Structure of key cancer drug target identified

Researchers from Monash’s Department of Biochemistry and Molecular Biology have determined the structure of the protein JAK2 kinase, a discovery with huge implications for the design and development of new cancer drugs.

NHMRC Industry Research Fellow Dr Isabelle Lucet, from Monash’s Protein Crystallography Unit headed by Dr Jamie Rossjohn, was part of the team that determined the structure. JAK2 kinase was the driving force for many cancers and cardiovascular disorders, she said.

The research, partly funded by a $1.2 million Australian Research Council Linkage Grant, was a joint project between drug development company Cytopia Limited and the Protein Crystallography Unit.

The JAK kinases, which were first discovered by Cytopia’s chief scientific officer Dr Andrew Wilks, are a well-validated drug target.

Dr Lucet said the discovery of JAK2 kinase’s structure had allowed an internationally competitive structure-based drug design on JAK kinase inhibitors to begin.

“This will help the development of drugs for cancer and other disorders by assisting with the design of specific molecules.”

She said the high expertise of the Monash research team, combined with the drug discovery capability of Cytopia, would undoubtedly enable more selective drug targets to be developed against diseases where the JAK kinases play a pivotal role.

Dr Lucet said the new discovery would allow the rapid growth of a portfolio of phase I therapeutics.