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Literature summary extracted from

  • Akita, S.; Umezawa, N.; Kato, N.; Higuchi, T.
    Array-based fluorescence assay for serine/threonine kinases using specific chemical reaction (2008), Bioorg. Med. Chem., 16, 7788-7794.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.1 staurosporine
-
 Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.1 Bos taurus
-
-
-
2.7.11.1 Homo sapiens P31749
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.1 ATP + Ac-LRRASLG an efficient fluorescence assay for serine/threonine kinases using a peptide array is developed. Assay is based on chemical reactions specific to phosphoserine and phosphothreonine residues, that is, base-mediated beta-elimination of the phosphate group and subsequent Michael addition of a thiol-containing fluorescent reagent. This procedure enables the covalent introduction of a fluorescent moiety into the phosphorylated peptide. Novel fluorescent reagents are designed for this purpose and synthesized. As a model peptide, a well-known PKA consensus sequence Kemptide 49 is chosen Bos taurus ADP + Ac-LRRApSLG
-
 ?
2.7.11.1 ATP + Ac-RPRAASF an efficient fluorescence assay for serine/threonine kinases using a peptide array is developed. Assay is based on chemical reactions specific to phosphoserine and phosphothreonine residues, that is, base-mediated beta-elimination of the phosphate group and subsequent Michael addition of a thiol-containing fluorescent reagent. This procedure enables the covalent introduction of a fluorescent moiety into the phosphorylated peptide. Novel fluorescent reagents are designed for this purpose and synthesized Homo sapiens ADP + Ac-Ac-RPRAApSF
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.11.1 Akt-1
-
 Homo sapiens
2.7.11.1 PKA
-
 Bos taurus
2.7.11.1 protein kinase A
-
 Bos taurus
2.7.11.1 serine-threonine kinase
-
 Bos taurus
2.7.11.1 serine-threonine kinase
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.7.11.1 30
-
 assay at Homo sapiens
2.7.11.1 37
-
 assay at Bos taurus

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.7.11.1 7.4
-
 assay at Bos taurus
2.7.11.1 7.5
-
 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.11.1 0.00025
-
 staurosporine
-
 Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.1 0.002
-
-
 Bos taurus staurosporine