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New Structural Biology Company Formed in San Diego, CA

The Woodlands, TX — November 3, 2003.  Rigaku announced the formation of ActiveSight, a new structural biology company in San Diego, California. ActiveSight will provide a proprietary high-throughput structural biology platform to pharmaceutical and biotech customers to rapidly solve three dimensional (3D) structures of proteins with drug development lead compounds bound in their active sites. The company's goal is to provide the pharmaceutical and biotechnology industry with access to the latest in crystallographic and protein engineering.

ActiveSight's team of scientists, under the direction of Duncan McRee, Ph.D., President, brings together the specific expertise needed to take structure based design services to a new level of productivity. Central to the business model is a streamlined approach to protein crystallography that provides affordable structures of exceptional quality. The company plans to build a catalog of proteins important in drug discovery and to use these to produce "co-crystal structures" on a contract basis with client compounds bound. These services will enable the development cycle for new therapeutics to be significantly shortened.

While other structural biology companies are providing service crystallography, they also are typically practicing medicinal chemistry in-house so as to eventually take drugs to market themselves. Most also provide services in the context of relatively large, multi-target collaborations. By focusing on service crystallography alone, ActiveSight intends to establish itself as a discreet, non-competing, and non-exclusive supplier of services to many pharmaceutical companies on a "pay-as-you-go" basis.

In addition to crystals of proteins that are currently drug targets, such as kinases, proteases and nuclear hormone receptors, ActiveSight will also deliver crystals of proteins involved in ADME/Tox. "A large number of promising leads fail because of negative interactions with proteins involved in drug metabolism" said Ronald V. Swanson, Ph.D., ActiveSight's Chief Scientific Officer, "By actually seeing their molecules interact with these proteins within the crystal, medicinal chemists can redesign their leads in a streamlined manner. This allows them to target the negative interactions directly and to iterate more rapidly and more economically."

Structure-based drug design is a technique that has been around since the 1980's but has not been fully exploited due to the laboriousness of obtaining crystal structures by traditional means. Utilizing a robotic crystallization system built by Rigaku's partner, RoboDesign, ActiveSight will crystallize target proteins rapidly and in large quantities. A new high-brilliance X-ray system, the HomeLab ™, will allow data collection rates up to 40 times faster than traditional laboratory sources. "The ActiveSight technical platform will allow automatic, efficient parsing of multiple crystallization conditions, and rapid in-house screening of crystals for the best diffraction." said Mark Knuth, Ph.D., Chief Technology Officer.

Rigaku—Leading With Innovation

Since its inception in Japan in 1951, Rigaku has been at the forefront of analytical and industrial instrumentation technology. Rigaku and its subsidiaries form a global group focused on life sciences and general purpose analytical instrumentation. With hundreds of major innovations to its credit, Rigaku and its subsidiary companies are world leaders in the fields of small molecule and protein crystallography, X-ray spectrometry and diffraction, X-ray optics, as well as semiconductor metrology. Rigaku employs over 1,100 people in the manufacture and support of its analytical equipment. Its products are in use in more than 70 countries—supporting research, development, and quality assurance activities. Throughout the world, Rigaku continuously promotes partnerships, dialog, and innovation within the global scientific and industrial community.

For further information, contact:

Joseph D. Ferrara, Ph.D.
VP Product Marketing and CSO
Rigaku Americas Corporation
(281) 362-2300
eMail: joseph.ferrara@rigaku.com