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Literature summary extracted from

  • Luzi, N.M.; Lyons, C.E.; Peterson, D.L.; Ellis, K.C.
    Kinetics and inhibition studies of the L205R mutant of cAMP-dependent protein kinase involved in Cushings syndrome (2018), FEBS open bio, 8, 606-613 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.7.11.11 expression in Escherichia coli Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
2.7.11.11 L205R the mutation affects the kinetics of both Kemptide and ATP as substrates, decreasing the catalytic efficiency (kcat/KM) for each substrate by 12-fold and 4.5-fold, respectively. The L205R mutation has no effect on the potency of the inhibitor N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H89), but causes a more than 250-fold loss in potency for cAMP-dependent protein kinase inhibitor(5-24) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.11.11 cAMP-dependent protein kinase inhibitor(5-24) peptide substrate-competitive inhibitor Homo sapiens
2.7.11.11 N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide i.e. H89, ATP-competitive inhibitor Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.7.11.11 0.00974
-
 Kemptide 25°C, pH 7.4, wild-type enzyme Homo sapiens
2.7.11.11 0.0169
-
 ATP 25°C, pH 7.4, wild-type enzyme Homo sapiens
2.7.11.11 0.0276
-
 ATP 25°C, pH 7.4, mutant enzyme L205R Homo sapiens
2.7.11.11 0.0609
-
 Kemptide 25°C, pH 7.4, mutant enzyme L205R Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.11.11 ATP + Kemptide Homo sapiens
-
 ADP + phosphorylated Kemptide
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.11.11 Homo sapiens P17612
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.7.11.11
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
2.7.11.11 adrenal adenoma cell of patients with adrenocorticotropic hormone-independent Cushing's syndrome Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.11.11 ATP + Kemptide
-
 Homo sapiens ADP + phosphorylated Kemptide
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
2.7.11.11 2.15
-
 ATP 25°C, pH 7.4, mutant enzyme L205R Homo sapiens
2.7.11.11 6.03
-
 ATP 25°C, pH 7.4, wild-type enzyme Homo sapiens
2.7.11.11 7.5
-
 Kemptide 25°C, pH 7.4, mutant enzyme L205R Homo sapiens
2.7.11.11 14.5
-
 Kemptide 25°C, pH 7.4, wild-type enzyme Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.7.11.11 0.0000037
-
 cAMP-dependent protein kinase inhibitor(5-24) 25°C, pH 7.4, wild-type enzyme Homo sapiens
2.7.11.11 0.0000255
-
 N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide 25°C, pH 7.4, wild-type enzyme Homo sapiens
2.7.11.11 0.000278
-
 N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide 25°C, pH 7.4, mutant enzyme L205R Homo sapiens
2.7.11.11 0.00125
-
 cAMP-dependent protein kinase inhibitor(5-24) 25°C, pH 7.4, mutant enzyme L205R Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.11.11 0.0000074
-
 25°C, pH 7.4, wild-type enzyme Homo sapiens cAMP-dependent protein kinase inhibitor(5-24)
2.7.11.11 0.0000606
-
 25°C, pH 7.4, mutant enzyme L205R Homo sapiens N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide
2.7.11.11 0.0000633
-
 25°C, pH 7.4, wild-type enzyme Homo sapiens N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide
2.7.11.11 0.00187
-
 25°C, pH 7.4, mutant enzyme L205R Homo sapiens cAMP-dependent protein kinase inhibitor(5-24)

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.7.11.11 77.9
-
 ATP 25°C, pH 7.4, mutant enzyme L205R Homo sapiens
2.7.11.11 123.2
-
 Kemptide 25°C, pH 7.4, mutant enzyme L205R Homo sapiens
2.7.11.11 356.8
-
 ATP 25°C, pH 7.4, wild-type enzyme Homo sapiens
2.7.11.11 1488.7
-
 Kemptide 25°C, pH 7.4, wild-type enzyme Homo sapiens