Histones and lung cancer: are the histone deacetylases a promising therapeutic target?

Petta, Vasiliki; Gkiozos, Ioannis; Strimpakos, Alexios S; Syrigos, Konstantinos

doi:10.1007/s00280-013-2223-9

Cited by 28 publications

(22 citation statements)

References 70 publications

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“…Histone deacetylase inhibitors (HDACi) are currently popular potential anti-cancer therapeutics 20, 21 . While HDAC inhibitors increase acetylation at the majority of acetylation sites, the ability to increase acetylation at specific sites would better enable us to determine the role of those sites in vivo , and possibly lead to new treatment ideas, with fewer adverse effects.…”

Section: Resultsmentioning

confidence: 99%

Changing the Selectivity of p300 by Acetyl-CoA Modulation of Histone Acetylation

et al. 2014

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Determining how histone acetylation is regulated is vital for treating the many diseases associated with its misregulation, including heart disease, neurological disorders, and cancer. We have previously reported that acetyl-CoA levels alter p300 histone acetylation in a site-specific manner in vitro. Here we further investigate how changing acetyl-CoA concentrations alter the histone acetylation pattern by altering p300 specificity. Interestingly, these changes are not a simple global change in acetylation, but rather site specific changes, whereby acetylation at some sites increase while others decrease. We also demonstrate how the p300 inhibitor C646 can pharmacologically alter p300 histone acetylation patterns in vitro and in cells. This study provides insight into the mechanisms regulating p300 residue specificity, a potential means for altering p300 dependent histone acetylation, and an investigation into altering histone acetylation patterns in cells.

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Section: Resultsmentioning

confidence: 99%

Changing the Selectivity of p300 by Acetyl-CoA Modulation of Histone Acetylation

et al. 2014

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“…Vorinostat, also known as suberanilohydroxamic acid (SAHA), on the other hand targets the activity of all 11 known human HDACs. It has been shown to cause cell growth inhibition, differentiation, and apoptosis of different tumor types both in vitro and in vivo [118]. Vorinostat also reduced the expression of human telomerase reverse transcriptase (hTERT) in A549 cells by inducing DNA demethylation at the first exon of hTERT [119].…”

Section: Chromatin Modifiers As Targeted Therapy In Lung Cancermentioning

confidence: 99%

Epigenetics in lung cancer diagnosis and therapy

Mehta

Dobersch

Romero‐Olmedo

et al. 2015

Cancer Metastasis Rev

155

121

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Lung cancer is the leading cause of cancer-related deaths worldwide. The initiation and progression of lung cancer is the result of the interaction between permanent genetic and dynamic epigenetic alterations. DNA methylation is the best studied epigenetic mark in human cancers. Altered DNA methylation in cancer was identified in 1983. Within 30 years of this discovery, DNA methylation inhibitors are used clinically to treat a variety of cancers, highlighting the importance of the epigenetic basis of cancer. In addition, histone modifications, nucleosome remodeling, and micro RNA (miRNA)-mediated gene regulation are also fundamental to tumor genesis. Distinct chromatin alterations occur in all stages of lung cancer, including initiation, growth, and metastasis. Therefore, stage-specific epigenetic changes can be used as powerful and reliable tools for early diagnosis of lung cancer and to monitor patient prognosis. Moreover, since epigenetic changes are dynamic and reversible, chromatin modifiers are promising targets for the development of more effective therapeutic strategies against cancer. This review summarizes the chromatin alterations in lung cancer, focusing on the diagnostic and therapeutic approaches targeting epigenetic modifications that could help to reduce the high case-fatality rate of this dreadful disease.

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“…The balance between acetylation and deacetylation is critical for normal cell function, and loss of protein acetylation has been shown to play a role in cancer initiation and progression [Ropero and Esteller, 2007;New et al 2012]. Indeed, aberrant recruitment of HDACs to gene promoters has been shown to occur in hematological malignancies and HDAC deregulated expression has been reported in tumors of various origins including blood, colon, lung, bladder, pancreas, prostate, breast, cervix, brain, kidney, liver and stomach [Ropero and Esteller, 2007;Van Damme et al 2012;Müller et al 2013;Niegisch et al 2013;Petta et al 2013;Stenzinger et al 2013;West and Johnstone, 2014). Because of their role in tumorigenesis, HDACs have long been considered an attractive therapeutic target.…”

Section: Multiple Myelomamentioning

confidence: 99%

The potential of panobinostat as a treatment option in patients with relapsed and refractory multiple myeloma

Andreu-Vieyra

Berenson

2014

Therapeutic Advances in Hematology

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Panobinostat is an investigational and potent histone deacetylase inhibitor (HDACi) that has shown promise as an antimultiple myeloma agent in the preclinical setting. In this review, we discuss the rationale for the use of panobinostat as a combination therapy for multiple myeloma and provide an overview of recent and ongoing clinical trials testing the safety and efficacy of panobinostat for the treatment of the disease.

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Histones and lung cancer: are the histone deacetylases a promising therapeutic target?

Cited by 28 publications

References 70 publications

Changing the Selectivity of p300 by Acetyl-CoA Modulation of Histone Acetylation

Changing the Selectivity of p300 by Acetyl-CoA Modulation of Histone Acetylation

Epigenetics in lung cancer diagnosis and therapy

The potential of panobinostat as a treatment option in patients with relapsed and refractory multiple myeloma

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