History - Peptides Academy

The Pioneers (1901-1953)

The story of peptide science begins with a German chemist who coined the word "peptide" and ends with the first protein ever fully sequenced. This era laid the foundation for everything that followed.

1901

The Word "Peptide"

Emil Fischer coins "peptide" and synthesizes glycylglycine -- the first peptide made in a lab. He also established the concept of the peptide bond. Nobel Prize in Chemistry, 1902.

1921

Insulin Discovered

Banting and Best isolate insulin from dog pancreas at the University of Toronto. In 1922, 14-year-old Leonard Thompson becomes the first human treated with insulin, transforming diabetes from a death sentence to a manageable condition.

1953

Insulin Sequenced

Frederick Sanger determines the complete amino acid sequence of insulin -- the first protein ever fully sequenced. This proved proteins have definite chemical structures, not random mixtures. Nobel Prize 1958.

Sanger's sequencing work took 12 years. He painstakingly broke insulin into fragments using different enzymes, identified the amino acids in each fragment, then pieced together the overlapping sequences like a molecular jigsaw puzzle.

The Synthesis Revolution (1963-1982)

With sequences known, the next challenge was building peptides from scratch. A revolutionary technique made it possible to synthesize any peptide in days instead of years, while genetic engineering opened a completely new frontier.

1963

Solid-Phase Synthesis

Bruce Merrifield invents SPPS (solid-phase peptide synthesis). By anchoring amino acids to an insoluble resin bead, he automated what had been tedious solution chemistry. SPPS reduced synthesis time from months to days. Nobel Prize 1984.

1977

Recombinant DNA

Genentech engineers E. coli bacteria to produce human somatostatin -- the first human protein made by recombinant DNA. This proved that bacteria could be programmed to manufacture human peptides at scale.

1982

Humulin Approved

FDA approves Humulin (Genentech/Eli Lilly) -- the first recombinant DNA drug. Human insulin made by bacteria replaced pig and cow insulin, eliminating allergic reactions. This marked the birth of the biotech pharma industry.

The Discovery Era (1992-2005)

Sometimes the most important discoveries come from unexpected places. A Gila monster in the Arizona desert would inspire an entirely new class of drugs that would eventually reshape modern medicine.

1992

Gila Monster Discovery

John Eng at the VA Medical Center discovers exendin-4 in Gila monster venom -- a peptide that mimics human GLP-1 but resists enzymatic breakdown. Where natural GLP-1 lasts 2 minutes in the body, exendin-4 lasts hours.

2005

First GLP-1 Drug

FDA approves exenatide (Byetta) -- the first GLP-1 receptor agonist drug. Based directly on the Gila monster peptide from 13 years earlier. This launched the entire GLP-1 drug class that would later produce Ozempic.

Why Gila monster venom? Gila monsters eat only 3-4 times per year. Their venom contains peptides that dramatically regulate blood sugar and appetite during these rare meals -- exactly the mechanism researchers needed for diabetes drugs.

The GLP-1 Revolution (2017-2024)

In less than a decade, GLP-1 receptor agonists went from niche diabetes drugs to a cultural phenomenon generating over $30 billion in annual revenue. This era transformed how the world thinks about obesity and metabolic disease.

2017

Semaglutide Era Begins

FDA approves semaglutide (Ozempic) for type 2 diabetes. Novo Nordisk's engineering -- a fatty acid chain enabling albumin binding -- extended the half-life to a full week, enabling once-weekly dosing.

2021

Wegovy for Obesity

FDA approves higher-dose semaglutide (Wegovy) specifically for obesity, showing ~15% weight loss in trials. Celebrity adoption and social media attention trigger a global demand surge and widespread shortages.

2022

Dual Agonist Breakthrough

Tirzepatide (Mounjaro) approved -- the first dual GIP/GLP-1 agonist. SURMOUNT trials show up to 22.5% weight loss, surpassing semaglutide. Eli Lilly's market cap surges past $800 billion.

2024

Regulation Catches Up

FDA cracks down on compounding pharmacies making copycat semaglutide. Shortage officially resolved. Legal battles between pharma companies and compounders reshape the peptide access landscape.

What's Next?

The peptide pipeline has never been more active. Over 150 peptide therapeutics are currently in clinical trials, and several breakthroughs could fundamentally change medicine in the coming decade.

Oral Peptides

The end of injections? -- oral semaglutide proved it's possible. Next-gen oral GLP-1 drugs (orforglipron, danuglipron) use small-molecule agonists that survive stomach acid. If successful, they could make peptide therapy as simple as taking a pill.

Triple Agonists

Beyond dual agonism -- retatrutide targets GLP-1, GIP, and glucagon receptors simultaneously. Phase II trials showed up to 24% weight loss. If Phase III confirms, it could become the most effective weight-loss drug ever made.

AI Discovery

Machine learning + peptide design -- companies like Evotec, Nuritas, and Peptone are using AI to predict peptide structures, optimize stability, and discover entirely new therapeutic peptides that evolution never produced.

The peptide market is projected to reach $50+ billion by 2030. GLP-1 drugs alone generated over $30 billion in 2024. With new targets (amylin, GDF-15, activin) entering clinical trials, peptide therapeutics are becoming one of pharma's fastest-growing segments.

Knowledge Check

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Practice Exercises

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