ActiveSight and CHDI Leverage Fragment-based Lead Discovery for Huntington Disease Therapies

San Diego, CA -- September 18, 2007—ActiveSight, a division of Rigaku Americas Corporation, announced today that it will collaborate on a Fragment-based Lead Discovery (FBLD) Project with CHDI, Inc.

FBLD involves the binding of small compounds, "fragments," to the active sites of protein drug targets. The fragments are much smaller than the compounds used in traditional high-throughput screening (HTS), allowing a more extensive sampling of chemical space with a smaller screening library. Utilizing a Huntington Disease (HD) target chosen by CHDI, ActiveSight will screen fragment libraries using X-ray crystallography to visualize fragments that bind to the target. The fragments will then be linked or grown into larger, drug-like compounds that are thought to be more efficiently binding than compounds resulting from HTS methodologies.

Several compounds based on Fragment-based Lead Discovery (FBLD) methodologies are currently in clinical trials, and the technology is thought to shorten the time from drug target selection to an investigational new drug (IND) filing. The two companies hope that the FBLD collaboration will lead to HD therapies in shorter time periods than conventional lead discovery methods such as HTS.

"ActiveSight's Fragment-based Lead Discovery technologies strengthen our diversified portfolio of parallel drug discovery and development campaigns for Huntington Disease," said Robert Pacifici, Ph.D., CSO of CHDI, Inc. "By obtaining and testing high quality lead compounds quickly, we hope to increase the chances of finding a treatment for HD soon."

ActiveSight's high-throughput structural biology capabilities will facilitate rapid screening of CHDI's HD target with hundreds of drug-like fragments. Automated data collection and structural determination will be facilitated by Rigaku.s tools for high-throughput X-ray crystallography, including the ACTOR™ crystal-mounting system robot and MIFit+ automated structural determination software. ActiveSight has leveraged these capabilities to screen several drug targets with their proprietary fragment libraries, and is pursuing lead development on promising fragment hits. The CHDI project will be overseen by Vicki Nienaber, Ph.D. at ActiveSight, a pioneer in the utilization of X-ray crystallography for Fragment-based screening and lead development.

"We are pleased to have the opportunity to work with CHDI to discover new treatments for Huntington Disease," said Duncan McRee, Ph.D., President of ActiveSight. "We will work closely with CHDI's drug discovery team to turn the results of our high-throughput FBLD screens into tightly binding lead compounds."

About Huntington Disease

Huntington Disease is a familial disease, passed from parent to child through a mutation in a gene. Each child of a Huntington Disease parent has a 50-50 chance of inheriting the Huntington Disease gene which causes programmed degeneration of brain cells and results in emotional disturbance, loss of intellectual faculties and uncontrolled movements. Most people with Huntington Disease develop the symptoms at midlife but in some people onset occurs in infancy or old age. The average survival time after onset is approximately fifteen to twenty years. It is estimated that about one in every 10,000 persons has the Huntington Disease gene. At this time, there is no way to stop or reverse the course of Huntington Disease.

About ActiveSight

ActiveSight® is a division of Rigaku Americas Corporation and is a leading provider of fragment-based lead discovery and structural biology for drug discovery. Utilizing high-throughput Rigaku X-ray crystallography instrumentation and world-class expertise, ActiveSight enables rapid lead discovery and development for its pharmaceutical, biotechnology, and institutional partners. For more information visit www.active-sight.com.

About CHDI, Inc. and High Q Foundation

CHDI, Inc. and the High Q Foundation, Inc. (High Q) are non-profit organizations that share the mission of bringing together academia, industry, governmental agencies, and other funding organizations in the search for Huntington Disease treatments.

CHDI, Inc. is pursuing a biotech approach to rapidly discover and develop drugs that prevent or slow Huntington Disease. Through collaborations with industrial and academic partners, CHDI, Inc. participates in all aspects of drug discovery and development from lead discovery to preclinical development. For more information about CHDI, Inc. and its collaborative programs please see www.chdi-inc.org

High Q supports Huntington Disease research aimed at target identification and validation, the development and use of animal models, drug delivery, and the search for markers of disease progression. For more information about High Q and its support of Huntington Disease research please see www.highqfoundation.org.

Vicki Nienaber Joins ActiveSight, Strengthening Their Structure-Based Drug Design Services

SAN DIEGO, April 5, 2007. — ActiveSight, a division of Rigaku Americas Corporation, announced today that Vicki Nienaber, Ph.D., a pioneer in the development of fragment-based screening for drug discovery, has joined as the Chief Scientific Officer (CSO). Vicki was most recently Senior Director of Lead Discovery and Crystallography at SGX Pharmaceuticals, where she ran the c-Abl kinase drug discovery project in collaboration with Novartis. While working at Abbott Laboratories, she was the lead inventor of fragment-based screening, co-inventor of the ACTOR^TM robotic system for automated crystal sample handling, and she developed one of the first automated structure-based drug design laboratories. Vicki has written numerous peer-reviewed scientific publications and is an author of four patents.

"We are very pleased to have Vicki join us" said Duncan McRee, Ph.D., President of ActiveSight. "Vicki will bring a new level of service and science to our drug discovery clients, especially in the area of fragment-based screening."

ActiveSight, the leading provider of X-ray crystallography services for structure-based drug design, also offers fragment-based screening services to its pharmaceutical and biotechnology clients. Fragment-based screening involves the binding of drug-like fragments to the active sites of crystallized protein drug targets, allowing scientists to develop novel, high-affinity inhibitors. Relying on state-of-the-art Rigaku X-ray crystallography automation, ActiveSight can screen up to 100 protein structures a day for pharmaceutical and biotechnology clients.

