Compounds with activity against cancer kinases available for licensing

Sareum Holdings plc, a structure-based drug discovery specialist has developed and filed patents on novel small molecule compounds which show promising activity against two significant cancer drug targets, the Aurora and FLT kinases. Chief Executive Officer, Tim Mitchell, said, “We are actively seeking licensing partners for this programme to assist the advancement of these novel chemical series through to clinical candidate nomination.”

These are believed to be key to the regulation of cell division and proliferation that controls different stages in the development of a tumour. It is thought that a drug simultaneously able to inhibit the function of both targets will be more effective against cancer than an inhibitor acting on a single target.  

The Cambridge-based company has used its expertise in fragment and structure-based drug discovery to identify novel chemical compounds, which it has then optimised using its high throughput medicinal chemistry and structure determination platforms.  

Additionally, the determination of a hitherto un-reported Aurora kinase sub-type structure, have been reported by scientists at Sareum.

Aurora kinases have been implicated in the onset of several human cancers. They are over-expressed in different tumour types including colon, breast and pancreatic cancers and in leukemias.  The enzymes are involved in regulating multiple steps of mitosis  including centrosome duplication, formation of a bipolar mitotic spindle, chromosome alignment on the mitotic spindle and regulation of the fidelity-monitoring spindle checkpoint.

Similarly, FLT kinases have been demonstrated to be important in many stages of tumour development. FLT-1 has been linked to angiogenesis, a duplication of the FLT-3 gene is seen in many leukemias and FLT-4 is associated with tumor metastasis.