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

Wednesday, September 19, 2007 General News J E 4
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SAN DIEGO, Sept. 18 ActiveSight, a division of RigakuAmericas Corporation, announced today that it will collaborate on aFragment-based Lead Discovery (FBLD) Project with CHDI, Inc.

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

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

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

ActiveSight's high-throughput structural biology capabilities willfacilitate rapid screening of CHDI's HD target with hundreds of drug-likefragments. Automated data collection and structural determination will befacilitated by Rigaku's tools for high-throughput X-ray crystallography,including the ACTOR(TM) crystal-mounting system robot and MIFit+ automatedstructural determination software. ActiveSight has leveraged thesecapabilities to screen several drug targets with their proprietary fragmentlibraries, and is pursuing lead development on promising fragment hits. TheCHDI project will be overseen by Vicki Nienaber, Ph.D. at ActiveSight, apioneer in the utilization of X-ray crystallography for Fragment-basedscreening and lead development.

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

About Huntington Disease

Huntington Disease is a familial disease, passed from parent to childthrough a mutation in a gene. Each child of a Huntington Disease parent has a50-50 chance of inheriting the Huntington Disease gene which causes programmeddegeneration of brain cells and results in emotional disturbance, loss ofintellectual faculties and uncontrolled movements. Most people with HuntingtonDisease develop the symptoms at midlife but in some people onset occurs ininfancy or old age. The average survival time after onset is approximatelyfifteen to twenty years. It is estimated that about one in every 10,000persons has the Huntington Disease gene. At this time, there is no way to stopor reverse the course of Huntington Disease.

About ActiveSight

ActiveSight(R) is a division of Rigaku Americas Corporation and is aleading provider of fragment-based lead discovery and structural biology fordrug discovery. Utilizing high-throughput Rigaku X-ray crystallographyinstrumentation and world-class expertise, ActiveSight enables rapid leaddiscovery and development for its pharmaceutical, biotechnology, andinstitutional partners. For more information visithttp://www.active-sight.com.

About CHDI, Inc. and High Q Foundation

CHDI
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