Dual targeting of Phosphoinositide 3-Kinase (PI3K) and histone deacetylase 6 (HDAC6) in cancer

Phosphoinositide 3-kinases (PI3Ks) and histone deacetylase 6 (HDAC6) have been widely studied as promising therapeutic targets in cancer. Both play key roles in maintaining cellular homeostasis, and their dysregulation is closely linked to oncogenesis. Consequently, several dual PI3K/HDAC6 inhibitors have been developed as potential anticancer agents. This review explores the cellular and molecular functions of PI3K and HDAC6, their involvement in cancer progression, and the structural and pharmacological properties of dual-targeting inhibitors. Additionally, we discuss future perspectives for designing clinically effective dual PI3K/HDAC6 inhibitors.

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Publication Details

Journal
Biochemical Pharmacology
Published
2025-09-21
DOI
https://doi.org/10.1016/j.bcp.2025.117361
Primary Topic
Histone Deacetylase Inhibitors Research
Type
article
Field-Weighted Citation Impact
0.00
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article

Dual targeting of Phosphoinositide 3-Kinase (PI3K) and histone deacetylase 6 (HDAC6) in cancer

Sharifah Aminah Syed Mohamad, Sami Hamdoun, Nafees Ahemad
Biochemical Pharmacology
Histone Deacetylase Inhibitors Research
article

Dual targeting of Phosphoinositide 3-Kinase (PI3K) and histone deacetylase 6 (HDAC6) in cancer

Sharifah Aminah Syed Mohamad, Sami Hamdoun, Nafees Ahemad
article en

Abstract

Phosphoinositide 3-kinases (PI3Ks) and histone deacetylase 6 (HDAC6) have been widely studied as promising therapeutic targets in cancer. Both play key roles in maintaining cellular homeostasis, and their dysregulation is closely linked to oncogenesis. Consequently, several dual PI3K/HDAC6 inhibitors have been developed as potential anticancer agents. This review explores the cellular and molecular functions of PI3K and HDAC6, their involvement in cancer progression, and the structural and pharmacological properties of dual-targeting inhibitors. Additionally, we discuss future perspectives for designing clinically effective dual PI3K/HDAC6 inhibitors.

Biochemical PharmacologyVol. 242(Pt 3)
Monash University Malaysia (MY), UCSI University (MY), Universiti Teknologi MARA (MY)
Openalex Percentile: Top 77%
Histone Deacetylase Inhibitors Research
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