Target type: molecularfunction
Catalysis of the reaction: nucleoside 3',5'-cyclic phosphate + H2O = nucleoside 5'-phosphate; catalytic activity is increased in the presence of cGMP. [GOC:mah]
cGMP-stimulated cyclic-nucleotide phosphodiesterase activity catalyzes the hydrolysis of 3',5'-cyclic GMP to 5'-GMP. This reaction is essential for regulating the levels of cGMP, a second messenger involved in a variety of cellular processes, including smooth muscle relaxation, neurotransmission, and phototransduction. The enzyme is typically activated by binding of cGMP to its regulatory domain, leading to a conformational change that exposes the catalytic site. This activation mechanism allows for rapid and sensitive control of cGMP levels in response to changes in cellular signaling. cGMP-stimulated phosphodiesterase activity is also regulated by other factors, including phosphorylation, protein-protein interactions, and the concentration of calcium ions. By controlling cGMP levels, this enzyme plays a crucial role in maintaining cellular homeostasis and mediating downstream signaling pathways.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| cGMP-dependent 3',5'-cyclic phosphodiesterase | [no definition available] | Bos taurus (cattle) |
| cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A | A cAMP and cAMP-inhibited cGMP 3,5-cyclic phosphodiesterase 10A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9Y233] | Homo sapiens (human) |
| Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A | A dual 3,5-cyclic-AMP and -GMP phosphodiesterase 11A that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q9HCR9] | Homo sapiens (human) |
| cGMP-dependent 3',5'-cyclic phosphodiesterase | A cGMP-dependent 3,5-cyclic phosphodiesterase that is encoded in the genome of human. [PRO:DNx, UniProtKB:O00408] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| my 5445 | MY 5445: potential platelet aggregation inhibitor | pyridazines; ring assembly | |
| theophylline | dimethylxanthine | adenosine 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 | |
| cilostamide | cilostamide: selective inhibitor of cyclic AMP phosphodiesterase & platelet aggregation; structure | quinolines | |
| dipyridamole | dipyridamole : A pyrimidopyrimidine that is 2,2',2'',2'''-(pyrimido[5,4-d]pyrimidine-2,6-diyldinitrilo)tetraethanol substituted by piperidin-1-yl groups at positions 4 and 8 respectively. A vasodilator agent, it inhibits the formation of blood clots. Dipyridamole: A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752) | piperidines; pyrimidopyrimidine; tertiary amino compound; tetrol | adenosine phosphodiesterase inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor; platelet aggregation inhibitor; vasodilator agent |
| 9-(2-hydroxy-3-nonyl)adenine | 9-(2-hydroxy-3-nonyl)adenine: specific inhibitor of adenosine deaminase | ||
| amrinone | amrinone : A 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. Amrinone: A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell. | bipyridines | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| 1-methyl-3-isobutylxanthine | 1-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 | |
| 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one | 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source | chromones; morpholines; organochlorine compound | autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector |
| milrinone | bipyridines; nitrile; pyridone | cardiotonic drug; EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor; platelet aggregation inhibitor; vasodilator agent | |
| papaverine | papaverine : A benzylisoquinoline alkaloid that is isoquinoline substituted by methoxy groups at positions 6 and 7 and a 3,4-dimethoxybenzyl group at position 1. It has been isolated from Papaver somniferum. Papaverine: An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels. | benzylisoquinoline alkaloid; dimethoxybenzene; isoquinolines | antispasmodic drug; vasodilator agent |
| pentoxifylline | oxopurine | ||
| proxyphylline | oxopurine | ||
