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Literature summary for 2.7.11.12 extracted from

  • Schlossmann, J.; Hofmann, F.
    cGMP-dependent protein kinases in drug discovery (2005), Drug Discov. Today, 10, 627-634.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
8-Br-cGMP
-
Mus musculus
8-Br-cGMP activation of cGKIalpha and cGKII, specificity overview Homo sapiens
8-Br-PET-cGMP
-
Mus musculus
8-Br-PET-cGMP activation of cGKIalpha and cGKII, specificity overview Homo sapiens
8-pCPT-CGMP i.e. 8-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphate Mus musculus
8-pCPT-CGMP i.e. 8-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphate, activation of cGKIalpha and cGKII, specificity overview Homo sapiens
Bay412272 YC1 analogue, stimulates the enzyme in a NO-dependent manner, inhibition of phosphodiesterase 5 Mus musculus
Bay412272 YC1 analogue, stimulates the enzyme in a NO-dependent manner, inhibition of phosphodiesterase 5 Homo sapiens
cGMP
-
Mus musculus
cGMP
-
Homo sapiens
cGMP
-
Rattus norvegicus
additional information cGKII is upregulated by aldosterone inducation e.g. via low salt diet, NO induces cGMP production and thus increases enzyme activity, cGK is also activates via increased cGMP level by inhibition of the phosphodiesterase 5 by sildenafil, vardenafil, and taladafil, or by inhibition of Ca2+/calmodulin-specific cGMP-dependent phosphodiesterase 1 Mus musculus
additional information cGKII is upregulated by aldosterone inducation e.g. via low salt diet, NO induces cGMP production and thus increases enzyme activity, cGK is also activates via increased cGMP level by inhibition of the phosphodiesterase 5 by sildenafil, vardenafil, and taladafil, or by inhibition of Ca2+/calmodulin-specific cGMP-dependent phosphodiesterase 1 Homo sapiens
PET-cGMP
-
Mus musculus
PET-cGMP activation of cGKIalpha and cGKII, specificity overview Homo sapiens
YC1 i.e. 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole, hem-dependent activation of cGK, inhibition of phosphodiesterase 5 Mus musculus
YC1 i.e. 3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole, hem-dependent activation of cGK, inhibition of phosphodiesterase 5 Homo sapiens

Application

Application Comment Organism
drug development the enzyme is a target for drug development Homo sapiens
pharmacology enzyme inhibitors are useful in treatment of diverse physiological dysfunctions, overview Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information construction of tissue-specific cGK-knockout mice causing several dysfunction phenotypes, overview Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
KT5823 staurosporine analogue, inhibits in vitro by selective blockage of ATP binding Homo sapiens
KT5823 staurosporine analogue, inhibits in vitro by selective blockage of ATP binding Mus musculus
additional information inhibition by DT-2 fusion peptide of in vitro peptide inhibitor W45 and the membrane translocation signal sequences from HIV tyrosine aminotransferase protein, and DT-3 fusion peptide of W45 and the Drosophila antennapedia homeodomain Homo sapiens
Rp-8-Br-pCPT-cGMPS
-
Homo sapiens
Rp-8-Br-pCPT-cGMPS i.e. Rp-8-bromo-(4-chlorophenylthio)guanosine 3',5'-cyclic monophosphate Mus musculus
Rp-8-Br-PET-cGMPS
-
Homo sapiens
Rp-8-Br-PET-cGMPS
-
Mus musculus

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required for e.g. inhibition of inositol-1,4,5-trisphosphate-dependent Ca2+-release Mus musculus
Ca2+ required for e.g. inhibition of inositol-1,4,5-trisphosphate-dependent Ca2+-release Homo sapiens
Mg2+
-
Mus musculus
Mg2+
-
Homo sapiens
Mg2+
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + big potassium channel BKCa Mus musculus phosphorylation by cGKI leads to activation of the channel, a mechanism leading to Ca2+-dependent smooth muscle relaxation ADP + phosphorylated big potassium channel BKCa
-
?
