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Natural HDAC Inhibitors for Epigenetic Combating of Cancer Progression deals only with HDAC inhibitors from natural origins including bacteria, fungi, marine organisms and, notably, from diverse plant sources. This book is unique in the sense that it is the only book that discusses wholly and solely HDAC inhibitors of natural origin in the context of cancer chemotherapy. Another peculiar feature of this book is that it debates futuristic nanotechnology approaches for escalating the aqueous solubility, cancer cell uptake, bioavailability and other favourable pharmacological parameters, including the cytotoxicity of natural HDAC inhibitors against cancer cells. The major features of this book encompass General compendium of HDAC inhibitors with deep emphasis on the toxicity issues of synthetic HDAC inhibitors Various groups of natural HDAC inhibitors, their representatives and premier sources Cyclic tetrapeptides of natural origin and their importance as cancer chemotherapeutic agents Hydroxamates and depsipeptides from natural sources and their promising role in cancer therapy Natural flavonoids, their HDAC inhibitory tendency and marvellous anticancer activity Non-flavonoid natural HDAC inhibitors and their pleasing cytotoxic effects towards cancer models Combined therapy involving natural flavonoids with other anticancer molecules for synergistic and additive benefits against cancer models Non-flavonoid HDAC inhibitors and conventional drugs in collaborative mode against aggressive malignancies Nanotechnology-based delivery of natural HDAC inhibitors for greater therapeutic efficacy over traditional combinatorial therapy This book is highly beneficial to university professors and research scholars working on epigenetic therapeutics in general, and natural HDAC inhibitors in particular. This book is equally important to medical oncologists, biochemistry as well as pharmacy candidates and students of master's and undergraduate level with a desire to do a doctorate on HDACs, natural HDAC inhibitors, HDAC inhibitor (natural)-based combinatorial chemotherapy and delivery of these inhibitors selectively to tumour sites through revolutionary nanotechnological tactics.
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.
Epigenetic Regulation in Overcoming Chemoresistance, Volume 19, explains how epigenetic agents can enhance the chemotherapy sensitivity of diverse types of cancers. The book provides a comprehensive delineation and the recent development of the scientific studies on the epigenetic regulation in enhancing chemo-sensitivity. In addition, it discusses several topics such as DNA methyltransferase inhibitors (DNMTi), Histone deacetylases inhibitors (HDACi), Histone lysine demethylases inhibitors (HDMi), Histone lysine methyltransferases inhibitors (HMTi) and drugs regulating the microRNA, long non-coding RNA (lncRNA) or RNA methylation. Finally, recent and future developments of the field of epigenetic regulation are explored. This is a valuable resource for cancer researchers, clinicians, graduate students and several members of biomedical field who are interested in learning about epigenetic regulation methods to reverse chemo-resistance in cancers. Presents detailed diagrams of the mechanisms of epigenetic regulation for easy consult Encompasses multiple clinical trial summary diagrams to help readers quickly and clearly get information from clinical trials Provides future perspectives in each section to inspire readers to use epigenetic regulation to overcome chemo-resistance
It is evident that epigenetics plays an important role in gene regulation. Consequently, any disruption in epigenetic memory will manifest into gene expression and lead to long-established transformation events. Covalent modification of histone is one of the epigenetic regulation mechanisms, and includes acetylation, methylation, phosphorylation, and ubiquitylation among others. Combination of two or more of these modifications acts like a sensor for gene expression or gene repression through highly condensed or uncondensed chromatin structures. The cancer epigenome is specifically marked with global DNA methylation and histone alteration patterns. The gene regulation is controlled by the opposing activities of histone acetyltransferases (HATs) and histone deacetylases (HDACs). Acetylation through HATs results in expansion of chromatin, and thus increases the accessibility of transcription factors to DNA. On the other hand, the deacetylation with HDACs leads to very condensed chromatin structures and consequently, to transcription repression. Owing to their specificity for cancer cells, HDAC inhibitors have now become a powerful target in anticancer drug development. The pharmacophore of HDAC inhibitors consists of a zinc-binding group, a linker and a capping group. These drugs exert their effect on cancer cells by arresting them in G1 or G2-M phases of the cell cycle, or by induction of differentiation and apoptosis. They can also inhibit angiogenesis and metastasis and regulate the host immune response. Generally, HDACs can be classified into four different classes (class I, II, III, and IV). It is well established that most HDAC inhibitors in clinical use lack specificity. It is believed that