ActiveSight also leads its own fragment-based screening projects, collaborating with The Scripps Research Institute to find novel inhibitors for HIV protease. The combination of ActiveSight’s high-throughput structural proteomics platform with Dr. Nienaber’s scientific leadership is expected to result in a greater accessibility of fragment-based screening technology to pharmaceutical companies for drug discovery. As a result, more novel, targeted compounds may be developed as drugs against diseases such as cancer, AIDS, and inflammation.

ActiveSight Signs Multi-Target Crystallography Service Agreement with Lexicon Pharmaceuticals

SAN DIEGO, January 5, 2007 /PRNewswire/ — ActiveSight announced that it has signed an expanded crystallography services agreement with Lexicon Pharmaceuticals. The agreement, the third between the companies, covers co-crystallography services for multiple proprietary targets of Lexicon Pharmaceuticals. ActiveSight's second co-crystallography agreement with Lexicon was announced in April of 2005. Lexicon Pharmaceuticals is the medicinal chemistry division of Lexicon Genetics Incorporated.

"We are delighted that Lexicon Pharmaceuticals has decided to expand their relationship with ActiveSight. We look forward to providing continued structural biology support for Lexicon's drug discovery programs," stated Duncan McRee, President of ActiveSight.

ActiveSight Releases Two New Drug Target Portfolio Crystals: iNOS and PPAR gamma

SAN DIEGO, September 5, 2006 /PR Newswire/ — ActiveSight has announced an expansion of their line of "ready to go" protein crystals for drug discovery. The two newly added proteins are inducible nitric oxide synthase (iNOS) and peroxisome proliferator-activated receptor gamma (PPAR gamma), both active targets of structure-based drug design programs.

iNOS produces large bursts of nitric oxide as part of the immune response. Overproduction of nitric oxide damages tissue and has been linked to inflammation and autoimmune diseases. iNOS is an ideal candidate for lead optimization using structure-based drug design because of the need for selectivity over closely related enzymes. Inhibitors are currently being investigated as treatments for septic shock, rheumatoid arthritis, inflammatory bowel disease and arteriosclerosis.

PPAR gamma is the target of the glitazone family of therapeutics. Synthetic PPAR gamma ligands have been shown to improve insulin sensitivity. In addition to its role as a diabetes target, PPAR gamma may also play a role in cancer and inflammation. PPAR gamma is the third nuclear hormone receptor (NHR) available from ActiveSight for rapid co-crystal structure determination. The other NHRs currently available are PPAR delta and the farnesoid X receptor (FXR).

The addition of iNOS and PPAR gamma brings the total number of available targets in ActiveSight's Protein Portfolio to fourteen.

ActiveSight Launches Fragment Screening Service and Four New Crystal Targets for Structure Based Drug Design: FAK, Caspase 3, PTP-1B, and DPP-4

SAN DIEGO, February 28, 2006 /PR Newswire/ — ActiveSight, the contract crystallography arm of Rigaku Americas Corporation, introduced four new targets to their popular "ready-to-go" co-crystallization proteins for structure-based drug design. The addition of a new kinase, a phosphatase, and two proteases brings the total number of targets available to biotech and pharmaceutical customers to twelve. Focal adhesion kinase (FAK) is the second Portfolio Protein kinase for oncology drug discovery. Protein tyrosine phosphatase 1B (PTP-1B) is a diabetes target which dephosphorylates the insulin receptor kinase. Dipeptidyl peptidase IV (DPP-4 or DPP-IV) is a diabetes target responsible for GLP-1 degradation. Caspase 3 is an emerging apoptosis target with promise in the treatment of ischemia. These new Portfolio targets expand a collection which includes the oncology targets Hsp90 and Aurora-A kinase; nuclear hormone receptor targets PPAR-delta and FXR, implicated in metabolic disorders; PDE-4 for asthma and inflammation; the hypertension target Renin; the type-II diabetes target FBPase; and the anti-infective target bacterial DNA gyrase.

Utilizing their in-house Rigaku ACTOR (TM) robot and FR-E SuperBright generator, ActiveSight has also initiated a comprehensive fragment screening program centered on targets in their Protein Portfolio product line. ActiveSight is offering a set of novel Hsp90 co-crystal structures suitable for new lead development, the result of fragment screening of Hsp90 against their >400 member, hand-selected library. The fragment screening service is also available for crystals and/or libraries provided by clients.

"We have experienced a very positive reaction to our Protein Portfolio services, particularly among biotech companies. We expect several of the new targets to be very popular," stated Ronald V. Swanson, Chief Scientific Officer and co-founder of ActiveSight. "Our fragment screening service is also being introduced in response to market demand. This service will appeal both to biotechs and to the larger pharmaceutical companies looking to leverage ActiveSight's automation for crystal screening."

ActiveSight Signs Protein Crystallography Agreement with Novo Nordisk

SAN DIEGO, January 23, 2006 /PR Newswire/ — ActiveSight announced that it has signed an agreement with Novo Nordisk A/S to provide protein crystallography services.   ActiveSight will co-crystallize Novo Nordisk proprietary molecules with proteins expressed by ActiveSight.  Additional details of the agreement were not disclosed.

"We are very pleased to add a company of Novo Nordisk's stature to our growing customer base. We look forward to supplying their scientists with structural information to accelerate their discovery efforts," stated Ronald V. Swanson, Ph.D., Chief Scientific Officer for ActiveSight.

This is the first announced agreement of 2006 for the protein crystallography services provider, which was founded in 2003.