Special issue: Deregulated transcription factors in the cancer therapeutic challenges: An update on cancer stemness features

Khan, Abdul Quaiyoom

doi:10.1016/j.semcancer.2023.08.004

Cited by 2 publications

(1 citation statement)

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“…Deregulated epigenetics is one of the major hallmarks of cancer. It refers to altered phenotypes which are inherited resulting from alteration in the gene expression while keeping the genetic sequence intact [1]. Exogenous influences and altered environmental conditions can change epigenetic signatures and may give a hint about the origin of different malignancies or neurological disorders [2, 3].…”

Section: Introduction 11 Epigeneticsmentioning

confidence: 99%

Advances in non-Hydroxamate based Histone Deacetylase Inhibitors as Anticancer Agents

Wafik,

Jaballah,

Serya

et al. 2024

Archives of Pharmaceutical Sciences Ain Shams University

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The carcinogenesis process includes several epigenetic modifications that mainly target the silencing of tumor suppressor genes (TS genes) including ribonucleic acid (RNA) editing, deoxyribonucleic acid (DNA) hypermethylation and histone modification, either by methylation and demethylation, or acetylation and deacetylation. Histone deacetylation is one of the most important epigenetic modifications responsible for cancer development, and thereby, the design of new selective histone deacetylase inhibitors (HDACIs) is a promising chemotherapeutic target. Up to this time, all HDACIs approved are hydroxamic acid based. Yet, hydroxamic acids often show several drawbacks upon administration, such as poor pharmacokinetic properties, poor selectivity, and multiple toxicities. That's why the urge of emersion of a new category of compounds was crucial. Thereby, nonhydroxamate based compounds attracted widespread attention by being a part of several biologically active compounds as a safer alternative for hydroxamate based ones. In this mini-review, we aim to focus on several nonhydroxamate based HDACIs, specifically those used as anticancer agents, and the concept behind their development.

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Section: Introduction 11 Epigeneticsmentioning

confidence: 99%