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This book provides an overview of the latest developments and future challenges in enzyme inhibitor research. It discusses the general enzyme inhibitory principles and mechanisms in enzyme activity regulation and application of enzyme inhibitors in different areas and sectors. The major areas of applications of enzyme inhibitors covered in this book are human health management, agriculture, food processing and research, which leads to drug discovery or enzyme activity mechanisms. The book also identifies the gaps in the existing knowledge and opens up new research ideas in this important area. Currently, most enzyme inhibitors are reported to inhibit various classes of enzymes. These enzyme inhibitors are the focus of the scientific community because they may answer an increasing array of questions in the research area of biological sciences, including biochemistry, medicine, physiology, pharmacy, agriculture, ecology etc. It also serves as a useful tool inthe study of enzyme structures and reaction mechanisms and in the development of technologies in agriculture, food processing, and health management. Chapters in this book cover topics such as plant-derived inhibitors of serine proteases, pancreatic lipase (PL) inhibitors from indigenous medicinal plants, amylase inhibitors and their applications in agriculture and food processing industries and advances in silico techniques used in the study of enzyme inhibitors. The book will serve as a valuable resource for students and researchers in Life Sciences, agriculture, medicine, food processing, and allied industries.