Histone Deacetylase Hdac Inhibitors In Recent Clinical Trials For Cancer Therapy PDF Download
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Author | : Julia Gajer |
Publisher | : |
Total Pages | : |
Release | : 2010 |
Genre | : |
ISBN | : |
Download Histone Deacetylase (HDAC) Inhibitors in Recent Clinical Trials for Cancer Therapy Book in PDF, ePub and Kindle
Author | : Christiane Pienna Soares |
Publisher | : Frontiers Media SA |
Total Pages | : 260 |
Release | : 2021-06-02 |
Genre | : Science |
ISBN | : 2889668355 |
Download Epigenetic Therapy with Histone Deacetylase Inhibitors: Implications for Cancer Treatment Book in PDF, ePub and Kindle
Author | : Steven Grant |
Publisher | : Academic Press |
Total Pages | : 290 |
Release | : 2012-11 |
Genre | : Business & Economics |
ISBN | : 0123943876 |
Download Histone Deacetylase Inhibitors as Cancer Therapeutics Book in PDF, ePub and Kindle
Provides information on the exciting and fast-moving field of cancer research.
Author | : Shabir Ahmad Ganai |
Publisher | : Springer Nature |
Total Pages | : 266 |
Release | : 2020-11-23 |
Genre | : Medical |
ISBN | : 9811581797 |
Download Histone Deacetylase Inhibitors in Combinatorial Anticancer Therapy Book in PDF, ePub and Kindle
This book reviews the latest developments in the design, synthesis, and molecular mechanism of action of Histone Deacetylase (HDAC) inhibitors in the context of potential cancer therapy. HDAC inhibitors are emerging as promising anticancer drug molecules that promote growth arrest, differentiation and apoptosis of cancer cells with tumor selective toxicity. The book begins with an overview of various epigenetic modifying enzymes that are involved in cancer transition and progression; before exploring the potential of HDACs in cancer treatment. It provides a classification of HDAC inhibitors based on their structural attributes, and addresses HDAC-induced cytotoxicity.. Lastly, it discusses and assesses the rationale behind therapies that combine HDAC inhibitors with other anticancer agents to treat solid tumors. Given its scope, it offers a valuable resource for all researchers, clinicians, and students working in formulation, drug discovery, oncology, and personalized medicine.
Author | : Chang-Shi Chen |
Publisher | : |
Total Pages | : |
Release | : 2006 |
Genre | : Antineoplastic agents |
ISBN | : |
Download Beyond Induction of Histone Acetylation Book in PDF, ePub and Kindle
Abstract: Histone deacetylase (HDAC) is recognized as one of the promising targets for cancer therapy as aberrant transcriptional regulation of the epigenetic system has been linked to tumorigenesis. To date, many HDAC inhibitors have entered clinical trials in light of their high potency in inhibiting tumor cell growth without incurring significant toxicity. Although the effects of HDAC inhibitors on chromatin remodeling and transcriptional regulation are well understood, an increasing body of evidence suggests that modulation of gene expression might not be exclusively responsible for the antineoplastic effects of these agents. In the first part of this study, we demonstrate a novel histone acetylation-independent mechanism by which HDAC inhibitor induces Akt dephosphorylation in U87MG glioblastoma cells by disrupting HDAC-protein phosphatase 1 (PP1) complexes. This selective histone acetylation-independent action of HDAC inhibitors on HDAC-PP1 complexes also represents the first example of modulating specific PP1 interactions by small-molecule agents. The results of the second part of this study present the efficacy of (S)-HDAC-42, a novel HDAC inhibitor synthesized in our laboratory, in prostate cancer cells. We demonstrate that the antitumor effects of (S)-HDAC-42 are attributed to both histone acetylation-dependent and -independent mechanisms by interfering with the activation or expression status of a number of signaling targets. Together, these mechanisms provide a molecular basis to account for the efficacy of (S)-HDAC-42 in suppressing established prostate xenograft tumor growth. The third part of this study reports another transcriptional regulation-independent anticancer effect of HDAC inhibitor; the inhibition of DNA damage repair. We show that pretreatment of the Bax-deficient DU-145 cells with HDAC inhibitors increased Ku70 acetylation, thereby reducing Ku70's DNA end-binding affinity and diminishing the cellular capability to repair DNA damage. The ability of HDAC inhibitors to modify DNA damage repair underlies the viability of their combination with DNA damaging agents as a therapeutic strategy for prostate cancer. This dissertation research characterizes two novel histone acetylation-/transcriptional regulation-independent anticancer effects of HDAC inhibitors. Moreover, we also show that these histone acetylation-dependent and -independent mechanisms underscore the pleiotropic antineoplastic effects of HDAC inhibitors at both epigenetic and cellular levels.
