JournalEducationThe History of Peptide Research: From Insulin to Modern Therapeutics
Education

The History of Peptide Research: From Insulin to Modern Therapeutics

The history of peptide research spans over a century, from the groundbreaking isolation of insulin to today cutting edge multi agonist compounds. This article traces the key milestones that shaped modern peptide science.

Dr. Sarah Mitchell

Research Director

20 February 2026
8 min read

The Dawn of Peptide Science

The story of peptide research begins in 1921 when Frederick Banting and Charles Best isolated insulin from pancreatic extracts. This discovery, which earned the Nobel Prize in 1923, demonstrated for the first time that a peptide hormone could be isolated, purified, and used therapeutically. Insulin remains the most widely used peptide therapeutic in the world.

Key Milestones

1921: Isolation of insulin by Banting and Best

1953: Frederick Sanger determines the complete amino acid sequence of insulin, proving that proteins have defined sequences

1963: Robert Bruce Merrifield develops solid phase peptide synthesis (SPPS), revolutionising peptide manufacturing and earning the Nobel Prize in 1984

1970s: Discovery of endorphins and enkephalins, revealing the role of neuropeptides

1980s: Development of recombinant DNA technology enables large scale peptide production

1990s: Discovery of GLP 1 and its role in glucose metabolism

2000s: Development of long acting GLP 1 analogues

2010s: Approval of Semaglutide and emergence of multi agonist compounds

2020s: Tirzepatide approval, Retatrutide trials, and the explosion of metabolic peptide research

The Solid Phase Synthesis Revolution

Merrifield's invention of solid phase peptide synthesis in 1963 was arguably the most important technical advance in peptide science. Before SPPS, peptide synthesis was laborious, time consuming, and limited to very short sequences. SPPS automated the process, enabling the rapid synthesis of peptides with dozens of amino acids and opening the door to the modern peptide research era.

The GLP 1 Era

The discovery of GLP 1's role in glucose metabolism in the 1980s and 1990s set the stage for what would become the most commercially successful class of peptide therapeutics. The development of Exenatide (from Gila monster venom), followed by Liraglutide and eventually Semaglutide, demonstrated the enormous therapeutic potential of incretin based peptides.

Modern Era: Multi Agonism

The current era of peptide research is defined by the concept of multi agonism, using a single molecule to activate multiple receptor targets simultaneously. Tirzepatide's dual GIP/GLP 1 agonism and Retatrutide's triple agonism represent the cutting edge of this approach, achieving efficacy levels that were unimaginable just a decade ago.

Conclusion

From insulin's isolation over a century ago to today's sophisticated multi agonist compounds, peptide research has undergone a remarkable evolution. Each breakthrough has built upon previous discoveries, creating an ever expanding toolkit for understanding human biology and developing new therapeutics.

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