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positive regulation of cGMP-mediated signaling

Definition

Target type: biologicalprocess

Any process that increases the rate, frequency or extent of cGMP-mediated signaling. [GOC:BHF, GOC:dph, GOC:tb]

Positive regulation of cGMP-mediated signaling is a complex biological process that involves the activation of signaling pathways mediated by cyclic guanosine monophosphate (cGMP). cGMP is a second messenger molecule that plays a crucial role in various cellular processes, including smooth muscle relaxation, neurotransmission, and phototransduction. The process begins with the activation of guanylate cyclase enzymes, which catalyze the conversion of GTP to cGMP. This activation can be triggered by various stimuli, such as hormones, neurotransmitters, or light. Once cGMP is produced, it binds to and activates downstream effector proteins, such as protein kinases and ion channels. These activated effector proteins initiate a cascade of signaling events that ultimately lead to specific cellular responses. For example, in smooth muscle cells, cGMP activation leads to the relaxation of muscle fibers by activating protein kinase G, which phosphorylates and inactivates myosin light chain kinase. This inactivation prevents myosin from binding to actin, resulting in muscle relaxation. In photoreceptor cells, cGMP activation regulates the flow of ions through ion channels, leading to the transduction of light signals. The process of positive regulation of cGMP-mediated signaling involves a delicate balance between the production and degradation of cGMP. Phosphodiesterases (PDEs) are enzymes that catalyze the breakdown of cGMP, terminating the signaling pathway. The activity of PDEs is regulated by various factors, including intracellular calcium levels and phosphorylation. Dysregulation of cGMP signaling can lead to various pathological conditions, including cardiovascular diseases, neurological disorders, and retinal diseases. Therefore, understanding the intricate mechanisms of positive regulation of cGMP-mediated signaling is essential for developing novel therapeutic strategies for these diseases.'
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Proteins (2)

ProteinDefinitionTaxonomy
Adenosine receptor A2bAn adenosine receptor A2b that is encoded in the genome of human. [PRO:WCB, UniProtKB:P29275]Homo sapiens (human)
Atrial natriuretic peptide receptor 1An atrial natriuretic peptide receptor 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P16066]Homo sapiens (human)

Compounds (107)

CompoundDefinitionClassesRoles
9-ethyladenine
1,3-diethyl-8-phenylxanthine1,3-diethyl-8-phenylxanthine: structure given in first source
1,3-dipropyl-8-cyclopentylxanthineDPCPX : An oxopurine that is 7H-xanthine substituted at positions 1 and 3 by propyl groups and at position 8 by a cyclohexyl group.oxopurineadenosine A1 receptor antagonist;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
1,3-dipropyl-8-(4-sulfophenyl)xanthine1,3-dipropyl-8-(4-sulfophenyl)xanthine: adenosine receptor antagonist
enprofyllineenprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.oxopurineanti-arrhythmia drug;
anti-asthmatic drug;
bronchodilator agent;
non-steroidal anti-inflammatory drug
5-(n,n-hexamethylene)amiloride5-(N,N-hexamethylene)amiloride : A member of the class of pyrazines that is amiloride in which the two amino hydrogens at position N-5 are replaced by a hexamethylene moiety, resulting in the formation of an azepane ring.

5-(N,N-hexamethylene)amiloride: inhibitor of Na+-H+ exchange; has anti-HIV-1 activity
aromatic amine;
azepanes;
guanidines;
monocarboxylic acid amide;
organochlorine compound;
pyrazines
antineoplastic agent;
apoptosis inducer;
odorant receptor antagonist;
sodium channel blocker
7-(2-chloroethyl)theophylline7-(2-chloroethyl)theophylline: adenosine antagonistoxopurine
etofyllineetofylline: etophyllin appeared once in PubMed: Wien Med Wochenschr. 1986 May 15;136(9):213-8 as a combination drug with theophylline (spelt without e, theophllin)oxopurine
8-(4-sulfophenyl)theophylline8-(4-sulfophenyl)theophylline: adenosine antagonist
8-cyclopentyl-1,3-dimethylxanthine8-cyclopentyl-1,3-dimethylxanthine: prolongs epileptic seizures in ratsoxopurine
8-phenyltheophylline8-phenyltheophylline: purinergic P1 receptor antagonist
theophyllinedimethylxanthineadenosine receptor antagonist;
anti-asthmatic drug;
anti-inflammatory agent;
bronchodilator agent;
drug metabolite;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
fungal metabolite;
human blood serum metabolite;
immunomodulator;
muscle relaxant;
vasodilator agent
caffeinepurine alkaloid;
trimethylxanthine
adenosine A2A receptor antagonist;
adenosine receptor antagonist;
adjuvant;
central nervous system stimulant;
diuretic;
EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
environmental contaminant;
food additive;
fungal metabolite;
geroprotector;
human blood serum metabolite;
mouse metabolite;
mutagen;
plant metabolite;
psychotropic drug;
ryanodine receptor agonist;
xenobiotic
cgs 159439-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist

CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors.
aromatic amine;
biaryl;
furans;
organochlorine compound;
primary amino compound;
quinazolines;
triazoloquinazoline
adenosine A1 receptor antagonist;
adenosine A2A receptor antagonist;
antineoplastic agent;
central nervous system stimulant
denbufyllinedenbufylline: structure given in first sourceoxopurine
1-methyl-3-isobutylxanthine1-Methyl-3-isobutylxanthine: A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES

3-isobutyl-1-methylxanthine : An oxopurine that is xanthine which is substituted at positions 1 and 3 by methyl and isobutyl groups, respectively.
3-isobutyl-1-methylxanthine
ns 2028NS 2028: structure in first source
pentoxifyllineoxopurine
8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine8-(4-((2-aminoethyl)aminocarbonylmethyloxy)phenyl)-1,3-dipropylxanthine: adenosine receptor antagonist
6-phenyl-1,3,5-triazine-2,4-diamine6-phenyl-1,3,5-triazine-2,4-diamine: structure in first source
2-chloroadenosine5-chloroformycin A: structure given in first sourcepurine nucleoside
9-benzyladenine
adenosinequinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlitadenosines;
purines D-ribonucleoside
analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
rolofyllinerolofylline: selective antagonist for adenosine receptors; a cardiovascular agentoxopurine
isoguanosinepurine nucleoside
aristeromycinaristeromycin: RN given refers to (1R-(1alpha,2alpha,3beta,5alpha)-isomer
metrifudil
acefyllineacefylline: RN given refers to parent cpdoxopurine
9-methyladenine9-methyladenine : Adenine substituted with a methyl group at position N-9.methyladeninemetabolite
3-methylxanthine3-methyl-7H-xanthine : A 3-methylxanthine tautomer where the imidazole proton is located at the 7-position.

3-methyl-9H-xanthine : A 3-methylxanthine tautomer where the imidazole proton is located at the 9-position.
3-methylxanthinemetabolite
7-methyladenine7-methyladenine : Adenine substituted with a methyl group at position N-7.

7-methyladenine: potential marker for monitoring exposure to methylatingcarcinogens
methyladeninemetabolite
9-(2,3-dihydroxypropyl)adenine, (s)-isomer
1-methylxanthine1-methyl-7H-xanthine : A 1-methylxanthine tautomer where the imidazole proton is located at the 7-position.

1-methylxanthine : A monomethylxanthine having the methyl group located at the 1-position. It is a metabolite of caffeine in humans.

1-methylxanthine: urinary metabolite of caffeine
1-methylxanthinemouse metabolite
8-bromoadenine8-bromoadenine: affects DNA repair
n(6)-benzyladenosineN(6)-benzyladenosine: RN given refers to parent cpd
phenylisopropyladenosinearomatic amine;
benzenes;
hydrocarbyladenosine;
purine nucleoside;
secondary amino compound
adenosine A1 receptor agonist;
neuroprotective agent
5'-n-methylcarboxamideadenosine5'-N-methylcarboxamideadenosine: RN given refers to (beta-D)-isomer
3,7-dimethyl-1-propargylxanthine3,7-dimethyl-1-propargylxanthine: potent & selective in vivo antagonist of adenosine analogs
n(6)-phenyladenosinepurine nucleoside
n-methyladenosineN-methyladenosine: is a inhibitor of cell differentiation

N(6)-methyladenosine : A methyladenosine compound with one methyl group attached to N(6) of the adenine nucleobase.
methyladenosine
bw a1433uBW A1433U: adenosine A3 receptor antagonist; attenuates hypoxia-induced AH interval prolongation; derivative of 1,3-dipropyl-8-phenylxanthine
n(6)-(3-iodobenzyl)-5'-n-methylcarboxamidoadenosine3-iodobenzyl-5'-N-methylcarboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and one of the hydrogens of the exocyclic amino function is substituted by a 3-iodobenzyl group.