ATP + big potassium channel BKCa Homo sapiens phosphorylation by cGKI leads to activation of the channel, a mechanism leading to Ca2+-dependent smooth muscle relaxation ADP + phosphorylated big potassium channel BKCa
-
?
ATP + CFTR Rattus norvegicus phosphorylation leads to stimulation of chloride channels ADP + phosphorylated CFTR
-
?
ATP + cysteine-riche protein 2 Mus musculus i.e. CRP2, phosphorylation by cGKI and cGKII ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + cysteine-riche protein 2 Homo sapiens i.e. CRP2, phosphorylation by cGKI and cGKII ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + IRAG Homo sapiens phosphorylation by cGKIbeta mediates the inhibition of inositol-1,4,5-trisphosphate-dependent Ca2+-release, a mechanism leading to smooth muscle relaxation, involved in platelet aggregation ADP + phosphorylated IRAG
-
?
ATP + IRAG Mus musculus phosphorylation by cGKIbeta mediates the inhibition of inositol-1,4,5-trisphosphate-dependent Ca2+-release, one mechanism leading to smooth muscle relaxation, involved in platelet aggregation ADP + phosphorylated IRAG
-
?
ATP + phospholamban Mus musculus phosphorylation leads to stimulation of the sarcoendoplasmic reticulum pump Ca2+-ATPase, i.e. SERCA ADP + phosphorylated phospholamban
-
?
ATP + phospholamban Homo sapiens phosphorylation leads to stimulation of the sarcoendoplasmic reticulum pump Ca2+-ATPase, i.e. SERCA ADP + phosphorylated phospholamban
-
?
ATP + phospholipase Cbeta3 Homo sapiens potentially involved in inhibition of phospholipase C activity ADP + phosphorylated phospholipase Cbeta3
-
?
ATP + Rho Mus musculus phosphorylation leads to inhibition of Rho ADP + phosphorylated rho
-
?
ATP + Rho Homo sapiens phosphorylation leads to inhibition of Rho ADP + phosphorylated rho
-
?
ATP + septin 3 Homo sapiens potentially involved in vesicle trafficking ADP + phosphorylated septin 3
-
?
ATP + TPIalpha Homo sapiens involved in desensitization of TPIalpha signalling ADP + phosphorylated TPIalpha
-
?
ATP + TRPC3 Homo sapiens involved in inhibition of store operated Ca2+ influx ADP + phosphorylated TRPC3
-
?
ATP + vasodilator-stimulated phosphoprotein Mus musculus
-
ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + vasodilator-stimulated phosphoprotein Homo sapiens
-
ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
additional information Mus musculus cGK is a key enzyme in the nitric oxide-cGMP and natriuretic signalling cascades, it modulates smooth muscle relaxation, platelet aggregation, renin release, intestinal secretion, learning amd memory, cGKII is involved in androsterone homeostasis, pleiotropic effets of the enzyme on diverse tissues, overview ?
-
?
