Going intracellular

Merck Research Laboratories scientists have found a small molecule made in fungi that bypasses the need for insulin when given to animals by directly stimulating the intracellular kinase domain of the insulin receptor.

While oral insulin sensitizers such as PPAR gamma agonists of the thiazolidinedione class are on the market, there is no direct replacement for injected insulin itself. A number of companies are trying to develop oral or inhaled versions of the hormone. Now Merck (Rahway, N.J.) has identified a nonpeptidyl fungal metabolite, L-783,281, that acts on the insulin receptor. The compound significantly lowered blood glucose levels in two mouse models of diabetes (p<0.002)...