Inhibition of tau phosphorylation: a new therapeutic strategy for the treatment of Alzheimer's disease and other neurodegenerative disorders

There is some evidence to suggest that hyperphosphorylation of tau protein is an early event in the development of neurofibrillary pathology and appears to compromise the ability of tau to bind to and stabilise microtubules. Thus, the blockade of this hyperphosphorylation step may be a prime target at which to interrupt the pathogenic cascade. Efforts to discover rational targets (mainly tau kinases) and inhibitors of tau hyperphosphorylation (protein kinase inhibitors) are discussed in this paper. Patenting activity from 1997 to date has focused on two major areas: development of methods for screening new compounds and discovery of tau protein kinases inhibitors. Some mention is also made regarding Alzheimer's disease (AD) diagnosis methods based on tau hyperphosphorylation.