Dual Inhibitors Against Topoisomerases and Histone Deacetylases

Seo, Young Ho

doi:10.15430/jcp.2015.20.2.85

Cited by 29 publications

(26 citation statements)

References 53 publications

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“…Inhibitors of Top1 and Top2, currently developed, also exert their effect against other cancer-related targets [ 202 ]. Dual Top inhibitors, e.g., Top 1/2 [ 203 ], Top2/microtubule [ 204 ], or Top2/histone deacetylase [ 205 ], may exert improved efficacy. Besides, Top1 inhibitors are nonspecific RNA polymerase inhibitors.…”

Section: Future Strategies For Copper Complexes As Top Inhibitors mentioning

confidence: 99%

Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Molinaro

Martoriati

Pélinski

et al. 2020

Cancers

131

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Organometallics, such as copper compounds, are cancer chemotherapeutics used alone or in combination with other drugs. One small group of copper complexes exerts an effective inhibitory action on topoisomerases, which participate in the regulation of DNA topology. Copper complexes inhibitors of topoisomerases 1 and 2 work by different molecular mechanisms, analyzed herein. They allow genesis of DNA breaks after the formation of a ternary complex, or act in a catalytic mode, often display DNA intercalative properties and ROS production, and sometimes display dual effects. These amplified actions have repercussions on the cell cycle checkpoints and death effectors. Copper complexes of topoisomerase inhibitors are analyzed in a broader synthetic view and in the context of cancer cell mutations. Finally, new emerging treatment aspects are depicted to encourage the expansion of this family of highly active anticancer drugs and to expend their use in clinical trials and future cancer therapy.

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Section: Future Strategies For Copper Complexes As Top Inhibitors mentioning

confidence: 99%

Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Molinaro

Martoriati

Pélinski

et al. 2020

Cancers

131

View full text Add to dashboard Cite

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“…The dual inhibitors are often characterized by high molecular weight that may reduce the chance of their drug abilities. Therefore, the safety profiles as well as pharmacokinetic properties need to be thoroughly considered in the design of dual inhibitors [ 7 ].…”

Section: Introductionmentioning

confidence: 99%

Pharmacological and Toxicological Screening of Novel Benzimidazole-Morpholine Derivatives as Dual-Acting Inhibitors

et al. 2017

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The aim of this study was to investigate acetylcholinesterase (AChE), monoamine oxidase A (MAO-A), monoamine oxidase B (MAO-B), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme inhibitory, and antimicrobial activities of a new series of 2-(4-substituted phenyl)-1-[2-(morpholin-4-yl)ethyl]-1H-benzimidazole derivatives, for their possible use as multi-action therapeutic agents. Target compounds (n = 15) were synthesized under microwave irradiation conditions in two steps, and their structures were elucidated by FT-IR, 1H-NMR, 13C-NMR and high resolution mass spectroscopic analyses. Pharmacological screening studies revealed that two of the compounds (2b and 2j) have inhibitory potential on both COX-1 and COX-2 enzymes. In addition, cytotoxic and genotoxic properties of the compounds 2b, 2j and 2m were investigated via the well-known MTT and Ames tests, which revealed that the mentioned compounds are non-cytotoxic and non-genotoxic. As a concise conclusion, two novel compounds were characterized as potential candidates for treatment of frequently encountered inflammatory diseases.

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“…A combination of R-ICE and vorinostat for relapsed or refractory NHL patients also had 70% ORR (Budde et al, 2013). Pre-clinical experiments showed that SAHA and topoisomerase inhibitors surprisingly defeated lymphoma cells, and this might be a new aspect for NHL therapies (Seo, 2015).…”

Section: Application Of Hdacis In B Cell Lymphomamentioning

confidence: 95%

Recent Update of HDAC Inhibitors in Lymphoma

Chen

Sethy

Liou

2020

Front. Cell Dev. Biol.

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Modulating epigenetic modification has been recognized for over a decade as an effective therapeutic approach to cancer and many studies of histone deacetylase (HDAC), one of the best known epigenetic modulators, have been published. HDAC modulates cell proliferation and angiogenesis and plays an essential role in cell growth. Research shows that up-regulated HDACs are present in many cancer types and synthetic or natural HDAC inhibitors have been used to silence overregulated HDACs. Inhibiting HDACs may cause arrest of cell proliferation, angiogenesis reduction and cell apoptosis. Recent studies indicate that HDAC inhibitors can provide a therapeutic effect in various cancers, such as B-cell lymphoma, leukemia, multiple myeloma and some virus-associated cancers. Some evidence has demonstrated that HDAC inhibitors can increase the expression of immune-related molecules leading to accumulation of CD8 + T cells and causing unresponsive tumor cells to be recognized by the immune system, reducing tumor immunity. This may be a solution for the blockade of PD-1. Here, we review the emerging development of HDAC inhibitors in various cancer treatments and reduction of tumor immunity.

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Dual Inhibitors Against Topoisomerases and Histone Deacetylases

Cited by 29 publications

References 53 publications

Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Copper Complexes as Anticancer Agents Targeting Topoisomerases I and II

Pharmacological and Toxicological Screening of Novel Benzimidazole-Morpholine Derivatives as Dual-Acting Inhibitors

Recent Update of HDAC Inhibitors in Lymphoma

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