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Updated: May 9, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Histone deacetylase inhibitors and epigenetic modifications as a novel strategy in renal cell carcinoma
Swathi Ramakrishnan1, Roberto Pili
1Genitourinary Program and Department of Cancer Pathology and Prevention, Roswell Park Cancer Institute, Buffalo, NY 14263, USA.
Abstract:
Recent investigations of renal cell carcinoma (RCC) have revealed several epigenetic modifications, as well as alterations in the genes and enzymes that regulate these changes. Preclinical models have revealed that histone gene modifiers and epigenetic alterations may play a critical role in RCC tumorigenesis. Specific changes in DNA methylation and mutations of histone modifiers have been identified and may be associated with an aggressive phenotype. In addition, the potential of reversing the effects of these enzymes and hence reversing the cellular epigenetic landscape to a "normal phenotype" have led to an increasing interest in developing targeted chromatin remodeling agents. However, the translation of the understanding of these changes to the clinic for the treatment of RCC has posed significant challenges, partly due to tumor heterogeneity. This review describes the aberrant histone and DNA alterations recently reported in RCC and highlights the potential targeted chromatin remodeling therapies in the management of this disease.
Insights
Epigenetic alterations in histone and DNA are key in renal cell carcinoma (RCC) development and progression. Targeted chromatin remodeling therapies show promise for treating RCC, despite clinical translation challenges.
Area of Science:
- Oncology
- Epigenetics
- Molecular Biology
Background:
- Renal cell carcinoma (RCC) exhibits significant epigenetic modifications, including DNA methylation changes and histone modifier gene alterations.
- These epigenetic changes are implicated in RCC tumorigenesis and may correlate with an aggressive disease phenotype.
- Tumor heterogeneity presents a challenge for translating these findings into effective clinical treatments for RCC.
Purpose of the Study:
- To review recent findings on aberrant histone and DNA alterations in RCC.
- To highlight the potential of targeted chromatin remodeling therapies for managing RCC.
- To discuss the challenges in translating epigenetic insights into clinical practice for RCC.
Main Methods:
- Literature review of recent investigations into epigenetic modifications in RCC.
- Analysis of preclinical models and identified genetic/enzymatic alterations.
- Examination of identified DNA methylation changes and histone modifier mutations.
Main Results:
- Aberrant histone and DNA alterations are frequently reported in RCC.
- Specific epigenetic changes are associated with a more aggressive RCC phenotype.
- Targeted chromatin remodeling agents are under investigation for their therapeutic potential.
Conclusions:
- Epigenetic dysregulation is a critical factor in RCC pathogenesis.
- Targeted chromatin remodeling therapies offer a promising avenue for RCC treatment.
- Overcoming tumor heterogeneity is crucial for successful clinical application of these therapies.
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