History

A Once-in-a-Generation
Paradigm Shift

In the early 1990s, the pharmaceutical industry was transformed by the widespread adoption of structure-based drug design—a process in which the three-dimensional structure of a given target protein is used to guide the design of drugs that bind to that target. 

Until recently, this process has been based largely on static “snapshots” of the target protein. Recent advances in experimental and computational technologies, however, have begun to reveal the dynamic structural changes undergone by such proteins, which are often central to their function.

The team and the tools that Relay has assembled are allowing it to observe the motion of pharmaceutically relevant target proteins and to predict how they would interact with hypothetical drug molecules. In particular, our approach is creating new opportunities for the design of powerful and selective allosteric drugs, which interact with one part of a target protein in order to change the behavior of another part.

By placing protein motion at the heart of drug discovery, Relay is pursuing what it believes will be a fundamental paradigm shift within the pharmaceutical industry, ushering in a new generation of drugs with the potential to improve and extend the lives of millions of patients.

  1. 1915 William and Lawrence Bragg are awarded the Nobel Prize for the use of X-rays to determine crystal structure
  2. 1961 Jacques Monod and Francois Jacob coin the term "allosteric inhibition" in written comments on the experiments on l-threonine deaminase carried out at the Institut Pasteur by Jean-Pierre Changeux as a Ph.D. student of Monod
  3. 1963 Hilary Muirhead and Max Perutz present the human hemoglobin X-ray structure and the concept of allosteric protein regulation is established
  4. 1989 Two research teams led by Manuel Navia and Alexander Wlodawer solve the first structures of HIV protease, an enzyme essential to the replication of HIV, contributing greatly to structure-based drug design efforts that ultimately transform HIV from an almost universally fatal disease to a potentially chronic one
  5. 1994 The carbonic anhydrase inhibitor dorzolamide is approved, providing the first example of structure-based drug design leading to an approved drug
  6. 2016 Relay Therapeutics is founded with the aim of incorporating protein motion as an integral component of its product engine