Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Kemp, B.E.; Pearson, R.B.; House, M.
    Pseudosubstrate-based peptide inhibitors (1991), Methods Enzymol., 201, 287-304.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.13 FTRKRQRAMRRVHQ autoregulatory pseudosubstrate sequence, residues 24-40, lung enzyme Homo sapiens
2.7.11.13 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential Drosophila melanogaster
2.7.11.13 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential, sequences of the different enzyme forms, required sequence properties, overview eukaryota
2.7.11.13 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential Homo sapiens
2.7.11.13 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential Saccharomyces cerevisiae
2.7.11.13 NKMKSRLRKGALKKNV autoregulatory pseudosubstrate sequence, residues 24-40 Drosophila melanogaster
2.7.11.13 QLMGGLHRHGAIINRKE autoregulatory pseudosubstrate sequence, residues 391-407 Saccharomyces cerevisiae
2.7.11.13 Tween 80 inhibits the enzyme at high concentration Drosophila melanogaster
2.7.11.13 Tween 80 inhibits the enzyme at high concentration eukaryota
2.7.11.13 Tween 80 inhibits the enzyme at high concentration Homo sapiens
2.7.11.13 Tween 80 inhibits the enzyme at high concentration Saccharomyces cerevisiae
2.7.11.17 ARRKWQKTGHAVRAIGRLSS calmodulin antagonist peptide, IC50: 33.3 nM in H2O, 10.6 nM in buffer containing 0.1% w/v Tween 80 eukaryota
2.7.11.17 additional information synthesis of peptides behaving as autoregulatory pseudosubstrates, determination of inhibitory potential, sequences of autoregulatory regions of the different enzyme forms, required sequence properties, overview eukaryota
2.7.11.18 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential eukaryota
2.7.11.18 SKDRMKKYMARRKWQKTGHAVRAI autoregulatory pseudosubstrate sequence of smooth muscle enzyme, residues 787-810 eukaryota
2.7.11.18 SQRLLKKYLMKRRWKKNFIAVSAA autoregulatory pseudosubstrate sequence of the skeletal muscle enzyme, residues 570-593 eukaryota
2.7.11.19 LLRDPYALRSVRHLIDNCAFRL autoregulatory pseudosubstrate sequence of the gamma subunit, residues 336-357 Homo sapiens
2.7.11.19 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential Homo sapiens
2.7.11.19 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential Mus musculus
2.7.11.19 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential Oryctolagus cuniculus
2.7.11.19 VIRDPYALPPLRRLIDAYAFRI autoregulatory pseudosubstrate sequence of the gamma subunit, residues 333-354 Mus musculus
2.7.11.19 VIRDPYALRPLRRLIDAYAFRI autoregulatory pseudosubstrate sequence of the gamma subunit, residues 332-353 Oryctolagus cuniculus
2.7.11.24 (hydroxy-2-naphthalenylmethyl)phosphonic acid inhibits the insulin receptor tyrosine kinase, IC50 is 0.01 mM eukaryota
2.7.11.24 additional information synthesis of peptides behaving as pseudosubstrates, determination of inhibitory potential eukaryota

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.7.11.13 Mg2+
-
Drosophila melanogaster
2.7.11.13 Mg2+
-
eukaryota
2.7.11.13 Mg2+
-
Homo sapiens
2.7.11.13 Mg2+
-
Saccharomyces cerevisiae
2.7.11.17 Ca2+ binding required for activity eukaryota
2.7.11.18 Mg2+
-
eukaryota
2.7.11.19 Mg2+
-
Mus musculus
2.7.11.19 Mg2+
-
Homo sapiens
2.7.11.19 Mg2+
-
Oryctolagus cuniculus
2.7.11.24 Mg2+
-
eukaryota

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.13 ATP + a protein Drosophila melanogaster
-
ADP + a phosphoprotein
-
?
2.7.11.13 ATP + a protein eukaryota
-
ADP + a phosphoprotein
-
?
2.7.11.13 ATP + a protein Homo sapiens
-
ADP + a phosphoprotein
-
?
2.7.11.13 ATP + a protein Saccharomyces cerevisiae
-
ADP + a phosphoprotein
-
?
2.7.11.17 ATP + a protein eukaryota
-
ADP + a phosphoprotein
-
?
2.7.11.18 ATP + myosin light chain eukaryota
-
ADP + phosphorylated myosin light chain
-
?
2.7.11.19 ATP + a protein Mus musculus
-
ADP + a phosphoprotein
-
?
2.7.11.19 ATP + a protein Homo sapiens
-
ADP + a phosphoprotein
-
?
2.7.11.19 ATP + a protein Oryctolagus cuniculus
-
ADP + a phosphoprotein
-
?
2.7.11.19 ATP + phosphorylase b Mus musculus
-
ADP + phosphorylase a
-
?
2.7.11.19 ATP + phosphorylase b Homo sapiens
-
ADP + phosphorylase a
-
?
2.7.11.19 ATP + phosphorylase b Oryctolagus cuniculus
-
ADP + phosphorylase a
-
?
2.7.11.24 ATP + a protein eukaryota
-
ADP + a phosphoprotein
-
?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.13 Drosophila melanogaster
-
-
-
2.7.11.13 eukaryota
-
enzyme forms alpha, betaI ans betaII, gamma, epsilon, delta, zeta
-
2.7.11.13 Homo sapiens
-
-
-
2.7.11.13 Saccharomyces cerevisiae
-
-
-
2.7.11.17 eukaryota
-
enzyme forms alpha, beta, gamma, delta
-
2.7.11.18 eukaryota
-
-
-
2.7.11.19 Homo sapiens
-
-
-
2.7.11.19 Mus musculus
-
-
-
2.7.11.19 Oryctolagus cuniculus
-
-
-
2.7.11.24 eukaryota
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
2.7.11.17 phosphoprotein autophosphorylation at Ser19 eukaryota
2.7.11.24 phosphoprotein autophosphorylation near the pseudosubstrate site eukaryota

