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Details on Person UniProt:O76074 PDE5A

Class:IdReferenceGeneProduct:52392
_chainChangeLogchain:1-875 added on Fri February 6 2015
_displayNameUniProt:O76074 PDE5A
_timestamp2024-11-03 20:06:55
chainchain:1-875
checksum9E30C6C182F13388
commentFUNCTION Plays a role in signal transduction by regulating the intracellular concentration of cyclic nucleotides. This phosphodiesterase catalyzes the specific hydrolysis of cGMP to 5'-GMP (PubMed:15489334, PubMed:9714779). Specifically regulates nitric-oxide-generated cGMP (PubMed:15489334).CATALYTIC ACTIVITY 3',5'-cyclic GMP + H2O = GMP + H(+)COFACTOR Binds 1 Zn(2+) ion per subunit. Binds 2 divalent metal cations per subunit: site 1 preferentially binds zinc, while site 2 has a preference for magnesium. Tightly binds zinc.COFACTOR Binds 1 Mg(2+) ions per subunit. Binds 2 divalent metal cations per subunit: site 1 preferentially binds zinc, while site 2 has a preference for magnesium. Binds magnesium less tightly than zinc.ACTIVITY REGULATION Sildenafil (Viagra) is a highly selective and potent inhibitor of PDE5A and is effective in the treatment of penile erectile dysfunction. Also inhibited by zaprinast.PATHWAY Purine metabolism; 3',5'-cyclic GMP degradation; GMP from 3',5'-cyclic GMP: step 1/1.INTERACTION Expressed in aortic smooth muscle cells, heart, placenta, skeletal muscle and pancreas and, to a much lesser extent, in brain, liver and lung.DOMAIN Composed of a C-terminal catalytic domain containing two putative divalent metal sites and an N-terminal regulatory domain which contains two homologous allosteric cGMP-binding regions, A and B.PTM Phosphorylation is regulated by binding of cGMP to the two allosteric sites (By similarity). Phosphorylation by PRKG1 leads to its activation.SIMILARITY Belongs to the cyclic nucleotide phosphodiesterase family.CAUTION Was initially thought to act as a major regulator of cardiac hypertrophy in myocytes and muscle and investigations have been made on selective PDE5A inhibitors that could protect against cardiovascular disease. However, while PDE5A regulates nitric-oxide-generated cGMP, nitric oxide signaling is often depressed by heart disease, limiting its effect. Moreover, clinical trial using PDE5A inhibitors were disappointing.
descriptionrecommendedName: fullName evidence="19"cGMP-specific 3',5'-cyclic phosphodiesterase ecNumber evidence="9 13"3.1.4.35 alternativeName: cGMP-binding cGMP-specific phosphodiesterase shortName: CGB-PDE
geneNamePDE5A
PDE5
identifierO76074
isSequenceChangedFALSE
keyword3D-structure
Allosteric enzyme
Alternative splicing
cGMP
cGMP-binding
Hydrolase
Metal-binding
Nucleotide-binding
Phosphoprotein
Proteomics identification
Reference proteome
Repeat
Zinc
modified[InstanceEdit:9836292] Weiser, Joel, 2023-05-25
[InstanceEdit:9852000] Weiser, Joel, 2023-11-03
[InstanceEdit:9917590] Weiser, Joel, 2024-08-09
[InstanceEdit:9926675] Weiser, Joel, 2024-11-03
namePDE5A
referenceDatabase[ReferenceDatabase:2] UniProt
referenceGene[ReferenceDNASequence:8997903] ENSEMBL:ENSG00000138735 PDE5A [Homo sapiens]
secondaryIdentifierPDE5A_HUMAN
A0AV69
A8K2C4
O75026
O75887
Q86UI0
Q86V66
Q9Y6Z6
sequenceLength875
species[Species:48887] Homo sapiens
(isoformParent)[ReferenceIsoform:145694] UniProt:O76074-2 PDE5A [Homo sapiens]
[ReferenceIsoform:401923] UniProt:O76074-1 PDE5A [Homo sapiens]
(referenceEntity)[EntityWithAccessionedSequence:418508] PDE5A [cytosol] [Homo sapiens]
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