Accelerating drug discovery at Exelixis through cryo-EM

TL;DR

This paper discusses how Exelixis uses cryo-EM to speed up drug discovery by enabling high-resolution structural analysis efficiently.

Contribution

The novel contribution is the implementation of a new cryo-EM facility at Exelixis for rapid and flexible structural enablement in drug design.

Findings

Exelixis' cryo-EM facility enables efficient structural enablement within days.

The facility supports continuous improvement of compound-target interactions and quick onboarding of new targets.

Abstract

Structure based drug design is now an established paradigm for the industrious task of making and optimizing novel therapeutics. The cryo- electron microscopy (cryo-EM) “resolution revolution”, and the recent automation improvements in data acquisition and processing make cryo-EM single particle analysis a pivotal method for high resolution structural enablement at an industrial scale. At Exelixis, our brand new cryo-EM facility allows a combination of efficient structural enablement within days and high flexibility. This allows i) efficient and reliable continuous support when improving the interaction between a compound and a target, and ii) quick on-boarding and optimization of new targets.