📜 History of Science

A Century of
Peptide Science

From the first synthetic dipeptide in 1901 to blockbuster GLP-1 drugs transforming obesity treatment — 120 years of discovery, Nobel Prizes, and molecular breakthroughs.

Key discovery
Nobel Prize
Major milestone
The Foundations (1900–1930)
1901
1901
First synthesis
The Birth of Peptide Chemistry
Emil Fischer & Ernest Fourneau
Emil Fischer synthesizes the first dipeptide, glycylglycine, naming the bond between amino acids the peptide bond — and giving us the word 'peptide' (from Greek peptos, digested).
1902
1902
First hormone
Secretin: The First Hormone
William Bayliss & Ernest Starling
Bayliss and Starling discover secretin — the first hormone — and coin the term 'hormone' for chemical messengers carried in the blood. Secretin is later found to be a 27-residue peptide.
1921
1921
Medicine
Insulin Discovered — Lives Saved
Frederick Banting, Charles Best, John Macleod, James Collip
A Toronto team extracts insulin and saves 14-year-old Leonard Thompson — the first person treated for diabetes. Before this, Type 1 diabetes was almost invariably fatal. Banting & Macleod receive the Nobel Prize in 1923.
1931
1931
Neuropeptide
Substance P Discovered
Ulf von Euler & John Gaddum
Von Euler and Gaddum discover Substance P — an 11-residue pain-signalling neuropeptide — in dried intestinal powder. The 'P' stands for 'powder,' the form it was in when discovered.
1921–22
1921–22
🏆 Nobel 1923Most important peptide
Insulin Discovered — A Million Lives Saved
Frederick Banting, Charles Best, James Collip & John Macleod — Toronto
In the summer of 1921, Frederick Banting and medical student Charles Best isolate a pancreatic extract that lowers blood sugar in diabetic dogs. Biochemist James Collip purifies it for human use. On January 11, 1922, 14-year-old Leonard Thompson — dying from Type 1 diabetes — receives the first human insulin injection. Within 24 hours his blood sugar normalises. Before insulin, Type 1 diabetes was a death sentence within months. Banting and Macleod receive the 1923 Nobel Prize in Physiology or Medicine. Insulin remains the single most important peptide in the history of medicine.
The Golden Age (1940–1970)
1942
1942
Antibiotic
Gramicidin S — First Peptide Antibiotic
Georgiy Gause & Maria Brazhnikova (Moscow)
Soviet scientists isolate gramicidin S from soil bacteria near Ryazan. It becomes a crucial wound treatment in WWII on the Eastern Front — the first non-ribosomal peptide antibiotic.
1953
1953
🏆 Nobel 1955
Insulin Sequenced — The Code is Readable
Frederick Sanger, Cambridge
After 10 years of work, Sanger determines the complete sequence of insulin — the first protein ever sequenced. It proves proteins have precise structures and earns the Nobel Prize in Chemistry 1955. Sanger later wins a second Nobel for DNA sequencing.
1953
1953
Hormone
Oxytocin & Vasopressin Synthesized
Vincent du Vigneaud, Cornell
Du Vigneaud achieves the first synthesis of a naturally occurring peptide hormone — oxytocin. Proof that biologically active hormones can be built from scratch. He receives the 1955 Nobel Prize in Chemistry.
1963
1963
Technology
Solid-Phase Synthesis — Peptides on Demand
Robert Bruce Merrifield, Rockefeller University
Merrifield invents solid-phase peptide synthesis (SPPS) — building peptide chains on resin beads. Weeks of chemistry condensed to hours. Makes peptide drugs commercially viable. Nobel Prize in Chemistry 1984. Still the foundation of peptide synthesis today.
1965
1965
Achievement
Insulin Synthesized — Chemistry Catches Up to Nature
Chinese team (Shanghai) & independent groups in USA, Germany
Three independent groups simultaneously synthesize active insulin. The Chinese team finishes first (September 1965), proving even complex disulfide-bonded hormones can be built entirely in a laboratory.
1969–77
1969–77
🏆 Nobel 1977Neuroendocrinology
Hypothalamic Peptides — The Brain Commands the Body