N(6)-(3-iodobenzyl)-5'-N-methylcarboxamidoadenosine: structure given in first source; a selective A(3) adenosine receptor agonist
adenosines;
monocarboxylic acid amide;
organoiodine compound
adenosine A3 receptor agonist
2-chloro-n(6)cyclopentyladenosine2-chloro-N(6)cyclopentyladenosine: highly selective agonist at A1 adenosine receptors
8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine8-(4-carboxymethyloxy)phenyl-1,3-dipropylxanthine: used to localize adenosine receptors in the brain
1-propylxanthine1-propylxanthine: structure given in first source
salvinorin asalvinorin A: from the herb, Salvia divinorumorganic heterotricyclic compound;
organooxygen compound
metabolite;
oneirogen
1,3-dipropyl-8-phenylxanthine1,3-dipropyl-8-phenylxanthine: selective antagonist at adenosine A1 receptorsoxopurine
8-(dicyclopropylmethyl)-1,3-dipropylxanthine8-(dicyclopropylmethyl)-1,3-dipropylxanthine: selective A1 adenosine receptor antagonist; structure given in first source
kfm 19KFM 19: a potential cognitive enhancer and a selective adenosine A1 receptor antagonist
2-(1-octynyl)adenosineYT 146: an adenosine receptor agonist; structure given in first source
1-isoamyl-3-isobutylxanthine
tecadenosontecadenoson: an A1 adenosine receptor agonist
1-deazaadenosine1-deazaadenosine: inhibits nucleic acid & protein synthesis; structure given in first source
1,3-dipropyl-7-methylxanthine1,3-dipropyl-7-methylxanthine: structure given in first source
bw a522BW A522: blocks adenosine A3 receptor-mediated hypotensive responses in rats
2-hexynyladenosine-5'-n-ethylcarboxamide2-hexynyladenosine-5'-N-ethylcarboxamide: adenosine receptor agonist
1,3-dipropylxanthine1,3-dipropylxanthine: has high affinity for adenosine receptors; structure given in first source
zm 241385ZM 241385: a high affinity radioligand selective for the A2a adenosine receptordiamino-1,3,5-triazine
sch 58261triazolopyrimidines
l 7340055-chloro-3-phenylthioindole-2-carboxamide: structure given in first source; an inhibitor of HIV-1 reverse transcriptase
regadenosonpurine nucleoside
8-cyclohexylcaffeine
5'-methylthioadenosine5'-methylthioadenosine: structure

5'-S-methyl-5'-thioadenosine : Adenosine with the hydroxy group at C-5' substituted with a methylthio (methylsulfanyl) group.
thioadenosinealgal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
adenosine-5'-(n-ethylcarboxamide)Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.

N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group.
adenosines;
monocarboxylic acid amide
adenosine A1 receptor agonist;
adenosine A2A receptor agonist;
antineoplastic agent;
EC 3.1.4.* (phosphoric diester hydrolase) inhibitor;
vasodilator agent
roflumilastaromatic ether;
benzamides;
chloropyridine;
cyclopropanes;
organofluorine compound
anti-asthmatic drug;
phosphodiesterase IV inhibitor
wr-142,490(+)-(11R,2'S)-erythro-mefloquine : An optically active form of [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol having (+)-(11R,2'S)-erythro-configuration. An antimalarial agent, used in racemic form, which acts as a blood schizonticide; its mechanism of action is unknown.[2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanolantimalarial
1-deaza-2-chloro-n(6)-cyclopentyladenosine1-deaza-2-chloro-N(6)-cyclopentyladenosine: adenosine A(1) receptor agonist
n(6)-cyclopentyladenosine
4-(2-furanyl)-6-methyl-2-sulfanylidene-3,4-dihydro-1H-pyrimidine-5-carboxylic acid ethyl esterpyrimidinecarboxylic acid
2-chloro-n(6)-(3-iodobenzyl)adenosine-5'-n-methyluronamide2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide: structure given in first source
adenosine-5'-(N-propyl)carboxamideadenosine-5'-(N-propyl)carboxamide : A monocarboxylic acid amide that is the propyl amide of adenosine 5'-carboxylic acid.adenosines;
monocarboxylic acid amide
2-(4-(2-carboxyethyl)phenethylamino)-5'-n-ethylcarboxamidoadenosine2-(4-(2-carboxyethyl)phenethylamino)-5'-N-ethylcarboxamidoadenosine: A2 adenosine receptor agonist; structure given in first source

