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Histone Deacetylase Inhibitors as Multitarget-Directed Epi-Drugs in Blocking PI3K Oncogenic Signaling: A Polypharmacology Approach

Department of Pharmaceutical Science, College of Pharmacy and Health Sciences, Texas Southern University, 3100 Cleburne St., Houston, TX 77004, USA
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Int. J. Mol. Sci. 2020, 21(21), 8198; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218198
Received: 20 September 2020 / Revised: 29 October 2020 / Accepted: 29 October 2020 / Published: 2 November 2020
(This article belongs to the Special Issue Phosphoinositides and Downstream Signalling Molecules)
Genetic mutations and aberrant epigenetic alterations are the triggers for carcinogenesis. The emergence of the drugs targeting epigenetic aberrations has provided a better outlook for cancer treatment. Histone deacetylases (HDACs) are epigenetic modifiers playing critical roles in numerous key biological functions. Inappropriate expression of HDACs and dysregulation of PI3K signaling pathway are common aberrations observed in human diseases, particularly in cancers. Histone deacetylase inhibitors (HDACIs) are a class of epigenetic small-molecular therapeutics exhibiting promising applications in the treatment of hematological and solid malignancies, and in non-neoplastic diseases. Although HDACIs as single agents exhibit synergy by inhibiting HDAC and the PI3K pathway, resistance to HDACIs is frequently encountered due to activation of compensatory survival pathway. Targeted simultaneous inhibition of both HDACs and PI3Ks with their respective inhibitors in combination displayed synergistic therapeutic efficacy and encouraged the development of a single HDAC-PI3K hybrid molecule via polypharmacology strategy. This review provides an overview of HDACs and the evolution of HDACs-based epigenetic therapeutic approaches targeting the PI3K pathway. View Full-Text
Keywords: epigenetics; histone deacetylase; histone deacetylase inhibitors; phosphatidylinositol kinase; HDAC-PI3K hybrid molecule; CUDC-907 epigenetics; histone deacetylase; histone deacetylase inhibitors; phosphatidylinositol kinase; HDAC-PI3K hybrid molecule; CUDC-907
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MDPI and ACS Style

Ranganna, K.; Selvam, C.; Shivachar, A.; Yousefipour, Z. Histone Deacetylase Inhibitors as Multitarget-Directed Epi-Drugs in Blocking PI3K Oncogenic Signaling: A Polypharmacology Approach. Int. J. Mol. Sci. 2020, 21, 8198. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218198

AMA Style

Ranganna K, Selvam C, Shivachar A, Yousefipour Z. Histone Deacetylase Inhibitors as Multitarget-Directed Epi-Drugs in Blocking PI3K Oncogenic Signaling: A Polypharmacology Approach. International Journal of Molecular Sciences. 2020; 21(21):8198. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218198

Chicago/Turabian Style

Ranganna, Kasturi; Selvam, Chelliah; Shivachar, Amruthesh; Yousefipour, Zivar. 2020. "Histone Deacetylase Inhibitors as Multitarget-Directed Epi-Drugs in Blocking PI3K Oncogenic Signaling: A Polypharmacology Approach" Int. J. Mol. Sci. 21, no. 21: 8198. https://0-doi-org.brum.beds.ac.uk/10.3390/ijms21218198

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