Polyamines are ubiquitous molecules that are involved in a number of important cellular processes. Aberrations in their function or metabolism play a role in diseases such as cancer and parasitic infection. A number of validated drug targets have been identified, including enzymes in the polyamine biosynthetic and catabolic pathways and the S-adenosylmethionine synthetic and salvage pathways. Polyamine Drug Discovery is the first comprehensive volume to cover all aspects of the design and development of potential therapeutics targeting polyamine metabolism. The book details research progress from 1975 to the present date and discusses the design and use of polyamine metabolism inhibitors as therapeutic agents. Various polyamine-containing drugs are described that can be used in chemotherapy, and as treatments for infections including trypanosomiasis, leishmaniasis and malaria. Finally, the roles of polyamine analogues in chemoprevention, polyamine-containing vectors for gene delivery, and the design of polyamine-based epigenetic modulators are detailed. Each chapter addresses a different aspect of polyamine drug discovery and all are written by medicinal and biological chemists with particular expertise in developing agents that modulate polyamine metabolism or function. The book will increase the visibility of polyamine drug discovery among pharmaceutical researchers and provide a valuable reference for everyone working in the field.
Polyamine Drug Discovery:: Synthetic Approaches to Therapeutic Modulators of Polyamine Metabolism; Structural Biology in Polyamine Drug Discovery; Antiparasitic Drug Discovery for the Polyamine Pathway; Inhibitors of Polyamine Biosynthetic Enzymes; Symmetrical- and Unsymmetrical Terminally Alkylated Polyamines; Targeting the Polyamine Catabolic Enzymes Spermine Oxidase, N1-Acetylpolyamine Oxidase and Spermidine/Spermine-N1-Acetyltransferase; Design of Polyamine Transport Inhibitors as Therapeutics; Non-Covalent Polynuclear Platinum Compounds as Polyamine Analogs; Polyamine-Based Agents for Gene and siRNA Transfer; The Design and Development of Polyamine-Based Analogs with Epigenetic Targets; Clinical Applications of Polyamine-Based Therapeutics; Subject Index
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