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Related Concept Videos

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors01:28

Treatment for Pulmonary Arterial Hypertension: Phosphodiesterase Inhibitors

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Phosphodiesterase 5 (PDE5) inhibitors are potent enzymes that function to hydrolyze cyclic nucleotides to their corresponding 5' monophosphates. Their unique biochemical properties have been applied in treating Pulmonary Arterial Hypertension (PAH).
Among the PDE5 inhibitors, sildenafil (Revatio) stands out as a competitive and selective inhibitor. It operates by elevating cellular levels of cGMP and augmenting signaling through the cGMP-PKG pathway, promoting vasodilation. Upon oral...
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Transducer Mechanism: Enzyme-Linked Receptors01:27

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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Protein Kinases and Phosphatases02:54

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Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
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Targeted Cancer Therapies02:57

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
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The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
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Related Experiment Video

Updated: Feb 17, 2026

Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
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Phosphodiesterase type 5 and cancers: progress and challenges.

Ines Barone1, Cinzia Giordano2, Daniela Bonofiglio1

  • 1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Arcavacata di Rende, Italy.

Oncotarget
|December 13, 2017
PubMed
Summary

Phosphodiesterase type 5 (PDE5) inhibition shows promise for cancer treatment by restoring cyclic guanosine monophosphate (cGMP) signaling. Further research is needed to confirm its role in cancer patient management.

Keywords:
biomarkerscancerchemopreventionphosphodiesterasetargeted therapy

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Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Cancer is a heterogeneous disease with diverse genetic profiles impacting treatment response.
  • Targeted therapies exploit cancer-specific cellular pathways for treatment.
  • Understanding cancer cell biology and tumor progression guides the development of tailored medical treatments.

Purpose of the Study:

  • To review experimental and clinical evidence on the role of phosphodiesterase type 5 (PDE5) in cancer.
  • To highlight PDE5's potential in the pathogenesis and prevention of various malignancies.
  • To assess the current status of PDE5-targeting drugs as anticancer agents.

Main Methods:

  • Review of experimental studies on PDE5 and cancer.
  • Analysis of clinical evidence regarding PDE5's role in malignancies.
  • Evaluation of data on PDE5 inhibition and its downstream effects on cancer cells.

Main Results:

  • PDE5 inhibition can restore intracellular cyclic guanosine monophosphate (cGMP) signaling.
  • This restoration activates downstream molecules that inhibit cancer cell proliferation, motility, and invasion.
  • Evidence suggests PDE5 plays a role in the pathogenesis and prevention of certain cancers.

Conclusions:

  • Current data are insufficient for definitive conclusions on cancer patient management.
  • PDE5-targeting drugs show potential as anticancer agents.
  • Further clinical investigation is warranted to validate PDE5 inhibitors in cancer therapy.