4.6.1.2: guanylate cyclase
This is an abbreviated version!
For detailed information about guanylate cyclase, go to the full flat file.
Word Map on EC 4.6.1.2
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4.6.1.2
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cgmp
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artery
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guanosine
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nitroprusside
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monophosphate
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phosphodiesterase
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methylene
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vasodilation
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endothelium
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cgmp-dependent
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l-name
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l-arginine
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pkg
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tone
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endothelium-dependent
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blocker
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aorta
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acetylcholine
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vasorelaxation
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endothelium-derived
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ng-nitro-l-arginine
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snap
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phenylephrine
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8-br-cgmp
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ng-monomethyl-l-arginine
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endothelium-denuded
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nnos
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nomega-nitro-l-arginine
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apamin
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no-dependent
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zaprinast
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tetraethylammonium
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8-bromo-cgmp
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glibenclamide
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sin-1
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s-nitroso-n-acetylpenicillamine
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no-mediated
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sildenafil
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no-induced
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precontracted
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nitroglycerin
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diagnostics
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trinitrate
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molecular biology
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analysis
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iberiotoxin
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cavernosum
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7-nitroindazole
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no-donors
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pharmacology
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medicine
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phototransduction
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charybdotoxin
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endothelium-intact
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drug development
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nitrergic
- 4.6.1.2
- cgmp
- artery
- guanosine
- nitroprusside
- monophosphate
- phosphodiesterase
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methylene
-
vasodilation
- endothelium
-
cgmp-dependent
-
l-name
- l-arginine
- pkg
-
tone
-
endothelium-dependent
-
blocker
- aorta
- acetylcholine
-
vasorelaxation
-
endothelium-derived
- ng-nitro-l-arginine
- snap
- phenylephrine
- 8-br-cgmp
- ng-monomethyl-l-arginine
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endothelium-denuded
- nnos
- nomega-nitro-l-arginine
-
apamin
-
no-dependent
- zaprinast
- tetraethylammonium
- 8-bromo-cgmp
- glibenclamide
- sin-1
- s-nitroso-n-acetylpenicillamine
-
no-mediated
- sildenafil
-
no-induced
-
precontracted
- nitroglycerin
- diagnostics
- trinitrate
- molecular biology
- analysis
-
iberiotoxin
- cavernosum
- 7-nitroindazole
-
no-donors
- pharmacology
- medicine
-
phototransduction
-
charybdotoxin
-
endothelium-intact
- drug development
-
nitrergic
Reaction
Synonyms
