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PDE5A Gene Record

  • Summary
  • Interactions
  • Claims
  • PDE5A 8654 Druggable Genome

    Alternate Names:

    8654
    PHOSPHODIESTERASE 5A
    PDE5A
    CGB-PDE
    CN5A
    PDE5
    603310
    8784
    ENSG00000138735
    OTTHUMG00000132971
    O76074
    PDE5A_HUMAN
    CGMP-SPECIFIC 3',5'-CYCLIC PHOSPHODIESTERASE
    cGMP-binding cGMP-specific phosphodiesterase
    CGMP-SPECIFIC 3',5'-CYCLIC PHOSPHODIESTERASE (EC 3.1.4.17) (CGB-PDE) (CGMP-BINDING CGMP-SPECIFIC PHOSPHODIESTERASE). [SOURCE:UNIPROT/SWISSPROT;ACC:O76074]
    T07663

    Gene Info:

    Human Readable Name DRUGGABLE GENOME
    Uniprot Evidence 1: Evidence at protein level
    Uniprot Status Swiss-Prot
    Interpro Acc IPR002073
    Interpro Type Domain
    Interpro Name 3'5'-cyclic nucleotide phosphodiesterase, catalytic domain
    Interpro Short Name PDEase_catalytic_dom
    Target Main Class Enzymes
    Target Subclass 3.1.4.35
    Target Class Enzymes
    Target Subclass EC:3.1.4.35
    Gene Biotype PROTEIN_CODING
    (7 More Sources)

    Gene Categories: Category Details

    DRUGGABLE GENOME
    ENZYME

    Publications:

    Gur et al., 2008, Novel phosphodiesterase-5 (PDE5) inhibitors in the alleviation of erectile dysfunction due to diabetes and ageing-induced oxidative stress., Expert Opin Investig Drugs
    Kouvelas et al., 2009, PDE5 inhibitors: in vitro and in vivo pharmacological profile., Curr. Pharm. Des.
    Ahn et al., 2009, Increased expression of the nitric oxide synthase gene and protein in corpus cavernosum by repeated dosing of udenafil in a rat model of chemical diabetogenesis., Asian J. Androl.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Zhao et al., 2011, Activity of phosphodiesterase type 5 inhibitors in patients with lower urinary tract symptoms due to benign prostatic hyperplasia., BJU Int.
    Kruuse et al., 2006, Dipyridamole may induce migraine in patients with migraine without aura., Cephalalgia
    Jackson et al., 2007, Characterization of renal ecto-phosphodiesterase., J. Pharmacol. Exp. Ther.
    Kulkarni et al., 2004, Phosphodiesterase 5 enzyme and its inhibitors: update on pharmacological and therapeutical aspects., Methods Find Exp Clin Pharmacol
    Santini et al., 2005, Hemodynamic effects of inhaled nitric oxide and phosphodiesterase inhibitor (dipyridamole) on secondary pulmonary hypertension following heart valve surgery in adults., Int. J. Cardiol.
    Roumeguère et al., 2003, [Erectile dysfunction and phosphodiesterase type 5 inhibitors]., Rev Med Brux
    Zoraghi et al., 2007, Critical amino acids in phosphodiesterase-5 catalytic site that provide for high-affinity interaction with cyclic guanosine monophosphate and inhibitors., Biochemistry
    Curran et al., 2003, Tadalafil., Drugs
    Montorsi et al., 2003, Pharmacological management of erectile dysfunction., BJU Int.
    Eardley et al., 2002, Tadalafil (Cialis) for men with erectile dysfunction., Int. J. Clin. Pract.
    Rotella, 2003, Tadalafil Lilly ICOS., Curr Opin Investig Drugs
    Scheen, 2003, [Medication of the month. Vardenafil (Levitra)]., Rev Med Liege
    Blount et al., 2006, A 46-amino acid segment in phosphodiesterase-5 GAF-B domain provides for high vardenafil potency over sildenafil and tadalafil and is involved in phosphodiesterase-5 dimerization., Mol. Pharmacol.
    Sung et al., 2003, Structure of the catalytic domain of human phosphodiesterase 5 with bound drug molecules., Nature
    Wang et al., 2008, Conformational variations of both phosphodiesterase-5 and inhibitors provide the structural basis for the physiological effects of vardenafil and sildenafil., Mol. Pharmacol.
    Saenz de Tejada et al., 2001, The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil., Int. J. Impot. Res.
    Carrier, 2003, Pharmacology of phosphodiesterase 5 inhibitors., Can J Urol
    Kim et al., 2001, Inhibition of cyclic GMP hydrolysis in human corpus cavernosum smooth muscle cells by vardenafil, a novel, selective phosphodiesterase type 5 inhibitor., Life Sci.
    Rybalkin et al., 2003, PDE5 is converted to an activated state upon cGMP binding to the GAF A domain., EMBO J.
    Corbin et al., 2002, Phosphodiesterase type 5 as a pharmacologic target in erectile dysfunction., Urology
    Wang et al., 1999, [Mode of action of sildenafil]., Zhongguo Yi Xue Ke Xue Yuan Xue Bao
    Kruuse et al., 2003, Migraine can be induced by sildenafil without changes in middle cerebral artery diameter., Brain
    Wang et al., 2006, Multiple conformations of phosphodiesterase-5: implications for enzyme function and drug development., J. Biol. Chem.
    Carson, 2003, Long-term use of sildenafil., Expert Opin Pharmacother
    Gardiner et al., 2005, Hemodynamic effects of phosphodiesterase 5 and angiotensin-converting enzyme inhibition alone or in combination in conscious SHR., J. Pharmacol. Exp. Ther.
    Kedia et al., 2013, Avanafil for the treatment of erectile dysfunction: initial data and clinical key properties., Ther Adv Urol
    Iwata F et al., 2009, Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete., J Nat Prod
  • UDENAFIL   PDE5A

