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Relay Therapeutics launches to tackle protein movement

Third Rock-backed firm will look for allosteric inhibitors for tough targets

by Lisa M. Jarvis
September 14, 2016 | A version of this story appeared in Volume 94, Issue 37

Credit: Relay
Relay’s interim CEO, Alexis Borisy.
Photo of Alexis Borisy.
Credit: Relay
Relay’s interim CEO, Alexis Borisy.

Backed by $57 million in funding, mostly from the venture capital firm Third Rock Ventures, Relay Therapeutics has launched with a drug discovery platform based on the concept of protein movement. The company wants to find novel allosteric sites on tough or intractable targets.

Relay, which Third Rock nurtured for two years before its launch, seeks to usher in the next wave of structure-based drug design. Decades ago, advances in X-ray crystallography allowed drug hunters to understand how their molecules were interacting with targets—and to tweak them accordingly. Those snapshots are now a routine part of drug discovery, but they don’t account for the inherent plasticity of biomolecules, which yawn and twist over time and as they interact with partners.

An understanding of protein movement will reveal new pockets for molecules to slip inside, explains Relay’s interim CEO, Alexis Borisy. “Now you see toeholds or handholds of places to put a drug, or a hinge you could interrupt, or how you could turn something on versus just inhibiting it,” he says.

To gain insight into protein movement, Relay has assembled technologies that, collectively, give it a “movie” rather than a snapshot of a protein. The nascent technologies Relay is tapping include room-temperature crystallography, which enables the firm to capture some protein movement, and novel NMR techniques that allow binding of small molecules to proteins to be detected and protein conformation changes to be studied.

One of Relay’s founders, Brandeis University biochemist Dorothee Kern, contributed to the development of both techniques.

The company is also tapping the computing power of D. E. Shaw Research to perform long-scale molecular dynamic simulations. The computational biochemistry firm is a contributor to Relay’s funding round.

Relay’s founders are counting on these technologies, combined with medicinal chemistry, biology, and biochemistry expertise, to help Relay scientists develop allosteric inhibitors—small molecules that alter the activity of a protein by binding outside of its active site.

The company, with a staff of roughly 25 people that will likely grow to 40 throughout the next year, will build a pipeline of compounds based on oncology targets that have eluded drug designers. Relay is also interested in establishing partnerships in neuroscience and immuno-inflammatory disease.



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