Oxidative stress has been implicated in a wide range of pathological conditions. The
transcription factor nuclear factor erythroid 2-related factor 2 (Nrf2) exerts a central role in …

Highlights•The Keap1-Nrf2 interaction is a major regulator of antioxidant and
antiinflammatory proteins.•Keap1-Nrf2 inhibitors activate Nrf2 leading to cytoprotection.• …

Introduction The nuclear factor erythroid 2-related factor 2 (Nrf2) is a pivotal transcription
factor that controls the expression of numerous cytoprotective genes and regulates cellular …

By controlling several antioxidant and detoxifying genes at the transcriptional level,
including NAD (P) H quinone oxidoreductase 1 (NQO1), multidrug resistance-associated …

Macrocycles are prominent among drugs for treatment of infectious disease, with many
originating from natural products. Herein we report on the discovery of a series of …

The disruption of the protein–protein interaction (PPI) between Nrf2 and Keap1 is an
attractive strategy to counteract the oxidative stress that characterises a variety of severe …

The Nrf2 transcription factor is a master regulator of the cellular response to oxidative stress,
and Keap1 is its primary negative regulator. Activating Nrf2 by inhibiting the Nrf2–Keap1 …

The process of developing new drugs is arduous and costly, particularly for targets classified
as “difficult-to-drug.” Macrocycles show a particular ability to modulate difficult-to-drug …

Nuclear factor erythroid 2-related factor 2 (Nrf2) signaling has become a key pathway for
cellular regulation against oxidative stress and inflammation, and therefore an attractive …

Drug discovery strategies have advanced significantly towards prioritizing target selectivity
to achieve the longstanding goal of identifying “magic bullets” amongst thousands of …