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Literature summary for 2.7.11.11 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
Search for more literature for 2.7.11.11

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Homo sapiens

Protein Variants

Protein Variants Comment Organism
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

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens P17612
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Source Tissue

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

Substrates and Products (Substrate)

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

Turnover Number [1/s]

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

Ki Value [mM]

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

IC50 Value

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

kcat/KM [mM/s]

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