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Literature summary for 2.7.11.12 extracted from

  • Valtcheva, N.; Nestorov, P.; Beck, A.; Russwurm, M.; Hillenbrand, M.; Weinmeister, P.; Feil, R.
    The commonly used cGMP-dependent protein kinase type I (cGKI) inhibitor Rp-8-Br-PET-cGMPS can activate cGKI in vitro and in intact cells (2009), J. Biol. Chem., 284, 556-562.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
cGMP
-
Mus musculus
cGMP
-
Bos taurus

Application

Application Comment Organism
additional information data obtained with Rp-8-Br-PET-cGMPS as cGKI inhibitor should be interpreted with caution and not be used as sole evidence to dissect the role of cGKI in signaling processes Mus musculus
additional information data obtained with Rp-8-Br-PET-cGMPS as cGKI inhibitor should be interpreted with caution and not be used as sole evidence to dissect the role of cGKI in signaling processes Bos taurus

Cloned(Commentary)

Cloned (Comment) Organism
cGKIalpha and cGKIbeta are cloned for expression in Sf9 insect cells Bos taurus

Inhibitors

Inhibitors Comment Organism Structure
KT5823
-
Bos taurus
KT5823
-
Mus musculus
Rp-8-Br-PET-cGMPS beta-phenyl-1,N2-etheno-8-bromoguanosine-3',5'-cyclic monophosphorothioate Bos taurus
Rp-8-Br-PET-cGMPS beta-phenyl-1,N2-etheno-8-bromoguanosine-3',5'-cyclic monophosphorothioate Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + a protein Mus musculus
-
ADP + a phosphoprotein
-
?
ATP + a protein Bos taurus
-
ADP + a phosphoprotein
-
?

Organism

Organism UniProt Comment Textmining
Bos taurus
-
-
-
Mus musculus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
by affinity chromatography Bos taurus

Source Tissue

Source Tissue Comment Organism Textmining
aorta
-
Mus musculus
-
vascular smooth muscle cell VSMC Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + a protein
-
Mus musculus ADP + a phosphoprotein
-
?
ATP + a protein
-
Bos taurus ADP + a phosphoprotein
-
?
ATP + GRTGRRNSI-amide assay substrate Bos taurus ADP + phosphorylated GRTGRRNSI-amide
-
?

Synonyms

Synonyms Comment Organism
cGKI isoforms alpha and beta Mus musculus
cGKI isoforms alpha and beta Bos taurus
cGMP-dependent protein kinase type I
-
Mus musculus
cGMP-dependent protein kinase type I
-
Bos taurus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
activity assay Bos taurus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00003
-
Rp-8-Br-PET-cGMPS cGKI alpha Bos taurus
0.00005
-
Rp-8-Br-PET-cGMPS cGKI beta Bos taurus