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ActiveSight Launches Four Crystal Targets for Structure Based Drug Design

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ActiveSight, the contract crystallography arm of Rigaku Americas Corporation, has introduced four targets to their "ready-to-go" co-crystallization proteins for structure-based drug design.

The addition of a 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 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™ 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 Hsp90 co-crystal structures suitable for 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."