Selective JAK inhibition: mimicking SOCS activity

Selective JAK inhibition: mimicking SOCS activity

The opportunity

  • JAK signalling is frequently dysregulated in inflammatory diseases and cancer.
  • Current JAK inhibitors are approved for rheumatoid arthritis and myelofibrosis.
  • Unlike current JAK inhibitors, SOCS mimetics are not ATP-competitive and selectively inhibit JAK signalling

JAK inhibitors are effective treatments in blood cancers and inflammatory diseases. Current JAK inhibitors bind in the ATP binding pocket and compete with endogenous ATP.

Development of small molecules that selectively inhibit JAK signalling in a non-ATP competitive way will avoid issues with kinase selectivity and potential resistance.

Scientific figure

The technology

Our researchers have solved the structure of SOCS proteins bound to JAK1 and JAK2, which allows the precise molecular details of this mechanism of inhibition to be understood.

This structural information provides important insights into substrate binding and paves the way for the development of a novel class of non-ATP competitive small molecule inhibitors of JAK kinases.

Opportunities for partnership

Our novel therapy has potential applications in a range of conditions. Specific indications will be identified based on scientific rationale and commercial opportunities.

We have:

  • Identified hit compounds that inhibit JAK2 in vitro.
  • Established methods for protein production and validated in vitro assays.
  • World-class expertise in structural biology of JAK-SOCS interactions.

We are seeking:

  • Investment to support lead development and validation.
  • Investment to enable preclinical studies.

Scientific team

Dr Jeff Babon, Laboratory head, Structural Biology division

Contact

Dr Anne-Laure Puaux, Head, Commercialisation

Phone: +61 3 9345 2175 

Email: partnering@wehi.edu.au