| pyrimethamine | Maloprim: contains above 2 cpds | aminopyrimidine; monochlorobenzenes | antimalarial; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| 4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone | 4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone: Inhibitor of phosphodiesterases. | methoxybenzenes | |
| rolipram | pyrrolidin-2-ones | antidepressant; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor | |
| sulmazole | sulmazole : An imidazopyridine that is 1H-imidazo[4,5-b]pyridine which is substituted at position 2 by a 2-methoxy-4-(methylsulfinyl)phenyl group. An A1 adenosine receptor antagonist, it was formerly used as a cardiotonic agent. sulmazole: structure given in first source | imidazopyridine; sulfoxide | adenosine A1 receptor antagonist; cardiotonic drug; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| trequinsin | trequinsin: RN given refers to parent cpd; structure given in first source | pyridopyrimidine | |
| zardaverine | zardaverine : A pyridazinone derivative in which pyridazin-3(2H)-one is substituted at C-6 with a 4-(difluoromethoxy)-3-methoxyphenyl group. It is a phosphodiesterase inhibitor, selective for PDE3 and 4. zardaverine: structure given in first source | organofluorine compound; pyridazinone | anti-asthmatic drug; bronchodilator agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; peripheral nervous system drug |
| papaverine hydrochloride | |||
| cinchophen | cinchophen: was heading 1963-94; ACIPHENOCHINOLIUM was see CHINOPHEN 1978-94; use QUINOLINES to search CINCHOPHEN 1966-94 | quinolines | |
| 2-chloroadenosine | 5-chloroformycin A: structure given in first source | purine nucleoside | |
| cycloguanil | cycloguanil : A triazine in which a 1,6-dihydro-1,3,5-triazine ring is substituted at N-1 by a 4-chlorophenyl group, at C-2 and -4 by amino groups and at C-6 by gem-dimethyl groups. A dihydrofolate reductase inhibitor, it is a metabolite of the antimalarial drug proguanil. cycloguanil: the active metabolite of proguanil; antifolate drug; structure in first source | triazines | antifolate; antiinfective agent; antimalarial; antiparasitic agent; antiprotozoal drug; EC 1.5.1.3 (dihydrofolate reductase) inhibitor |
| oxycinchophen | quinolines | ||
| 5-nitroquinoline | |||
| 2-amino-4,6-dimethyl pyrimidine | 2-amino-4,6-dimethyl pyrimidine: structure in first source | aminopyrimidine | |
| cladribine | organochlorine compound; purine 2'-deoxyribonucleoside | antineoplastic agent; immunosuppressive agent | |
| 5-nitroindazole | |||
| enoximone | Enoximone: A selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. It is used in patients with CONGESTIVE HEART FAILURE. | aromatic ketone | |
| imazodan | imazodan: RN & structure given in first source; | ||
| 7-chloro-4-hydroxyquinoline | 7-chloro-4-hydroxyquinoline: structure given in first source | ||
| bufrolin | bufrolin: inhibits the release of histamine; proposed for treatment of hay fever, asthma and skin allergies; minor descriptor (79-86); on line & INDEX MEDICUS search PHENANTHROLINES (79-86); RN given refers to parent cpd | ||
| tadalafil | benzodioxoles; pyrazinopyridoindole | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent | |
| clofarabine | adenosines; organofluorine compound | antimetabolite; antineoplastic agent | |
| 9-(2-hydroxy-3-nonyl)adenine | (2R,3S)-EHNA : EHNA of absolute configuration 2R,3S. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase. | EHNA | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| 9-(2-hydroxy-3-nonyl)adenine | (2S,3R)-EHNA : EHNA of absolute configuration 2S,3R. | EHNA | |
| cilomilast | methoxybenzenes | ||
| rp 73401 | piclamilast : A monocarboxylic acid amide resulting from the formal condensation of the carboxy group of 3-(cyclopentyloxy)-4-methoxybenzoic acid with the primary amino group of 3,5-dichloropyridin-4-amine. piclamilast: an antiasthmatic agent and phosphodiesterase 4 inhibitor; structure in first source | aromatic ether; benzamides; chloropyridine; monocarboxylic acid amide | anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; phosphodiesterase IV inhibitor |
