abstract |
A method for identifying modulators of the Keapl -NrG-ARE pathway is described. In particular, an assay is described that identifies molecules that inhibit the binding of a labeled Nrf2 peptide with the kelch domain of the Keapl protein. Molecules that inhibit the binding are activators of the Keap 1 -Nrf2- ARE pathway. Activation of the Keap 1 -Nrf2- ARE pathway may result in an increased accumulation of Nrf2 and the subsequent induction of protective enzymes, for example, the phase 2 detoxification enzymes. Activators of the Keapl- NrG-ARE pathway are useful for combating oxidative stress-related disorders, such as those associated with cancer, emphysema, Huntington's disease, light-induced retinal damage, and stroke. |