Gertrude Elion and the birth of rational drug design

HIST 7

Mark Michalovic, markm@chemheritage.org, Chemical Heritage Foundation, 315 Chestnut Street, Philadelphia, PA 19106-2702
Before the double helical structure of DNA had even been elucidated, Gertrude Elion along with George Hitchings began working to develop drugs that would interfere with the ability of cancer cells to incorporate purine bases into their DNA. Their strategy to jam the system with purine-derived compounds not only led to the discovery of new chemotherapeutic agents like 6-mercaptopurine and immunosuppressive drugs like Imuran, but also ushered in a new age of drug discovery, in which medicines were not discovered by trial-and-error but were invented based on a thorough understanding of the biochemistry of disease. This approach of rational drug design led Elion to invent many more new medicines, including the first antiviral drugs. It also earned her and Hitchings the Nobel Prize for Medicine or Physiology in 1988.