From Natural Insulin to Designed Analogs: A Chemical Biology Exploration

Abstract Since its discovery in 1921, insulin has been at the forefront of scientific breakthroughs. From its amino acid sequencing to the revelation of its three‐dimensional structure, the progress in insulin research has spurred significant therapeutic breakthroughs. In recent years, protein engineering has introduced innovative chemical and enzymatic methods for insulin modification, fostering the development of therapeutics with tailored pharmacological profiles. Alongside these advances, the quest for self‐regulated, glucose‐responsive insulin remains a holy grail in the field. In this article, we highlight the pivotal role of chemical biology in driving these innovations and discuss how it continues to shape the future trajectory of insulin research.