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

2/28/2006 11:43:03 AM

SAN DIEGO, Feb. 28 /PRNewswire/ -- 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(TM), a division of Rigaku Americas Corporation offers full gene-to-structure protein crystallography services for client's targets, including X-ray data collection and fragment-based screening, featuring the Rigaku FR-E and ACTOR (TM) automation systems. For more information visit

ActiveSight and ACTOR are trademarks of Rigaku.


CONTACT: Joy Silen, Director of Business Development of ActiveSight,+1-858-455-6870,

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