Roger Guillemin (Salk Institute) & Andrew Schally (Tulane)
After a famously bitter decade-long rivalry, Guillemin and Schally independently characterise the peptide hormones linking the brain to the endocrine system. Guillemin identifies TRH (3 AA — the smallest known hormone) and somatostatin. Schally identifies LH-RH / GnRH (10 AA — the master regulator of puberty and reproduction). Both teams processed tons of hypothalamic tissue from slaughterhouses to isolate microgram quantities. They share the 1977 Nobel Prize in Physiology or Medicine.
The Molecular Revolution (1970–2000)
1975
1975
Endorphins
The Endorphins: The Brain's Own Morphine
John Hughes & Hans Kosterlitz, Aberdeen
Hughes & Kosterlitz identify met-enkephalin and leu-enkephalin — the first endogenous opioids. The brain produces its own morphine. The word 'endorphin' is coined, and a new era in neuroscience begins.
1982
1982
Biotech
Recombinant Human Insulin — Biotech is Born
Genentech / Eli Lilly (Humulin)
Humulin — human insulin from genetically engineered E. coli — becomes the first recombinant DNA drug approved by the FDA. Modern biotech arrives as pharmaceutical reality. Bacteria become peptide factories.
1984
1984
🏆 Nobel 1984
Nobel for SPPS — Merrifield's Machine
Robert Bruce Merrifield
Merrifield receives the Nobel Prize for solid-phase synthesis. By now, automated synthesizers based on his method produce thousands of sequences for research worldwide — making the modern peptide drug industry possible.
1987
1987
Antimicrobial
Magainins — Frogs Fight Bacteria
Michael Zasloff, NIH
Zasloff notices frog wounds heal without infection in pond water — and isolates magainins. The discovery launches the modern field of antimicrobial peptides (AMPs).
1985
1985
First blockbusterOncology
Leuprolide — The First Peptide Blockbuster
Abbott Laboratories / Takeda (Lupron)
Leuprolide (Lupron) — a synthetic 9-residue GnRH analog — becomes the first peptide drug to exceed $1 billion in annual sales. It works paradoxically: continuous GnRH receptor stimulation causes downregulation, suppressing testosterone. This chemical castration effect makes it the standard treatment for prostate cancer and endometriosis. Lupron proves that peptide drugs can be commercial blockbusters — inspiring the modern peptide therapeutics industry.
The Drug Era (2000–present)
2004
2004
FDA approvalMarine-derived
Ziconotide — A Snail's Gift to Pain Medicine
Elan Pharmaceuticals / FDA
FDA approves ziconotide — a synthetic cone snail venom peptide. First marine-derived FDA drug, first non-opioid intrathecal analgesic, up to 1,000× more potent than morphine for certain pain types.
2005
2005
Diabetes
Exenatide (Byetta) — The Gila Monster Saves Lives
Amylin Pharmaceuticals / Eli Lilly
FDA approves exenatide — a Gila monster peptide analog — as the first GLP-1 receptor agonist. It sparks a revolution that culminates, two decades later, in semaglutide (Ozempic).
2015
2015
Antibiotic resistance
Teixobactin — First New Antibiotic Class in 30 Years
Kim Lewis, Northeastern University
Using the novel iChip device, Lewis's team discovers teixobactin — a new class of antimicrobial peptide from unculturable soil bacteria. Bacteria appear unable to rapidly develop resistance. Published in Nature.
2021–24
2021–24
Blockbuster
Semaglutide — The Obesity Revolution
Novo Nordisk (Ozempic 2017, Wegovy 2021)
Semaglutide (Wegovy) — a 31-residue GLP-1 analog — achieves 15–20% body weight loss in trials, comparable to bariatric surgery. By 2024 it is the best-selling drug in the world, grossing $20B+ annually, and inspires a new wave of peptide drug development.

🏆 Nobel Prizes for Peptides

1923 Banting & Macleod — Insulin 1955 Du Vigneaud — Oxytocin synthesis 1955 Sanger — Insulin sequencing 1977 Guillemin & Schally — Hypothalamic hormones 1984 Merrifield — Solid-phase synthesis 2002 Fenn & Tanaka — ESI/MALDI-MS

🔗 Related

🏆 Peptide world records 🌿 Peptides in nature 🔬 Peptide database 📖 Glossary