Rapid-access, high-throughput synchrotron crystallography for drug discovery

Area of Science:

• Structural biology
• Drug discovery
• Crystallography

Background:

• Synchrotron X-ray sources yield high-quality crystallographic data crucial for structure-guided drug design.
• Industrial use of synchrotrons is often limited and intermittent.
• The Lilly Research Laboratories Collaborative Access Team (LRL-CAT) beamline offers a unique solution for pharmaceutical and biotechnology companies.

Purpose of the Study:

• To describe how the LRL-CAT beamline integrates crystallographic experiments into the drug discovery process.
• To explain the methods for acquiring and disseminating protein crystallography results.
• To maximize the impact of structural data on developing new medicines.

Main Methods:

• Utilizing synchrotron X-ray sources for protein crystallography.
• Integrating crystallographic data acquisition directly into the drug discovery pipeline.
• Implementing routine and rapid daily use of structural data, including fragment library screening.

Main Results:

• The LRL-CAT beamline facilitates daily access to structural data.
• Crystallographic results are routinely integrated into pharmaceutical lead discovery and optimization.
• Fragment library screening is efficiently performed using the LRL-CAT data.

Conclusions:

• The LRL-CAT beamline provides a valuable resource for pharmaceutical and biotechnology companies.
• Daily integration of crystallographic data accelerates the drug discovery and development process.
• This approach enhances the impact of structural biology on creating new medicines.