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This book comprehensively reviews structure, optimization strategies, and function of natural and synthetic peptides. The initial section presents foundational aspects of therapeutic peptides, examining the potential of bioactive peptides derived from natural sources, it provides insights into the structure-function relationship of therapeutic peptides. The book also covers the de novo design, synthesis, modification, and mechanistic evaluation of therapeutic peptides, along with the generation and screening of peptide libraries for cell binding peptides. The second section focuses on the practical applications of therapeutic peptides in combating cancer cells and their application in treating neurological disorders using natural and synthetic neuropeptides. The potential of peptides in addressing metabolic disorders and their role in cardiovascular diseases through natriuretic peptides are also covered. The final section addresses the regulatory and safety aspects critical to the pharmaceutical development of therapeutic peptides. It covers quality specifications, regulatory considerations, and future prospects for therapeutic peptides. The toxicity of biologically active peptides and safety aspects are also discussed. This book is invaluable source for researchers and students of pharmaceutical sciences, biotechnology, and biomedical sciences.Key features:· Reviews the structure, optimization strategies, and functions of both natural and synthetic peptides.· Explores de novo design, synthesis, modification, and mechanistic evaluation of therapeutic peptides.· Discusses the generation and screening of peptide libraries for cell-binding peptides.· Covers conventional and advanced peptide-based targeted delivery systems.· Examines the practical applications of therapeutic peptides in various diseases.· Presents regulatory considerations, quality specifications, and toxicity of therapeutic peptides.