| ly 311727 | LY 311727: a potent & selective inhibitor of human non-pancreatic secretory phospholipase A2; structure given in first source | ||
| 2-amino-4-methyl-3-nitropyridine | |||
| vinpocetine | vinpocetine: whole issue of Arzneim Forsch (23 articles) discuss this drug; Arzneim Forsch 26(10a);1976; RN given refers to parent cpd with unspecified isomeric designation | alkaloid | geroprotector |
| roflumilast | aromatic ether; benzamides; chloropyridine; cyclopropanes; organofluorine compound | anti-asthmatic drug; phosphodiesterase IV inhibitor | |
| 4,5-dihydro-6-(4-(imidazol-1-yl)phenyl)-5-methyl-3(2h)-pyridazinone | 4,5-dihydro-6-(4-(imidazol-1-yl)phenyl)-5-methyl-3(2H)-pyridazinone: RN & structure given in first source | ||
| 1,3-dihydro-7,8-dimethyl-2h-imidazo(4,5-b)quinolin-2-one | 1,3-dihydro-7,8-dimethyl-2H-imidazo(4,5-b)quinolin-2-one: structure given in first source | ||
| N-(1,3-benzodioxol-5-ylmethyl)-6-chloro-4-quinazolinamine | quinazolines | ||
| sch 351591 | SCH 351591: a phosphodiesterase 4 inhibitor; structure in first source SCH-351591 : An aromatic amide resulting from the formal condensation of the carboxy group of 8-methoxy-2-(trifluoromethyl)quinoline-5-carboxylic acid with the primary amino group of 3,5-dichloropyridin-4-amine 1-oxide. It is a potent inhibitor of phosphodiesterase IV (PDE4). | ||
| pf-2545920 | |||
| (2R,3S)-EHNA hydrochloride | (2R,3S)-EHNA hydrochloride : A hydrochloride salt obtained by reaction of (2R,3S)-EHNA with one equivalent of hydrochloric acid. Selective inhibitor of cGMP-stimulated phosphodiesterase (PDE2) (IC50 = 0.8 - 4 mM). Also a potent inhibitor of adenosine deaminase. | hydrochloride | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; EC 3.5.4.4 (adenosine deaminase) inhibitor |
| pf 04217903 | quinolines | ||
| 3-(2,5-dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine | triazoles | ||
| azd7687 | AZD7687: structure in first source | ||
| an2728 | crisaborole : A member of the class of benzoxaboroles that is 5-hydroxy-1,3-dihydro-2,1-benzoxaborole in which the phenolic hydrogen has been replaced by a 4-cyanophenyl group. A phosphodiesterase 4 inhibitor that is used for treatment of mild to moderate atopic dermatitis in children and adults. crisaborole: NSAID, Dermatologic Agent; structure in first source | aromatic ether; benzoxaborole; nitrile | antipsoriatic; non-steroidal anti-inflammatory drug; phosphodiesterase IV inhibitor |
| chf6001 | tanimilast: a phosphodiesterase-4 inhibitor; structure in first source | ||
| sildenafil | sildenafil : A pyrazolo[4,3-d]pyrimidin-7-one having a methyl substituent at the 1-position, a propyl substituent at the 3-position and a 2-ethoxy-5-[(4-methylpiperazin-1-yl)sulfonyl]phenyl group at the 5-position. | piperazines; pyrazolopyrimidine; sulfonamide | EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor; vasodilator agent |
| zaprinast | zaprinast: anaphylaxis inhibitor; structure | triazolopyrimidines | |
| vardenafil | vardenafil : The sulfonamide resulting from formal condensation of the sulfo group of 4-ethoxy-3-(5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one-2-yl)benzenesulfonic acid and the secondary amino group of 4-ethylpiperazine. | imidazotriazine; N-alkylpiperazine; N-sulfonylpiperazine | EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| 2-methyl-4(3h)-quinazolinone | 2-methyl-4(3H)-quinazolinone: from Bacillus cereus; structure given in first source | ||
| 4-hydroxyquinazoline | 4-oxo-3,4-dihydroquinazoline: structure in first source | quinazolines | |
| bl 4162a | anagrelide : A 1,5-dihydroimidazo[2,1-]quinazoline having an oxo substituent at the 2-position and chloro substituents at the 6- and 7-positions. anagrelide: imidazoquinazoline derivative which lowers platelet count probably by inhibiting thrombopoiesis and reduces platelet aggregation; used for thrombocythemia; structure in first source | imidazoquinazoline | anticoagulant; antifibrinolytic drug; cardiovascular drug; platelet aggregation inhibitor |
| bay 60-7550 |