This book guides readers between different chemical ligation methodologies and applications, from the basics to more recent and sophisticated applications. The book moves from the fundamental aspects, so that novice readers can follow the entire book and apply these reactions in the lab. Attention is reserved to the synthetic aspects, so the book also serves as a valuable reference for experimental work. Finally, a selection of outstanding applications – including nanoscience, drug discovery, and biomaterials – provides an overview of chemical ligation’s potential and get other scientists involved bringing new idea and applications.