additional information Homo sapiens cGK is a key enzyme in the nitric oxide-cGMP and natriuretic signalling cascades, it modulates smooth muscle relaxation, platelet aggregation, renin release, intestinal secretion, learning amd memory, cGKII is involved in androsterone homeostasis, pleiotropic effets of the enzyme on diverse tissues, overview ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
enzyme forms cGKI, in 2 isoforms cGKIalpha and cGKIbeta, and cGKII
-
Mus musculus
-
enzyme forms cGKI, in 2 isoforms cGKIalpha and cGKIbeta, and cGKII
-
Rattus norvegicus
-
enzyme forms cGKI, in 2 isoforms cGKIalpha and cGKIbeta, and cGKII
-

Source Tissue

Source Tissue Comment Organism Textmining
aorta smooth muscle Mus musculus
-
aorta smooth muscle Homo sapiens
-
bladder
-
Mus musculus
-
bladder
-
Homo sapiens
-
blood platelet
-
Mus musculus
-
blood platelet
-
Homo sapiens
-
brain
-
Mus musculus
-
brain
-
Homo sapiens
-
cardiac myocyte
-
Mus musculus
-
cerebellum Purkinje cells Mus musculus
-
cerebellum Purkinje cells Homo sapiens
-
chondrocyte
-
Mus musculus
-
chondrocyte
-
Homo sapiens
-
gastrointestinal tract
-
Mus musculus
-
gastrointestinal tract
-
Homo sapiens
-
heart
-
Mus musculus
-
heart
-
Homo sapiens
-
HEK-293 cell
-
Homo sapiens
-
hippocampus
-
Mus musculus
-
hippocampus
-
Homo sapiens
-
IEC-CF7 cell intestinal cell line Rattus norvegicus
-
intestine
-
Mus musculus
-
intestine
-
Homo sapiens
-
intestine
-
Rattus norvegicus
-
kidney
-
Mus musculus
-
kidney
-
Homo sapiens
-
neuron enteric Mus musculus
-
neuron enteric Homo sapiens
-
penis
-
Mus musculus
-
penis
-
Homo sapiens
-
Purkinje cell
-
Mus musculus
-
Purkinje cell
-
Homo sapiens
-
smooth muscle
-
Mus musculus
-
smooth muscle
-
Homo sapiens
-
zona glomerulosa expression of cGKII Mus musculus
-
zona glomerulosa expression of cGKII Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + big potassium channel BKCa phosphorylation by cGKI leads to activation of the channel, a mechanism leading to Ca2+-dependent smooth muscle relaxation Mus musculus ADP + phosphorylated big potassium channel BKCa
-
?
ATP + big potassium channel BKCa phosphorylation by cGKI leads to activation of the channel, a mechanism leading to Ca2+-dependent smooth muscle relaxation Homo sapiens ADP + phosphorylated big potassium channel BKCa
-
?
ATP + big potassium channel BKCa phosphorylation by cGKI Mus musculus ADP + phosphorylated big potassium channel BKCa
-
?
ATP + big potassium channel BKCa phosphorylation by cGKI Homo sapiens ADP + phosphorylated big potassium channel BKCa
-
?
ATP + CFTR phosphorylation leads to stimulation of chloride channels Rattus norvegicus ADP + phosphorylated CFTR
-
?
ATP + CFTR phosphorylation by cGKI and cGKII Rattus norvegicus ADP + phosphorylated CFTR
-
?
ATP + cysteine-riche protein 2 i.e. CRP2, phosphorylation by cGKI and cGKII Mus musculus ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + cysteine-riche protein 2 i.e. CRP2, phosphorylation by cGKI and cGKII Homo sapiens ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + IRAG phosphorylation by cGKIbeta mediates the inhibition of inositol-1,4,5-trisphosphate-dependent Ca2+-release, a mechanism leading to smooth muscle relaxation, involved in platelet aggregation Homo sapiens ADP + phosphorylated IRAG
-
?
ATP + IRAG phosphorylation by cGKIbeta mediates the inhibition of inositol-1,4,5-trisphosphate-dependent Ca2+-release, one mechanism leading to smooth muscle relaxation, involved in platelet aggregation Mus musculus ADP + phosphorylated IRAG
-
?
ATP + IRAG i.e. inositol-1,4,5-trisphosphate-receptor-associated cGMP kinase substrate, phosphorylation by cGKIbeta Mus musculus ADP + phosphorylated IRAG
-
?
ATP + IRAG i.e. inositol-1,4,5-trisphosphate-receptor-associated cGMP kinase substrate, phosphorylation by cGKIbeta Homo sapiens ADP + phosphorylated IRAG
-
?
ATP + phospholamban
-
Mus musculus ADP + phosphorylated phospholamban
-
?
ATP + phospholamban
-
Homo sapiens ADP + phosphorylated phospholamban
-
?
ATP + phospholamban phosphorylation leads to stimulation of the sarcoendoplasmic reticulum pump Ca2+-ATPase, i.e. SERCA Mus musculus ADP + phosphorylated phospholamban
-
?
