Three Methods for Peptide Cyclization via Lactamization -- Solid-Phase Peptide Cyclization with Two Disulfide Bridges -- Peptide Macrocyclization through Palladium-Catalyzed Late-Stage C-H Activation -- Three Methods for the Solution Phase Synthesis of Cyclic Peptides -- Computational Design of Structured and Functional Peptide Macrocycles -- On-Resin Peptide Cyclization Using the 3-4-Amino-(Methylamino)Benzoic Acid (MeDbz) Linker -- Scalable and Efficient in planta Biosynthesis of Sunflower Trypsin Inhibitor-1 (SFTI) Peptide Therapeutics -- Ligation, Macrocyclization, and Simultaneous Functionalization of Peptides by Multicomponent Reactions (MCR) -- Diels-Alder Cycloadditions for Peptide Macrocycle Formation -- Protein Catalyzed Capture (PCC) Agents for Antigen Targeting -- Preparation of Bacterial Cell-Surface Displayed Semisynthetic Cyclic Peptides -- The Discovery of Peptide Macrocycle Rescuers of Pathogenic Protein Misfolding and Aggregation by Integrating SICLOPPS Technology and Ultra-Throughput Screening in Bacteria -- In Vitro Selection of Thioether-Closed Macrocycle Peptide Ligands by Means of the RaPID System -- MOrPH-PhD: A Phage Display System for the Functional Selection of Genetically Encoded Macrocyclic Peptides -- Discovery of Antimicrobial Peptide Macrocycles Through Bacterial Display -- Assessing the Cellular Uptake, Endosomal Escape, and Cytosolic Entry Efficiencies of Cyclic Peptides -- In silico Analysis of Peptide Macrocycle-Protein Interactions -- Binding Characterization of Cyclic Peptide Ligands to Target Proteins and Chemical Epitopes using ELISA and Fluorescence Polarization Assays -- Determining the Binding Kinetics of Peptide Macrocycles using Bio-Layer Interferometry (BLI) -- Different Approaches to Cyclize a Cell-Penetrating Peptide and to Tether Bioactive Payloads -- Helical Stabilization of Peptide Macrocycles by Stapled Architectures -- Development and Characterization of Light Responsive Peptide Macrocycles -- Hydrogel Formation with Enzyme-Responsive Cyclic Peptides -- Cyclization and Self-Assembly of Cyclic Peptides. .

This volume explores the latest techniques and strategies used to study the field of peptide macrocycles. The chapters in this book ae organized into four parts: macrocycles synthesis, combinational library synthesis and screening, macrocycle characterization, and unique applications. Part One looks at a variety of peptide cyclization methodologies, and Part Two describes methods for the creation of peptide macrocycles libraries and their subsequent screening against biological targets of interest. Part Three discusses the study and characterization of peptide macrocycle-target interactions, and Part Four introduces unique applications for peptide macrocycles, from higher-order structure formation to post-synthetic functional modifications. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and comprehensive, Peptide Macrocycles: Methods and Protocols is a valuable resource for both novice and expert researchers looking to learn more about this developing field.