    Interaction Score: 29.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Phosphodiesterase 5A inhibitor
    Direct Interaction yes
    Trial Name udenafil,Zydena

    PMIDs:
    18491987 19860692 19465935 11752352 21054754


    Sources:
    TdgClinicalTrial ChemblInteractions TEND TTD

  • VARDENAFIL   PDE5A

    Interaction Score: 19.53

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name vardenafil HCL,Levitra, Staxyn
    Novel drug target Established target

    PMIDs:
    14626653 16926278 12955149 17979301 17959709 11890515 12625845 11752352 11669467


    Sources:
    TdgClinicalTrial TEND TTD

  • AVANAFIL   PDE5A

    Interaction Score: 13.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name avanafil, TA-1790
    Mechanism of Interaction Phosphodiesterase 5A inhibitor

    PMIDs:
    23372609


    Sources:
    TdgClinicalTrial ChemblInteractions TTD

  • TADALAFIL   PDE5A

    Interaction Score: 11.93

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Phosphodiesterase 5A inhibitor
    Direct Interaction yes
    Trial Name Cialis

    PMIDs:
    12891884 17979301 14498756 11752352 12603396 12074215 12625031


    Sources:
    TdgClinicalTrial ChemblInteractions TEND TTD

  • LORNEIC ACID A   PDE5A

    Interaction Score: 6.51

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    19856955


    Sources:
    DTC

  • SILDENAFIL   PDE5A

    Interaction Score: 5.11

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name Duromist
    Novel drug target Established target
    Trial Name sildenafil citrate,Revatio, Viagra

    PMIDs:
    12554648 17979301 17959709 12414329 12567500 12477710 16735511 11752352 12614192


    Sources:
    TdgClinicalTrial TEND

  • ICARIIN   PDE5A

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • CP-461   PDE5A

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Trial Name OSI-461
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial

  • SILDENAFIL CITRATE   PDE5A

    Interaction Score: 3.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Phosphodiesterase 5A inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CHEMBL460293   PDE5A

    Interaction Score: 3.25

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • VARDENAFIL HYDROCHLORIDE   PDE5A

    Interaction Score: 3.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Phosphodiesterase 5A inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RHUCIN   PDE5A

