Peptide drug development has made great progress in the last decade thanks to new production, modification, and analytic technologies. Peptides have been produced and modified using both chemical and biological methods, together with novel design and delivery strategies, which have helped to overcome the inherent drawbacks of peptides and have allowed the continued advancement of this field. A wide variety of natural and modified peptides have been obtained and studied, covering multiple therapeutic areas.

Therapeutic peptides are a unique class of pharmaceutical agents composed of a series of well-ordered amino acids, usually with molecular weights of 500-5000 Da. Research into therapeutic peptides started with fundamental studies of natural human hormones, including insulin, oxytocin, vasopressin, and gonadotropin-releasing hormone (GnRH), and their specific physiological activities in the human body. Since the synthesis of the first therapeutic peptide, insulin, in 1921, remarkable achievements have been made resulting in the approval of more than 80 peptide drugs worldwide. The development of peptide drugs has thus become one of the hottest topics in pharmaceutical research.

Although the field of therapeutic peptides started with natural hormones, the discovery and development trends have since shifted from simply mimicking natural hormones or peptides derived from nature to the rational design of peptides with desirable biochemical and physiological activities. Major breakthroughs in molecular biology, peptide chemistry and peptide delivery technologies have allowed significant progress in the fields of peptide drug discovery, peptide production, and their therapeutic applications. More than 80 therapeutic peptides have reached the global market to date, and hundreds of peptides are undergoing preclinical studies and clinical development. These peptide drugs have been applied to a wide range of diseases, such as diabetes mellitus, cardiovascular diseases, gastrointestinal diseases, cancer, infectious diseases, and vaccine development. Considering their huge therapeutic potentials, market prospects, and economic values, we expect therapeutic peptides to continue to attract investment and research efforts and to achieve long-term success. From Signal Transduct Target Ther. 2022; 7: 48.

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