ATP + phospholamban phosphorylation leads to stimulation of the sarcoendoplasmic reticulum pump Ca2+-ATPase, i.e. SERCA Homo sapiens ADP + phosphorylated phospholamban
-
?
ATP + phospholipase Cbeta3 potentially involved in inhibition of phospholipase C activity Homo sapiens ADP + phosphorylated phospholipase Cbeta3
-
?
ATP + phospholipase Cbeta3 phosphorylation by cGKIbeta Homo sapiens ADP + phosphorylated phospholipase Cbeta3
-
?
ATP + Rho phosphorylation leads to inhibition of Rho Mus musculus ADP + phosphorylated rho
-
?
ATP + Rho phosphorylation leads to inhibition of Rho Homo sapiens ADP + phosphorylated rho
-
?
ATP + Rho a small GTP-binding protein, cGKI Mus musculus ADP + phosphorylated rho
-
?
ATP + Rho a small GTP-binding protein, cGKI Homo sapiens ADP + phosphorylated rho
-
?
ATP + septin 3 potentially involved in vesicle trafficking Homo sapiens ADP + phosphorylated septin 3
-
?
ATP + septin 3 phosphorylation by cGKIbeta Homo sapiens ADP + phosphorylated septin 3
-
?
ATP + TPIalpha involved in desensitization of TPIalpha signalling Homo sapiens ADP + phosphorylated TPIalpha
-
?
ATP + TPIalpha phosphorylation by cGKIbeta Homo sapiens ADP + phosphorylated TPIalpha
-
?
ATP + TRPC3 involved in inhibition of store operated Ca2+ influx Homo sapiens ADP + phosphorylated TRPC3
-
?
ATP + TRPC3 phosphorylation by cGKIbeta Homo sapiens ADP + phosphorylated TRPC3
-
?
ATP + vasodilator-stimulated phosphoprotein
-
Mus musculus ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + vasodilator-stimulated phosphoprotein
-
Homo sapiens ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + vasodilator-stimulated phosphoprotein i.e. VASP, phosphorylation at Ser239 by cGKI Mus musculus ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
ATP + vasodilator-stimulated phosphoprotein i.e. VASP, phosphorylation at Ser239 by cGKI Homo sapiens ADP + phosphorylated vasodilator-stimulated phosphoprotein
-
?
additional information cGK is a key enzyme in the nitric oxide-cGMP and natriuretic signalling cascades, it modulates smooth muscle relaxation, platelet aggregation, renin release, intestinal secretion, learning amd memory, cGKII is involved in androsterone homeostasis, pleiotropic effets of the enzyme on diverse tissues, overview Mus musculus ?
-
?
additional information cGK is a key enzyme in the nitric oxide-cGMP and natriuretic signalling cascades, it modulates smooth muscle relaxation, platelet aggregation, renin release, intestinal secretion, learning amd memory, cGKII is involved in androsterone homeostasis, pleiotropic effets of the enzyme on diverse tissues, overview Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
CGK
-
Mus musculus
CGK
-
Homo sapiens
CGK
-
Rattus norvegicus
cGMP kinase
-
Mus musculus
cGMP kinase
-
Homo sapiens
cGMP kinase
-
Rattus norvegicus
cyclic guanosine-3',5'-monophoshate-dependent protein kinase
-
Mus musculus
cyclic guanosine-3',5'-monophoshate-dependent protein kinase
-
Homo sapiens
cyclic guanosine-3',5'-monophoshate-dependent protein kinase
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
ATP
-
Mus musculus
ATP
-
Homo sapiens
ATP
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.035
-
Rp-8-Br-PET-cGMPS cGKI Homo sapiens
0.23
-
KT5823 cGKIalpha Homo sapiens
0.23 0.5 Rp-8-Br-pCPT-cGMPS cGKII Homo sapiens
0.5
-
Rp-8-Br-pCPT-cGMPS cGKI Homo sapiens
0.9
-
Rp-8-Br-PET-cGMPS cGKII Homo sapiens