New therapeutic target for diabetes uncovered

February 24, 2002

eMedicine News-

Medical and Science News

The insulin-signalling pathway is responsible for the body's response to

insulin and glucose uptake. Protein kinases such as GSK3, which is targeted in

this latest research, carry out the transfer of phosphate from ATP to particular

amino acids.

Previous research has shown that GSK3 is involved in multiple signalling

pathways, that it regulates blood glucose levels and becomes less active in the

presence of insulin. The reason for the alteration in function has not been

identified, however.

Dr Ernst ter Haar and colleagues from pharmaceuticals company Vertex

solved the structure of GSK3 using molecular replacement. They found that the

protein prefers to add phosphates to proteins that have already been

phosphorylated. This unusual property is explained by the structure of GSK3.

The researchers hope that these findings will lead to the development of

drugs targeting the enzyme, thereby improving the function of impaired cells,

and potentially benefiting millions of people.

Writing in the journal Nature Structural Biology, Dr ter Haar and

colleagues said, " The crystal structure of GSK3 presented here is the first

reported within the GSK3 family. The structure provides evidence that GSK3 uses

the phosphorylated serine or threonine at the P + 4 position of the substrate to

align the two domains for optimum catalytic activity. "

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