| 摘要 |
A method for identifying modulators of the Keap1-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 Keap1 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 Keap1-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.
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