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 | 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 | Comment | Organism |
---|---|---|
additional information | construction of tissue-specific cGK-knockout mice causing several dysfunction phenotypes, overview | Mus musculus |
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 | 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 | 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 | 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 | 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 | 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 | 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 | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Mus musculus | |
ATP | - |
Homo sapiens | |
ATP | - |
Rattus norvegicus |
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 |