variations in the nature of the capping group can lead to variations in HDAC inhibitory activity and isoform selectivity. Our group has successfully developed a new class of HDAC inhibitors incorporating an imidazole ketone moiety as the capping group. Cytotoxicity studies of these molecules have shown promising activity. Efforts are underway in our laboratory to modulate the activity and selectivity of these compounds by changing the capping group. Guanidines have been reported to possess a wide range of biological activity. The biochemical and biophysical properties of guanidine are partly attributed to their specific hydrogen bonding, Y aromaticity, and pi-stacking properties. A molecule with such properties is able to bind to carboxylates, phosphates and metals. In this study, several HDAC inhibitors with imidazole ketone metal-binding group and guanidine moieties as the capping group were designed for synthesis and methods for making versatile cyclic guanidine molecules to be used in the synthesis of HDAC inhibitors were developed. In addition, two HDAC inhibitors incorporating guanidine moieties were synthesized. One of the analogues showed potent cytotoxic properties in the NCI 60 cell line assay with a mean growth inhibition of 64.5% and GI50 values in the low micro molar range against some cell lines. The cytotoxic activity of the compound was confirmed in studies performed in the laboratory of Dr. William Taylor of the Biological Sciences Department. The other compound did not show activity in studies carried out in Dr. Taylor's lab and is yet to be tested at NCI for its cytotoxic activity. The incorporation of other guanidine moieties in to target molecules proved problematic, probably due to poor nucleophilicity of their amine groups. However, synthesis of these target molecules using different reaction conditions and changing synthetic design is currently in progress.
This open access textbook leads the reader from basic concepts of chromatin structure and function and RNA mechanisms to the understanding of epigenetics, imprinting, regeneration and reprogramming. The textbook treats epigenetic phenomena in animals, as well as plants. Written by four internationally known experts and senior lecturers in this field, it provides a valuable tool for Master- and PhD- students who need to comprehend the principles of epigenetics, or wish to gain a deeper knowledge in this field. After reading this book, the student will: Have an understanding of the basic toolbox of epigenetic regulation Know how genetic and epigenetic information layers are interconnected Be able to explain complex epigenetic phenomena by understanding the structures and principles of the underlying molecular mechanisms Understand how misregulated epigenetic mechanisms can lead to disease
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.
The growing knowledge about disturbances of epigenetic gene regulation in hematopoietic stem cell disorders is now being translated into treatment approaches that target the epigenetic defects pharmacologically. This book first presents the latest evidence regarding the epigenetic regulation of hematopoietic stem cell differentiation and hemoglobin production. The significance of DNA methylation abnormalities in hematopoietic disorders and of epigenetic disturbances in lung cancer and other solid tumors is then discussed. A major part of the book, however, relates specifically to the translation of basic research and drug development to clinical applications, and in this context both present and future clinical strategies are considered. Individual chapters are devoted to the use of DNA hypomethylating agents and chromatin-modifying agents, and the treatment of hematologic malignancies and solid tumors by means of epigenetic agents is discussed in detail.
This multivolume reference work addresses the fact that the well being of humankind is predicated not only on individuals receiving adequate nutrition but also on their genetic makeup. The work includes more than 100 chapters organized in the following major sections: Introduction and Overview; Epigenetics of Organs and Diseases in Relation to Diet and Nutrition; Detailed Processes in Epigenetics of Diet and Nutrition; Modulating Epigenetics with Diet and Nutrition; and Practical Techniques. While it is well known that genes may encode proteins responsible for structural and dynamic components, there is an increasing body of evidence to suggest that nutrition itself may alter the way in which genes are expressed via the process of epigenetics. This is where chemically imposed alteration in the DNA sequence occurs or where the functional expression of DNA is modulated. This may include changes in DNA methylation, non-coding RNA, chromatin, histone acetylation or methylation, and genomic imprinting. Knowledge regarding the number of dietary components that impact on epigenetic processes is increasing almost daily. Marshalling all the information on the complex relationships between diet, nutrition, and epigenetic processes is somewhat difficult due to the wide myriad of material. It is for this reason that the present work has been compiled.
This book is a printed edition of the Special Issue "Natural Products for Cancer Prevention and Therapy" that was published in Nutrients