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.13 lung
-
Homo sapiens
-
2.7.11.18 skeletal muscle
-
eukaryota
-
2.7.11.18 smooth muscle
-
eukaryota
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.13 ATP + a protein
-
Drosophila melanogaster ADP + a phosphoprotein
-
?
2.7.11.13 ATP + a protein
-
eukaryota ADP + a phosphoprotein
-
?
2.7.11.13 ATP + a protein
-
Homo sapiens ADP + a phosphoprotein
-
?
2.7.11.13 ATP + a protein
-
Saccharomyces cerevisiae ADP + a phosphoprotein
-
?
2.7.11.13 additional information substrate specificity Drosophila melanogaster ?
-
?
2.7.11.13 additional information substrate specificity eukaryota ?
-
?
2.7.11.13 additional information substrate specificity Homo sapiens ?
-
?
2.7.11.13 additional information substrate specificity Saccharomyces cerevisiae ?
-
?
2.7.11.17 ATP + a protein
-
eukaryota ADP + a phosphoprotein
-
?
2.7.11.17 additional information substrate specificity eukaryota ?
-
?
2.7.11.18 ATP + myosin light chain
-
eukaryota ADP + phosphorylated myosin light chain
-
?
2.7.11.18 additional information substrate specificity eukaryota ?
-
?
2.7.11.19 ATP + a protein
-
Mus musculus ADP + a phosphoprotein
-
?
2.7.11.19 ATP + a protein
-
Homo sapiens ADP + a phosphoprotein
-
?
2.7.11.19 ATP + a protein
-
Oryctolagus cuniculus ADP + a phosphoprotein
-
?
2.7.11.19 ATP + phosphorylase b
-
Mus musculus ADP + phosphorylase a
-
?
2.7.11.19 ATP + phosphorylase b
-
Homo sapiens ADP + phosphorylase a
-
?
2.7.11.19 ATP + phosphorylase b
-
Oryctolagus cuniculus ADP + phosphorylase a
-
?
2.7.11.19 additional information substrate specificity Mus musculus ?
-
?
2.7.11.19 additional information substrate specificity Homo sapiens ?
-
?
2.7.11.19 additional information substrate specificity Oryctolagus cuniculus ?
-
?
2.7.11.24 ATP + a protein
-
eukaryota ADP + a phosphoprotein
-
?
2.7.11.24 additional information substrate specificity eukaryota ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.13 PKC
-
Drosophila melanogaster
2.7.11.13 PKC
-
eukaryota
2.7.11.13 PKC
-
Homo sapiens
2.7.11.13 PKC
-
Saccharomyces cerevisiae
2.7.11.17 Cam-II PK
-
eukaryota
2.7.11.18 MLCK
-
eukaryota
2.7.11.24 receptor-linked ribosomal protein S6
-
eukaryota

Cofactor

EC Number Cofactor Comment Organism Structure
2.7.11.13 ATP
-
Drosophila melanogaster
2.7.11.13 ATP
-
eukaryota
2.7.11.13 ATP
-
Homo sapiens
2.7.11.13 ATP
-
Saccharomyces cerevisiae
2.7.11.17 ATP
-
eukaryota
2.7.11.17 Calmodulin binding required for activity eukaryota
2.7.11.18 ATP
-
eukaryota
2.7.11.19 ATP
-
Mus musculus
2.7.11.19 ATP
-
Homo sapiens
2.7.11.19 ATP
-
Oryctolagus cuniculus
2.7.11.24 ATP
-
eukaryota

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.11.13 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range Drosophila melanogaster
2.7.11.13 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range eukaryota
2.7.11.13 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range Homo sapiens
2.7.11.13 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range Saccharomyces cerevisiae
2.7.11.17 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range eukaryota
2.7.11.18 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range eukaryota
2.7.11.19 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range Mus musculus
2.7.11.19 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range Homo sapiens
2.7.11.19 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range Oryctolagus cuniculus
2.7.11.24 additional information
-
additional information Ki values of the pseudosubstrates in nano- to micromolar range eukaryota

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.17 0.0000333
-
calmodulin antagonist peptide, IC50: 33.3 nM in H2O, 10.6 nM in buffer containing 0.1% w/v Tween 80 eukaryota ARRKWQKTGHAVRAIGRLSS
2.7.11.24 0.01
-
inhibits the insulin receptor tyrosine kinase, IC50 is 0.01 mM eukaryota (hydroxy-2-naphthalenylmethyl)phosphonic acid