CGS-21680 : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by N-ethylcarboxamido and the hydrogen at position 2 on the adenine is replaced by a 4-(2-carboxyethyl)phenethylamino group.
adenosines;
dicarboxylic acid monoamide;
monocarboxylic acid
adenosine A2A receptor agonist;
anti-inflammatory agent
mrs 15232,3-diethyl-4,5-dipropyl-6-phenylpyridine-3-thiocarboxylate-5-carboxylate: adenosine A3 receptor antagonist
mre 3008-f20MRE 3008-F20: InChIKey: CJRNHKSLHHWUAB-UHFFFAOYSA-N
istradefyllineoxopurine
osip 339391UCS15A: from Streptomyces; structure in first source
psb 1115oxopurine
n-(1-methyl-2-phenylethyl)adenosine, (s)-isomer
8-(3-chlorostyryl)caffeine8-(3-chlorostyryl)caffeine : Caffeine substituted at its 8-position by an (E)-3-chlorostyryl group.

8-(3-chlorostyryl)caffeine: adenosine antagonist
monochlorobenzenes;
trimethylxanthine
adenosine A2A receptor antagonist;
EC 1.4.3.4 (monoamine oxidase) inhibitor
isoalloxazineisoalloxazine: structurebenzo[g]pteridine-2,4-dione
ciproxifanaromatic ketone
bw a1433BW A1433: adenosine receptor antagonist
fk 453FK 453: adenosine A1 receptor antagonist; structure given in first source; a new antihypertensive agent with diuretic action in isolated rabbit aorta; FR113452 is the S-(-) enantiomer of FK 453
kf 17837
mrs 1754oxopurine
cv 18082-phenylaminoadenosine: has coronary & cardiohemodynamic effectspurine nucleoside
binodenoson
n(6)-cyclohexyladenosineN(6)-cyclohexyladenosine: structure given in first source; receptors, purinergic P1 agonist
st 1535
2-(2-(4-chlorophenyl)ethoxy)adenosine2-(2-(4-chlorophenyl)ethoxy)adenosine: a adenosine A2A receptor agonist
2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)-7h-pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidine-5-amine
n(6)-(2,2-diphenylethyl)adenosineN(6)-(2,2-diphenylethyl)adenosine: adenosine receptor agonist; structure given in first source
cgs 24012CGS 24012: adenosine agonist with both high affinity & selectivity for the adenosine A2 receptor
n-cyclopropyl adenosine-5'-carboxamide
sch 442416SCH 442416: an adenosine A2A receptor ligandtriazolopyrimidines
mrs 3558
cvt-68833-ethyl-1-propyl-8-(1-(3-trifluoromethylbenzyl)-1H-pyrazol-4-yl)-3,7-dihydropurine-2,6-dione: structure in first source
tozadenanttozadenant: an adenosine A2A receptor antagonistbenzothiazoles
psb 361-butyl-8-(3-noradamantyl)-3-(3-hydroxypropyl)xanthine: an A1 receptor antagonistoxopurine
bay 60-6583BAY 60-6583 : A member of the class of cyanopyridines that is 6-amino-3,5-dicyano-4-(4-hydroxyphenyl)-2-sulfanylpyridine in which the hydroxy and sulfanyl hydrogens are replaced by cyclopropylmethyl and carboxamidomethyl groups respectively.

BAY 60-6583: structure in first source
aminopyridine;
aromatic ether;
aryl sulfide;
cyanopyridine;
cyclopropanes;
monocarboxylic acid amide
adenosine A2B receptor agonist;
anti-inflammatory agent;
cardioprotective agent
atrial natriuretic factorAtrial Natriuretic Factor: A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.polypeptide
v 20063-(4-amino-3-methylbenzyl)-7-(2-furyl)-3H-(1,2,3)triazolo(4,5-d)pyrimidine-5-amine: antiparkinson agent; structure in first source
psb603PSB603: an adenosine A2B receptor antagonist
natriuretic peptide, brainNatriuretic Peptide, Brain: A PEPTIDE that is secreted by the BRAIN and the HEART ATRIA, stored mainly in cardiac ventricular MYOCARDIUM. It can cause NATRIURESIS; DIURESIS; VASODILATION; and inhibits secretion of RENIN and ALDOSTERONE. It improves heart function. It contains 32 AMINO ACIDS.polypeptide
psb 11
n-benzo(1,3)dioxol-5-yl-2-(5-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1h-purin-8-yl)-1-methyl-1h-pyrazol-3-yloxy)-acetamide
luf 58342-amino-4-(4-hydroxyphenyl)-6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarbonitrile: structure in first source