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Pros and cons of pharmacological manipulation of cGMP-PDEs in the prevention and treatment of breast cancer


Di Iorio, P and Ronci, M and Giuliani, P and Caciagli, F and Ciccarelli, R and Caruso, V and Beggiato, S and Zuccarini, M, Pros and cons of pharmacological manipulation of cGMP-PDEs in the prevention and treatment of breast cancer, International Journal of Molecular Sciences, 23, (1) pp. 1-16. ISSN 1422-0067 (2022) [Substantial Review]

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DOI: doi:10.3390/ijms23010262


The cyclic nucleotides, cAMP and cGMP, are ubiquitous second messengers responsible for translating extracellular signals to intracellular biological responses in both normal and tumor cells. When these signals are aberrant or missing, cells may undergo neoplastic transformation or become resistant to chemotherapy. cGMP-hydrolyzing phosphodiesterases (PDEs) are attracting tremendous interest as drug targets for many diseases, including cancer, where they regulate cell growth, apoptosis and sensitization to radio- and chemotherapy. In breast cancer, PDE5 inhibition is associated with increased intracellular cGMP levels, which is responsible for the phosphorylation of PKG and other downstream molecules involved in cell proliferation or apoptosis. In this review, we provide an overview of the most relevant studies regarding the controversial role of PDE inhib-itors as off-label adjuvants in cancer therapy.

Item Details

Item Type:Substantial Review
Keywords:purinergic system, drug discovery
Research Division:Biomedical and Clinical Sciences
Research Group:Pharmacology and pharmaceutical sciences
Research Field:Pharmaceutical sciences
Objective Division:Health
Objective Group:Clinical health
Objective Field:Treatment of human diseases and conditions
UTAS Author:Caruso, V (Dr Vanni Caruso)
ID Code:148907
Year Published:2022
Web of Science® Times Cited:1
Deposited By:Pharmacy
Deposited On:2022-02-18
Last Modified:2022-02-21

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