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10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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PDE5A
phosphodiesterase 5A
Chromosome 4 · 4q26
NCBI Gene: 8654Ensembl: ENSG00000138735.16HGNC: HGNC:8784UniProt: G5E9C5
110PubMed Papers
20Diseases
13Drugs
0Pathogenic Variants
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
3',5'-cyclic-GMP phosphodiesterase activityprotein binding3',5'-cyclic-AMP phosphodiesterase activitynegative regulation of cAMP/PKA signal transductioncoronary artery diseaseerectile dysfunctionpulmonary arterial hypertensionbenign prostatic hyperplasia
✦AI Summary

PDE5A encodes phosphodiesterase type 5, a cGMP-specific phosphodiesterase that catalyzes hydrolysis of cyclic GMP to 5'-GMP, thereby regulating intracellular cGMP levels generated by nitric oxide signaling 1. The gene produces three isoforms (PDE5A1, PDE5A2, PDE5A3) from two alternate promoters, with tissue-specific expression patterns 2. PDE5A1 and PDE5A2 are ubiquitously expressed, while PDE5A3 is predominantly found in tissues with substantial smooth muscle 2. Clinically, PDE5A inhibitors (sildenafil, vardenafil, tadalafil) represent the most successful class of phosphodiesterase-selective therapeutics 3. These agents effectively treat erectile dysfunction by increasing penile blood flow during sexual stimulation 45. Beyond erectile dysfunction, PDE5A inhibition shows therapeutic potential in pulmonary arterial hypertension, where sildenafil reduces vascular remodeling and improves hemodynamics 6. Emerging evidence suggests PDE5A upregulation in bipolar disorder basal ganglia contributes to neuroinflammation and disease-like behaviors, which can be reversed by PDE5A inhibitors like tadalafil 7. Additionally, PDE5A is highly expressed in skeletal tissue, and preclinical data support potential therapeutic applications of PDE5A inhibitors in osteoporosis treatment by enhancing the NO-cGMP-PKG osteoanabolic pathway 8.

Sources cited
1
PDE5A catalyzes hydrolysis of cGMP and specifically regulates nitric-oxide-generated cGMP
PMID: 15489334
2
PDE5A gene encodes three isoforms from two alternate promoters with tissue-specific expression patterns
PMID: 11896473
3
PDE5 inhibitors are the most successfully developed isoenzyme-selective PDE inhibitors for therapeutic use
PMID: 16402111
4
Vardenafil, a PDE5 inhibitor, increases blood flow to the penis and restores erectile function
PMID: 12387708
5
Tadalafil, a selective PDE5 inhibitor, is effective for erectile dysfunction in diverse populations including those with diabetes
PMID: 14498756
6
PDE5A is a direct target of miR-30d and its inhibition by sildenafil reduces pulmonary arterial hypertension and vascular remodeling
PMID: 39206778
7
PDE5A is upregulated in bipolar disorder basal ganglia, contributing to neuroinflammation and BD-like behaviors reversible by tadalafil
PMID: 39695100
8
PDE5A is highly expressed in skeletal tissue and inhibition may enhance osteoanabolic signaling for osteoporosis treatment
PMID: 32860248
Disease Associationsⓘ20
coronary artery diseaseOpen Targets
0.66Moderate
erectile dysfunctionOpen Targets
0.61Moderate
pulmonary arterial hypertensionOpen Targets
0.61Moderate
benign prostatic hyperplasiaOpen Targets
0.61Moderate
pulmonary hypertensionOpen Targets
0.59Moderate
strokeOpen Targets
0.55Moderate
ImpotenceOpen Targets
0.54Moderate
hypertensionOpen Targets
0.48Moderate
cardiovascular diseaseOpen Targets
0.44Moderate
heart failureOpen Targets
0.40Weak
fetal growth restrictionOpen Targets
0.38Weak
connective tissue diseaseOpen Targets
0.37Weak
Airway obstructionOpen Targets
0.37Weak
Castleman diseaseOpen Targets
0.37Weak
dysuriaOpen Targets
0.37Weak
intermittent vascular claudicationOpen Targets
0.37Weak
Recurrent thrombophlebitisOpen Targets
0.37Weak
Raynaud diseaseOpen Targets
0.37Weak
heart diseaseOpen Targets
0.37Weak
chronic kidney diseaseOpen Targets
0.36Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets13
AVANAFILApproved
Phosphodiesterase 5A inhibitor
erectile dysfunction
DIPYRIDAMOLEApproved
3',5'-cyclic phosphodiesterase inhibitor
coronary artery disease
GISADENAFILPhase II
Phosphodiesterase 5A inhibitor
Impotence
IBUDILASTApproved
Phosphodiesterase 10A inhibitor
Castleman disease
PENTOXIFYLLINEApproved
Adenosine A2 receptor antagonist
cardiovascular disease
PF-00489791Phase II
Phosphodiesterase 5A inhibitor
chronic obstructive pulmonary disease
PF-03049423Phase II
Phosphodiesterase 5A inhibitor
Ischemic stroke
SILDENAFILApproved
Phosphodiesterase 5A inhibitor
erectile dysfunction
SILDENAFIL CITRATEApproved
Phosphodiesterase 5A inhibitor
erectile dysfunction
TADALAFILApproved
Phosphodiesterase 5A inhibitor
dysuria
UDENAFILApproved
Phosphodiesterase 5A inhibitor
erectile dysfunction
VARDENAFILApproved
Phosphodiesterase 5A inhibitor
erectile dysfunction
VARDENAFIL HYDROCHLORIDEApproved
Phosphodiesterase 5A inhibitor
erectile dysfunction
Related Genes
PRKG1Protein interaction95%GMPSProtein interaction93%ENTPD6Protein interaction91%ITPAProtein interaction90%ADCY3Protein interaction86%GUCY2CProtein interaction85%
Tissue Expression6 tissues
Heart
100%
Lung
83%
Brain
49%
Ovary
30%
Bone Marrow
13%
Liver
9%
Gene Interaction Network
Click a node to explore
PDE5APRKG1GMPSENTPD6ITPAADCY3GUCY2C
PROTEIN STRUCTURE
Preparing viewer…
PDB1TBF · 1.30 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.70LoF Tolerant
pLIⓘ
0.01Tolerant
Observed/Expected LoF0.49 [0.35–0.70]
RankingsWhere PDE5A stands among ~20K protein-coding genes
  • #4,327of 20,598
    Most Researched110 · top quartile
  • #158of 1,025
    FDA-Approved Drug Targets10 · top quartile
  • #5,370of 17,882
    Most Constrained (LOEUF)0.70
Genes detectedPDE5A
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Vardenafil.
PMID: 12387708
Expert Opin Investig Drugs · 2002
1.00
2
Tadalafil.
PMID: 14498756
Drugs · 2003
0.90
3
miR-30d Attenuates Pulmonary Arterial Hypertension via Targeting MTDH and PDE5A and Modulates the Beneficial Effect of Sildenafil.
PMID: 39206778
Adv Sci (Weinh) · 2024
0.80
4
Phosphodiesterase inhibitors.
PMID: 16402111
Br J Pharmacol · 2006
0.70
5
Identification and regulation of human PDE5A gene promoter.
PMID: 11162575
Biochem Biophys Res Commun · 2001
0.60