alpha1 sGC, alpha1 soluble guanylyl cyclase, alpha1beta1 guanylyl cyclase, alpha1beta1 sGC, ANF-RGC, ANPRA, ANPRB, atrial natriuretic factor receptor guanylate cyclase, Atrial natriuretic peptide A-type receptor, Atrial natriuretic peptide B-type receptor, atrial natriuretic peptide receptor 2, BERhGC, BR1-GC, brassinosteroid receptor 1, CaRhGC, CNP-sensitive guanyly cyclase, CNP-sensitive guanylyl cyclase, CsGC-YO1, GC-A, GC-A receptor, GC-B, GC-C, GC-D, GC-G, GC1, GC2, GCA, GCC, gcy-18, gcy-23, GCY-35, gcy-8, GTP-pyrophosphate liase cyclizing, GTP-pyrophosphate lyase, guanyl cyclase, guanyl cyclase B, Guanylate cyclase, guanylate cyclase 1, guanylate cyclase 2, Guanylate cyclase 2D, retinal, Guanylate cyclase 2E, Guanylate cyclase 2F, retinal, guanylate cyclase A, guanylate cyclase B, guanylate cyclase C, Guanylate cyclase, olfactory, guanylyl cyclase, guanylyl cyclase A, guanylyl cyclase B, guanylyl cyclase C, guanylyl cyclase C receptor, guanylyl cyclase-A, guanylyl cyclase-A receptor, guanylyl cyclase-C, guanylyl cyclase-D, guanylyl cyclase-G, Gyc-88E, Gyc-89Da, Gyc-89Db, Gyca-99B, Gycb-100B, H-NOX, hSTAR, Intestinal guanylate cyclase, KSGC, L1 H-NOX, L2 H-NOX, membrane bound guanylate cyclase, membrane bound guanylyl cyclase, membrane guanylate cyclase, membrane guanylyl cyclase receptor, membrane-bound GC, membrane-bound guanylate cyclase, membrane-bound guanylyl cyclase, mGc, More, natriuretic peptide-activated guanylate cyclase, nitric oxid sensitive guanylyl cyclase, nitric oxide sensitive guanylyl cyclase, nitric oxide sensitive-guanylyl cyclase, nitric oxide-sensitive guanylate cyclase, nitric-oxide-sensitive guanylyl cyclase, NO receptor, NO receptor soluble guanylyl cyclase, NO sensitive guanylyl cyclase, NO- and haem-independent sGC, NO- and haem-independent soluble guanylate cyclase, NO-GC, NO-GC1, NO-GC2, NO-independent, heme-dependent soluble guanylate cyclase, NO-sensitive GC, NO-sensitive guanylyl cyclase, NO-sGC, NOGC1, NOsGC, NP-GC, NPR A, NPR-A, NPR-B, NPR1, NPR2, ONE-GC, ONE-GC membrane guanylate cyclase, Pac2, Pac3, particulate GC, particulate guanylate cyclase, particulate guanylyl cyclase, PepR1-GC, peptide hormone receptor guanylyl cyclase-C, PGC, photoreceptor guanylyl cyclase, phytosulfokine receptor, PSK receptor, PSKR1, ratGC, receptor guanylyl cyclase, receptor-type guanylyl cyclase, RET-GC1, retGC, RetGC1, RetGC2, retinal guanylate cyclase, retinal guanylyl cyclase, retinal membrane guanylyl cyclase, rGC, rhodopsin-guanylyl cyclase, Rod outer segment membrane guanylate cyclase, rod outer segment membrane guanylate cyclase type 1, ROS-GC, ROS-GC1, ROS-GC2, sGC, sGC alpha2 inhibitory isoform, sGC alpha2 isoform, sGCalpha1, sGCalpha2beta1, sGCbeta1, sGCbeta3, soluble GC, soluble guanylate cyclase, soluble guanylate cyclase alpha1, soluble guanylate cyclase alpha2, soluble guanylyl cyclase, SONO, STA, STA receptor, Tar4 protein
ECTree
4.6.1.2 guanylate cyclaseAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 4.6.1.2 - guanylate cyclase
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
17beta-estradiol
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decreases enzyme activity in immature rats, while the amount of sGC alpha subuit increases, estrogen receptor-dependent effects, overview
1H-[1,2,4] oxadiazole [4,3-a] quinoxalin-1-one
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effectively blocks guanylyl cyclase activity in response to low O2 levels
1H-[1,2,4]-oxadiazole[4,3-a]quinoxalin-1-one
i.e. ODQ, a highly selective sGC inhibitor; i.e. ODQ, a highly selective sGC inhibitor
1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin 1-one
decreases infectivity of promastigotes
1H-[1,2,4]oxadiazolo[4.3a]quinoxalin-1-one
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inhibition of the enzyme is blocked by 8-bromo-cGMP or L-arginine
2'-dADP
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mixture of competitive and noncompetitive inhibition, binding to the substrate site excludes the substrate GTP, whereas binding to the noncompetitive site has no effect on GTP binding, although the resulting complex is catalytically inactive. It binds to the high and low affinity sites with equivalent affinities. BAY 41-2272, which shares an analogous core structure to YC-1, fully inhibits 2'-dADP binding to the low affinity site, whereas the inhibition by YC-1 is incomplete
2'-deoxy-3'-O-(N-methylanthraniloyl)-guanosine 5'-[beta,gamma-imido]triphosphate
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6-anilino-quinoline-5-8-quinone
decreases infectivity of promastigotes
8-aza-3ATP
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inhibition of basal and sodium nitroprusside activated sGC activity
8-bromo-4H-[1,2,4]oxadiazolo[3,4-c][1,4]benzoxazin-1-one
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i.e. NS-2028, a selective sGC inhibitor, 95% inhibition of enzyme activity at 0.01 mM, inhibits cell proliferation
8-[3-(trifluoromethyl)phenyl]-4H-[1,2,4]oxadiazolo[3,4-c]-benzoxazin-1-one
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adenosine 5'-beta,gamma-imido triphosphate
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competitive inhibitor, reduces the Bmax for the binding of guanosine 5'-beta,gamma-methylene triphosphate, is tightly and selectively associated with the high affinity site
adenosine-5'-tetraphosphate
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
ADPbetaS
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
aldosterone
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diminishes GC activity by activating NADPH oxidase in bovine aortic VSMC to increase ROS levels and induce oxidative posttranslational modification of Cys122, a beta1-subunit cysteinyl residue
