ActiveSight Releases two Drug Target Portfolio Crystals

ActiveSight has announced an expansion of their line of "ready to go" protein crystals for drug discovery.

The two 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 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.