    Interaction Score: 1.63

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • EXISULIND   PDE5A

    Interaction Score: 1.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • ROLIPRAM   PDE5A

    Interaction Score: 0.65

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • DIPYRIDAMOLE   PDE5A

    Interaction Score: 0.57

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name CRx-102, prednisolone plus dipyridamole,Synavive
    Novel drug target Established target
    Trial Name CRx-150, amoxapine plus dipyridamole

    PMIDs:
    16886928 17308037 15672122 11752352 16080974


    Sources:
    TdgClinicalTrial ChemblInteractions TEND TTD

  • THEOPHYLLINE   PDE5A

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name ADC4022, low-dose inhaled theophylline
    Novel drug target Established target

    PMIDs:
    11752352


    Sources:
    TdgClinicalTrial TEND

  • PENTOXIFYLLINE   PDE5A

    Interaction Score: 0.38

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction 3',5'-cyclic phosphodiesterase inhibitor
    Direct Interaction yes
    Trial Name pentoxifylline, EHT0201

    PMIDs:
    11752352


    Sources:
    TdgClinicalTrial ChemblInteractions TEND

  • ENALAPRIL   PDE5A

    Interaction Score: 0.33

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15452190


    Sources:
    NCI

  • PAPAVERINE   PDE5A

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • Ensembl: ENSG00000138735

    • Version: 101_38

    Alternate Names:
    PDE5A Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • HopkinsGroom: O76074

    • Version: 11-September-2012

    Alternate Names:
    ENSG00000138735 Ensembl Gene Id
    PDE5A Uniprot Gene Name
    O76074 Uniprot Accession

    Gene Info:
    Human Readable Name DRUGGABLE GENOME
    Uniprot Evidence 1: Evidence at protein level
    Uniprot Status Swiss-Prot

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TEND: O76074

    • Version: 01-August-2011

    Alternate Names:
    8654 Entrez Gene Id
    PDE5A_HUMAN Uniprot Id
    ENSG00000138735 Ensembl Gene Id

    Gene Info:
    Target Main Class Enzymes
    Target Subclass 3.1.4.35

    Publications:

  • TdgClinicalTrial: O76074

    • Version: January-2014

    Alternate Names:
    PDE5A Gene Symbol

    Gene Info:
    Target Class Enzymes
    Target Subclass EC:3.1.4.35

    Publications:

  • RussLampel: ENSG00000138735

    • Version: 26-July-2011

    Alternate Names:
    PDE5A Display Id
    ENSG00000138735 Ensembl Gene Id
    CGMP-SPECIFIC 3',5'-CYCLIC PHOSPHODIESTERASE (EC 3.1.4.17) (CGB-PDE) (CGMP-BINDING CGMP-SPECIFIC PHOSPHODIESTERASE). [SOURCE:UNIPROT/SWISSPROT;ACC:O76074] Description

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • NCI: PDE5A

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Gardiner et al., 2005, Hemodynamic effects of phosphodiesterase 5 and angiotensin-converting enzyme inhibition alone or in combination in conscious SHR., J. Pharmacol. Exp. Ther.

  • DTC: PDE5A

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Iwata F et al., 2009, Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete., J Nat Prod

  • HingoraniCasas: ENSG00000138735

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000138735 Gene Symbol
    PDE5A Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • ChemblInteractions: PDE5

    • Version: chembl_23

    Alternate Names:
    PDE5 GENE_SYMBOL
    PDE5A GENE_SYMBOL
    cGMP-specific 3',5'-cyclic phosphodiesterase UNIPROT

    Gene Info:

    Publications:

  • TTD: Phosphodiesterase 5A

    • Version: 2020.06.01

    Alternate Names:
    PDE5A TTD Gene Abbreviation
    T07663 TTD Target ID

    Gene Info:

    Publications:

  • Pharos: PDE5A

    • Version: 01-February-2022

    Alternate Names:
    cGMP-specific 3',5'-cyclic phosphodiesterase Gene Name
    O76074 UniProt ID

    Gene Info:

    Gene Categories:
    ENZYME

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21