atrial natriuretic peptide
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elicits GC-A desensitization, can induce decreased GC-A activity in MA-10 Leydig cells, based on mechanisms directly affecting the hormone responsiveness of the receptor. Protein kinase A blocks homologous atrial natriuretic peptide induced desensitization, in which cGMP is generated as second messenger
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BaY 63-2521
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the sGC inhibitor gives apositive effect in severe pulmonary hypertention patients
Ca2+ ionophore A23187
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Ca2+-dependent inhibition of sGC can be achieved with the Ca2+ ionophore A23187 (0.01 mM)
Calmidazolium
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uncompetitive inhibition, time-dependent inhibition at 0.03 mM, pre-treatment of sGC with calmidazolium, followed by filtration, causes an 80% inhibition of sGC activation by nitric oxide and a 23% inhibition of activation by protoporphyrin IX
DNIC-G
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a dinitrosyl iron complex, solutions contain 18fold molar excess of free thiosulfate, inhibition of the NO-stimulated enzyme, inhibited by GSH
DNIC-Y
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a dinitrosyl iron complex, no free thiosulfate in solutions of the binuclear complex DNIC-Y, inhibition of the NO-stimulated enzyme, inhibited by GSH
GDPbetaS
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
Go6976
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competitive inhibitor. Go6976 reduces GTP binding to the catalytic site of isoforms GC-A and GC-B. Inhibition of isoform GC-B is minimal in the absence of ATP and 1 mM ATP increases the inhibition 4fold
guanosine-5'-tetraphosphate
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
guanylyl cyclase activating protein 1
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GCAP1, a Ca2+/Mg2+-binding protein, metal binding in EF-hand 4 has no role in the primary attachment of GCAP1 to the cyclase, it only triggers the activator-to-inhibitor functional switch in GCAP1, differential binding of GCAP1 mutants, e.g. E75Q/E111Q/E155Q or D100N/D102G mutants, to RetGC1 in HEK-293 cells, overview
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H2O2
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diminishes GC activity by activating NADPH oxidase in bovine aortic VSMC to increase ROS levels and induce oxidative posttranslational modification of Cys122, a beta1-subunit cysteinyl residue
HS-142-1
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natriuretic peptide released from the heart with acute heart failure target particulate GC, results in a decrease in UNaV and cGMP excretion together with a reduction in glomerular filtration rate and an increase in distal fractional tubular sodium reabsorption
LY-83583
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inhibits the enzyme and completely blocks at 5 mM high frequency stimuli at 20 Hz/20 s-induced gLTP in superior cervical ganglia isolated from control rats
lysophosphatidic acid
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preincubations for 30 min before assessments of atrial natriuretic peptide-induced cGMP generation reveals inhibitory effects, exerted in a dose-dependent manner, elicits GC-A desensitization, protein kinase A does not block lysophosphatidic acid-induced heterologous desensitization. MEK inhibitor PD 98059 does not protect against the lysophosphatidic acid-mediated decrease in GC-A hormone sensitivity
Mg2+ATPgammaS
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inhibits cyclase activity through a mixed, non-competitive mechanism, only observable under NO stimulation and not under basal conditions
Mg2+GTPgammaS
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inhibits cyclase activity through a mixed, non-competitive mechanism, only observable under NO stimulation and not under basal conditions
ONE-GC 900VGFTTISALSEPIEVVGFLNDL921
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most effective inhibitor, causes ca. 95% inhibition
S-nitrosocysteine
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inhibition of sGC activity by S-nitrosocysteine occurs only in parallel with the loss of cellular glutathione suggesting that loss of sGC activity may occur as a result of the severe depletion of the reduced thiol pool that occurs after exposure of cells to S-nitrosocysteine
sGC alpha1 splice variant
inhibits the enzyme, no co-precipitation of the N1-alpha1 sGC with the beta-subunit
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tetanus toxin
expression of tetanus toxin in the neurons, that express isozyme Gyc-89Da, blocks their synaptic activity; expression of tetanus toxin in the neurons, that express isozyme Gyc-89Db, blocks their synaptic activity
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thrombospondin-1
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thrombospondin-1 is a universal inhibitor of sGC, blocking both hemedependent and heme-independent activation
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XDP
