The characterization of a new potent and selective PI3Kdelta inhibitor, GS-9820, is being reported in a paper published in the December 6 issue of The Journal of Biological Chemistry.
The discovery was made by members of Western University's Bone and Joint Initiative with collaborators from Nihon University, the University of Calgary and Gilead Sciences, Inc.
Graduate student Ryan Shugg, working under the supervision of Stephen Sims, PhD, and Jeff Dixon, PhD, of Western's Department of Physiology and Pharmacology, used a panel of isoform-selective inhibitors and found that one isoform in particular, PI3Kdelta, regulates osteoclast shape and resorptive activity.
Sims says, "These findings suggest that selective inhibition of PI3K isoforms offers a new approach for the treatment of inflammatory bone diseases and skeletal metastases."
The studies were carried out by an interdisciplinary team, which included undergraduate student Ashley Thomson, visiting professor Natsuko Tanabe, research scientist Alexey Pereverzev, investigator Frank Jirik at the McCaig Institute for Bone and Joint Health (University of Calgary), along with researchers Adam Kashishian, Bart Steiner, Kamal Puri, and Brian Lannutti from Gilead Sciences.