Polyamine Drug Discovery (eBook)

Patrick M. Woster, Ph.D. is Professor and Center for Economic Excellence Endowed Chair in the Department of Pharmaceutical and Biomedical Sciences at the Medical University of South Carolina. He is a medicinal chemist with an interest in the synthesis of molecules that modulate polyamine metabolism or chromatin remodeling as potential antitumor agents. Dr. Woster also maintains a program in antiparasitic drug discovery with a particular emphasis on malaria and trypanosomiasis. He has produced a number of inhibitors that target enzymes in the polyamine biosynthetic pathway, and synthesized the first unsymmetrically substituted alkylpolyamine analogues. Molecules developed in the Woster laboratory have been shown to produce dramatic effects on a variety of tumor cells by initiating apoptosis, binding to DNA and by producing epigenetic changes in gene expression. Robert A. Casero, Jr., Ph.D. is a Professor of Oncology in the Johns Hopkins University School of Medicine. Dr. Casero is a molecular pharmacologist who has spent most of the last 30 years studying the role of polyamines in normal and tumour cell growth, and devising strategies to target polyamine function and metabolism for therapeutic benefit. His laboratory was responsible for cloning several genes involved in human polyamine catabolism; genes whose expression are thought to play a role in determining cellular responses to specific polyamine analogues.

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