3D Structures Could Lead to Improved Drugs

13 January 2010 (Last Updated January 13th, 2010 18:30)

Pioneering work from a team of US scientists has provided the first 3D view of the design structure of an important drug target implicated in a wide range of diseases including cancer. The paper published by Intellikine provides an important insight into the design of the atomic structu

Pioneering work from a team of US scientists has provided the first 3D view of the design structure of an important drug target implicated in a wide range of diseases including cancer.

The paper published by Intellikine provides an important insight into the design of the atomic structure of the PI3Kdelta enzyme, which is implicated in the cause of cancer, asthma and rheumatoid arthritis.

Howard Hughes Medical Institute investigator at the University of California Kevan Shokat said that this work is significant as it explains for the first time the structure-based design of highly selective inhibitors of PI3Kdelta.

"Nine structurally distinct inhibitors are reported and, as such, this paper represents the cutting-edge of isoform-selective inhibitor design in the PI3K drug target family," Shokat said.

The achievement is the result of a collaboration led by Roger Williams, PhD, professor in the Laboratory of Molecular Biology at the Medical Research Council in Cambridge, UK alongside scientists from the University of California, San Francisco, Intellikine in La Jolla, California, and Merck-Serono Research Center in Geneva, Switzerland.

Intellikine is a private, clinical-stage company focused on the discovery and development of innovative small molecule drugs against the PI3K/mTOR pathway.