3D structure of key drug target sheds light on how to design better drugs

California, USA-based small-molecule drug developer Intellikine has announced the publication of an article, titled "The p110delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors," now available as an advanced on-line publication at Nature Chemical Biology.

The paper provides the first glimpse at the three-dimensional structure of PI3Kdelta (p110delta), an important drug target implicated in a wide range of diseases, including cancer, asthma and rheumatoid arthritis. There has been intense interest in the design of selective inhibitors against the family of PI3K drug targets, and this paper reports the atomic structure of the PI3Kdelta enzyme co-crystallized with both broad spectrum and isoform-selective inhibitors, says Intellikine.

The pioneering work was the result of a collaboration led by Roger Williams, Professor in the Laboratory of Molecular Biology at the Medical Research Council in Cambridge, UK, and it included scientists from the University of California, San Francisco, Intellikine in La Jolla, California, and the Merck-Serono Research Center in Geneva, Switzerland.