INNOVATION

1. Improving Crystal Quality to Enable the Development of New Drugs Small Business Innovation Research BioSpace International, Inc. Gaithersburg, MD A major bottleneck for the drug industry and research groups continues to be the inability to obtain high-quality, diffractable crystals for structure determination in new drug design. BioSpace International (BSI) has developed cutting-edge technologies that can crystallize hard-to-crystallize proteins. Results are repeatable and have been demonstrated in the laboratory and in space. INNOVATION • ACCOMPLISHMENTS • First production run of eight systems successfully used on STS-95 and STS-93. • X-ray topography has demonstrated the higher quality of space-grown crystals. • Meetings with interested aerospace/drug companies and federal laboratories are being scheduled. • COMMERCIALIZATION • Product: New drugs from the Dynamically Controlled Crystallization Systems (DCCS™), which is operable in space and ground environments. The DCCS can monitor, measure, and control the parameters that affect aggregation, nucleation, and crystal growth. Size and quality of crystal can be optimized accordingly. • Service: Crystal growth and x-ray diffractometry and topography analysis to improve crystal quality. X-ray topography is used to measure crystal quality, determine growth-induced defects, and provide a means of identifying corrective actions. • Unlike hanging/sitting drop-diffusion technique hardware, the DCCS technology can be used for protein crystal growth in Earth and space environments interchangeably, with repeatable results. • Patented in the U.S.; Patent Cooperation Treaty for 55 countries worldwide. • Primary market targets: Commercial drug companies, National Institute of Health, National Cancer Institute, and federal laboratories. • BSI technologies will be licensed to drug companies. Will also operate as a Contact Technical Organization to crystallize proteins for drug companies/researchers. Collaborations with peer-group companies and spinoffs are being explored. At left, a sharper, more uniform crystal is grown in microgravity; right, a terrestrial crystal grown under otherwise identical circumstances is more diffuse and shows a subgrain with a misorientation of 0.061º. • GOVERNMENT/SCIENCE APPLICATIONS • For NASA, efforts will increase the understanding of the influence of gravity on macromolecules and protein structure. • For NIH and NIST, supports the aims of the Human Genome Program by enabling structures to be determined. • Hard-to-crystallize proteins have been provided by NIH and Brookhaven National Laboratories to BSI for crystallization with the DCCS. Contacts: MSFC, Tom Knight; 256-544-5353 BioSpace, Shirley Arnowitz; 301-990-3586 1999 Phase II; NAS8-99080 Marshall Space Flight Center March 2000; Success Story #