1alpha is 157 nM Homo sapiens okadaic acid