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
XTP
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
1H-[1,2,4]oxadiazolo [4,3,-a]quinoxalin-1-one
i.e. ODQ, in vivo treatment with the sGC inhibitors ODQ does not decrease plasmatic and jejunal cGMP levels, nor does it influence the change in electrical field-induced relaxation; i.e. ODQ, in vivo treatment with the sGC inhibitors ODQ does not decrease plasmatic and jejunal cGMP levels, nor does it influence the change in electrical field-induced relaxation
1H-[1,2,4]oxadiazolo[4,3-a]-quinoxalin-1-one
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guanylyl cyclase inhibitor, completely abrogates chemotactic and chemokinetic cellular movement to both diethylamine/NO and diethylenetriamine/NO exposure
1H-[1,2,4]oxadiazolo[4,3-a]-quinoxalin-1-one
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specific sGC inhibitor, significantly blocks the capsaicin-induced reduction of mechanical threshold to noxious stimulation of the masseter
1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
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i.e. ODQ, inhibits the enzyme, and also inhibits Y-27632- and staurosporine-induced neurite outgrowth and triggered neurite retraction, but in an sGC-independent manner. The NO/sGC/cGMP signaling cascade is not, but the the ERK signaling pathway is critically involved in ODQ-induced neurite remodeling
1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one
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a soluble guanylate cyclase inhibitor, maximal inhibition (70%) at 0.01 mM
1H-[1,2,4]oxadiazolo[4,3a]quinoxalin-1-one
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acute addition to pulmonary artery does not affect phenylephrine responsiveness, but restores the responsiveness in pulmonary artery treated with an NO-donor, overview
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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NS-2028, a soluble guanylyl cyclase inhibitor, complete inhibition at 0.01 mM
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
4H-8-bromo-1,2,4-oxadiazolo(3,4-d)benz(b)(1,4)oxazin-1-one
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i.e. NS-2028, acts via the heme domain
8-oxoguanosine triphosphate
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i.e. oxo8GTP, a potent inhibitor of nitric oxide-stimulated soluble guanylyl cyclase
8-oxoguanosine triphosphate
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i.e. oxo8GTP, a potent competitive inhibitor of nitric oxide-stimulated soluble guanylyl cyclase
ATP
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mechanism involving ATP pre-binding is physiologically relevant to activation of retinal guanylate cyclase, inhibition at high concentrations
ATP
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80% inhibition at 0.1 mM, affects C-type NP 1-53 stimulation of the enzyme, in the presence of Mn2+ inhibition of mastoparan-induced activation of the enzyme
ATP
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allosteric inhibition of basal and sodium nitroprusside activated sGC activity
ATP
inhibits the enzyme by 70% at 1 mM in presence of stoichiometric concentrations of NO
ATP
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in solubilized membranes ATP exerts an inhibitory role on basal and atrial natriuretic peptide 1-28-induced GC activity
Ca2+
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inhibition of both, the basal and NO-stimulated forms of sGC, competitive vs. Mg2+, noncompetitive vs. MgGTP
Ca2+
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modulates the membrane guanylate cyclase transduction machinery by both inhibiting and stimulating it involving the guanylate cyclae, the guanylate cyclase activating protein type 1, S100B, and neurocalcin delta, mechanism, overview
ITP
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basal activity of wild-type enzyme is considerably less sensitive than NO-stimulated wild-type activity
methylene blue
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non-specific sGC inhibitor, significantly blocks the capsaicin-induced reduction of mechanical threshold to noxious stimulation of the masseter
methylene blue
inhibits by oxidation of the enzyme's ferrous heme; inhibits by oxidation of the enzyme's ferrous heme
methylene blue
in vivo treatment with the sGC inhibitor methylene blue does not decrease plasmatic and jejunal cGMP levels, nor does it influence the change in electrical filed stimulation-induced relaxation; in vivo treatment with the sGC inhibitor methylene blue does not decrease plasmatic and jejunal cGMP levels, nor does it influence the change in electrical filed stimulation-induced relaxation
NO
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long acting NO donors pentaerythrityl tetranitrate and isosorbide mononitrate have a significant impact on the regulation of vascular sGC expression and activity, overview
NO
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long acting NO donors pentaerythrityl tetranitrate and isosorbide mononitrate have a significant impact on the regulation of vascular sGC expression and activity, overview
Zn2+