Author | : Eva Sahakian |
Publisher | : Elsevier Inc. Chapters |
Total Pages | : 39 |
Release | : 2013-06-04 |
Genre | : Medical |
ISBN | : 0128059184 |
Download Cancer Immunotherapy Book in PDF, ePub and Kindle
Histone deacetylase inhibitors (HDI) have been largely known for their ability to induce cell cycle arrest and apoptosis of tumor cells, effects that have translated into clinically significant antitumor activity against certain malignancies. In addition, there is now increasing evidence that HDIs are also endowed with immunoregulatory properties. Interestingly, while some reports have highlighted the anti-inflammatory effects of these compounds, others have shown pro-inflammatory effects triggered by HDIs in in vitro and in vivo studies. Known targets for HDIs are histone deacetylases (HDACs), enzymes that are recruited to gene promoters where they regulate transcription through histone modifications. Some HDACs, however, can also deacetylate nonhistone proteins, indicating that the role of HDACs in cell biology goes beyond their initial described effects on histones and encompasses now more complex regulatory functions. This complexity, along with the fact that most of the HDI currently in use are pan-HDI (multiple HDAC targets), might explain the divergent immunoregulatory effects of these compounds. Given this conundrum, in this chapter we have summarized the current understanding of the expression/function of specific HDACs in immune cells, knowledge that is providing important insights into their role in immunobiology and also paving the way for the development of more selective and potentially less toxic epigenetic-based approaches to effectively harness antitumor immune responses.
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Download Lucine Amara Collection Book in PDF, ePub and Kindle
Collection contains clipping, photograph, program and publicity files.
Author | : Tso-Pang Yao |
Publisher | : Springer Science & Business Media |
Total Pages | : 269 |
Release | : 2011-08-31 |
Genre | : Medical |
ISBN | : 3642216315 |
Download Histone Deacetylases: the Biology and Clinical Implication Book in PDF, ePub and Kindle
The book highlights work from many different labs that taught us abnormal HDACs potentially contribute to the development or progression of many human diseases including immune dysfunctions, heart disease, cancer, memory impairment, aging, and metabolic disorders.
Author | : Ramón Cacabelos |
Publisher | : Academic Press |
Total Pages | : 0 |
Release | : 2024-09-01 |
Genre | : Science |
ISBN | : 9780443187223 |
Download Pharmacoepigenetics Book in PDF, ePub and Kindle
Pharmacoepigenetics, Second Edition, Volume Ten in the Translational Epigenetics series, is a comprehensive reference on the role of epigenetics and epigenomics in drug discovery and development. Here, leading international researchers from across academia, clinical settings, and the pharmaceutical industry discuss the influence of epigenetics and epigenomics in human pathology, epigenetic biomarkers for disease prediction, diagnosis, and treatment, current epigenetic drugs, and the application of epigenetic procedures in drug development. Throughout the book, chapter authors offer a balanced and objective discussion of the future of pharmacoepigenetics and its crucial contribution to the growth of precision and personalized medicine. This new edition has been fully revised to address recent advances in epigenetics, from new natural and synthetic compounds with epigenetic effects to the role of epigenetics in the pathogenesis of a growing number of complex diseases, including further cancers, cardiovascular disorders, and brain disorders. Newly identified molecular components in the functional architecture of the epigenetic machinery, as well as practical and relevant pharmacoepigenetics topics related to COVID-19 and other world health challenges are also discussed.
Author | : William Guerrant |
Publisher | : |
Total Pages | : |
Release | : 2012 |
Genre | : Cancer |
ISBN | : |
Download Targeted Histone Deacetylase Inhibition Book in PDF, ePub and Kindle
Histone deacetylase (HDAC) inhibitors (HDACi) have demonstrated a wealth of biological effects, including anti-proliferative, anti-inflammatory, anti-parasitic, and cognition-enhancing activities. The recent FDA approvals of the inhibitors SAHA and FK-228 have validated HDACi clinical use in cutaneous T cell lymphoma, while numerous clinical trials are currently ongoing using HDACi against a variety of disease states. While the future of the HDAC field looks increasingly promising, there are lingering issues hindering broader use. Recent data point to dysregulation of specific HDAC isoforms in many disease states. However, most current HDACi are pan-inhibitors, lacking the specificity to target individual isoforms. Adding to this, there are currently 18 identified HDAC isoforms, and most lack a defined crystal structure, further complicating the task of designing isoform-specific inhibitors. Most importantly, HDACi have demonstrated a lack of efficacy against solid tumors in the clinic, a major obstacle to broader use in cancer therapy. Several of these issues could more fully be addressed through specific targeting of HDACi, and could bring HDACi into wider and more efficacious pharmaceutical use. Targeting the specific tissue or organelle where HDAC dysregulation occurs could confer greater efficacy in vivo. To this end, we have created four classes of compounds: (1) aryltriazolyl HDACi that potently inhibit HDAC activity and prostate cancer cell growth, (2) dual-targeted inhibitors of Topoisomerase II and HDAC and (3) dual-targeted inhibitors of Topoisomerase I and HDAC, both of which have potent inhibition against both target enzymes as well as cancer cell lines, and finally (4) macrocyclic HDACi that potently inhibit the growth of lung cancer cell lines and preferentially target lung tissue in vivo.