This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by…mehr
This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification.
This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
Antonello Mai is a Full Professor of Medicinal Chemistry at the Faculty of Pharmacy and Medicine, Sapienza University of Rome, since 2011. He completed his Pharmacy degree in 1984, and his PhD in Medicinal Chemistry and Pharmaceutical Sciences in 1992, both at Sapienza. In 1998 he was appointed as Associate Professor of Medicinal Chemistry at Sapienza's Faculty of Pharmacy. From 2012 to 2018 he was the Coordinator of the PhD Course in Pharmaceutical Science, and from 2013 to 2019 he was President of the Degree Course in Pharmaceutical Chemistry and Technologies. From 2004 to 2009, Prof. Mai was a member of the Executive Committee of the Medicinal Chemistry Division of the Italian Chemical Society, and from 2009 to 2014 he was a member of the Scientific Committee of the European School of Medicinal Chemistry. He is an Editor of the journal ChemMedChem (Wiley), Regional Editor of Mini Reviews in Medicinal Chemistry and Medicinal Chemistry (Bentham), and Associate Editor of Clinical Epigenetics (Springer) and the Journal of Enzyme Inhibition and Medicinal Chemistry (Taylor and Francis). His career has largely focused on the synthesis of new potential bioactive compounds, particularly in the field of epigenetics (since 1999: inhibitors of HDACs, HATs, sirtuins, PRMTs, HKMTs, KDMs and DNMTs). Prof. Mai is the author of more than 280 publications in high-impact international journals [h-index = 52] and three book chapters.
Inhaltsangabe
Targeting the Zinc-Dependent Histone Deacetylases (HDACs) for Drug Discovery.- Hydroxamic Acid-Containing Peptides in the Study of Histone Deacetylases.- Sirtuin Inhibitors and Activators.- Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors.- Lysine Methyltransferases and Their Inhibitors.- PRMT Inhibitors.- Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and Their Inhibitors.- Inhibitors of JmjC-Containing Histone Demethylases.- Chemical Compounds Targeting DNA Methylation and Hydroxymethylation.- Applied Biophysics for Bromodomain Drug Discovery.- Methyl-Readers and Inhibitors.- Altered Long Non-coding RNA Expression in Cancer: Potential Biomarkers and Therapeutic Targets? - Acetylation and Methylation in Asthma, COPD, and Lung Cancer.- Structure-Based Design ofEpigenetic Inhibitors.- Experimental Methodologies for Detection and Mapping of Epigenetic DNA Marks.- Advanced Assays in Epigenetics.
Targeting the Zinc-Dependent Histone Deacetylases (HDACs) for Drug Discovery.- Hydroxamic Acid-Containing Peptides in the Study of Histone Deacetylases.- Sirtuin Inhibitors and Activators.- Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors.- Lysine Methyltransferases and Their Inhibitors.- PRMT Inhibitors.- Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and Their Inhibitors.- Inhibitors of JmjC-Containing Histone Demethylases.- Chemical Compounds Targeting DNA Methylation and Hydroxymethylation.- Applied Biophysics for Bromodomain Drug Discovery.- Methyl-Readers and Inhibitors.- Altered Long Non-coding RNA Expression in Cancer: Potential Biomarkers and Therapeutic Targets? - Acetylation and Methylation in Asthma, COPD, and Lung Cancer.- Structure-Based Design ofEpigenetic Inhibitors.- Experimental Methodologies for Detection and Mapping of Epigenetic DNA Marks.- Advanced Assays in Epigenetics.
Targeting the Zinc-Dependent Histone Deacetylases (HDACs) for Drug Discovery.- Hydroxamic Acid-Containing Peptides in the Study of Histone Deacetylases.- Sirtuin Inhibitors and Activators.- Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors.- Lysine Methyltransferases and Their Inhibitors.- PRMT Inhibitors.- Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and Their Inhibitors.- Inhibitors of JmjC-Containing Histone Demethylases.- Chemical Compounds Targeting DNA Methylation and Hydroxymethylation.- Applied Biophysics for Bromodomain Drug Discovery.- Methyl-Readers and Inhibitors.- Altered Long Non-coding RNA Expression in Cancer: Potential Biomarkers and Therapeutic Targets? - Acetylation and Methylation in Asthma, COPD, and Lung Cancer.- Structure-Based Design ofEpigenetic Inhibitors.- Experimental Methodologies for Detection and Mapping of Epigenetic DNA Marks.- Advanced Assays in Epigenetics.
Targeting the Zinc-Dependent Histone Deacetylases (HDACs) for Drug Discovery.- Hydroxamic Acid-Containing Peptides in the Study of Histone Deacetylases.- Sirtuin Inhibitors and Activators.- Histone Acetyltransferase Enzymes: From Biological Implications to Most Relevant Inhibitors.- Lysine Methyltransferases and Their Inhibitors.- PRMT Inhibitors.- Lysine-Specific Histone Demethylases 1/2 (LSD1/2) and Their Inhibitors.- Inhibitors of JmjC-Containing Histone Demethylases.- Chemical Compounds Targeting DNA Methylation and Hydroxymethylation.- Applied Biophysics for Bromodomain Drug Discovery.- Methyl-Readers and Inhibitors.- Altered Long Non-coding RNA Expression in Cancer: Potential Biomarkers and Therapeutic Targets? - Acetylation and Methylation in Asthma, COPD, and Lung Cancer.- Structure-Based Design ofEpigenetic Inhibitors.- Experimental Methodologies for Detection and Mapping of Epigenetic DNA Marks.- Advanced Assays in Epigenetics.
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