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0.08 mM, 50% inhibition of the intracellular domain of GCC catalytic activity
[1,2,4]-oxadiazolo[4,3-a]quinoxalin-1-one
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i.e. QDC, a selective sGC inhibitor, inhibits cell proliferation
[1,2,4]-oxadiazolo[4,3-a]quinoxalin-1-one
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inhibits the enzyme and the enzyme activating effect of sodium nitroprusside
additional information
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the ATP analogs ATP-Sp-alphaS and ATP-Rp-alphaS are potent inhibitors
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
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additional information
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desensitization of the enzyme to NO and inactivation of soluble guanylate cyclase by stoichiometric S-nitrosation through dinitrosyl iron complexes, which is slowly reversible by GSH, overview
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
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additional information
the ATP analogs ATP-Sp-alphaS and ATP-Rp-alphaS are potent inhibitors
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additional information
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the ATP analogs ATP-Sp-alphaS and ATP-Rp-alphaS are potent inhibitors
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additional information
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heme moiety of sGC has some inhibitory function on sGC activity
-
additional information
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competitive GC-C isozyme inhibition by exogenous 18-residue heat-stable enterotoxins, STa, produced by diarrheagenic bacteria, binding to GC-C by quantifying competitive displacement of [125I]STa from GC-C expressed in membranes, overview
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
-
additional information
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inhibition of the enzyme is involved in inhibition of tumor cell migration in lung
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additional information
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inhibition of soluble guanylyl cyclase requires binding to cell-surface receptor CD47. A thrombospondin-1 C-terminal fragment (E3CaG1) readily inhibits sGC in Jurkat T cells. This inhibition requires an increase in intracellular Ca+ concentration. Addition of angiotensin II also strongly inhibits soluble guanylyl cyclase activity by increasing intracellular Ca+ concentration
-
additional information
sGC is influenced by the light conditions, overview
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additional information
native and recombinant enzyme unaffected by chlorpromazine and trifluoprazine
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additional information
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native and recombinant enzyme unaffected by chlorpromazine and trifluoprazine
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additional information
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competitive GC-C isozyme inhibition by exogenous 18-residue heat-stable enterotoxins, STa, produced by diarrheagenic bacteria, Ki values of 1.5-57.6 nM, binding to GC-C by quantifying competitive displacement of [125I]STa from GC-C expressed in membranes, overview
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
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additional information
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c-Src-dependent phosphorylation of sGC in induced by acetylcholine and inhibits NO-sensitive sGC activity and cGMP production
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additional information
effects of activators and inhibitors on enzyme regulation, overview
-
additional information
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the N-terminal heme-bound regulatory domain of the beta1 subunit of soluble guanylate cyclase inhibits the activity of the alphacatbetacat complex in trans, suggesting a domain-scale mechanism of regulation by NO
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additional information
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phosphorylation at Ser64 of the alpha1 subunit inhibits the enzyme
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additional information
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desensitization of the soluble guanylyl cyclase/cGMP pathway by lipopolysaccharide in rat isolated pulmonary artery but not aorta
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
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additional information
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12-oxo-6,12-dihydroquinazolino[2,3-c][1,4]benzoxazine, 2-bromo-12-oxo-6,12-dihydroquinazolino[2,3-c][1,4]-benzoxazine, and 8-bromo-2,4-dihydro-1H-[1,2,4]triazolo[3,4-c][1,4]-benzoxazin-1-one do not exhibit an inhibitory effect on sGC
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additional information
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effects of activators and inhibitors on enzyme regulation, overview
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