Late-stage functionalization (LSF) constitutes a powerful strategy for the assembly or
diversification of novel molecular entities with improved physicochemical or biological …

We have analyzed FDA-approved macrocyclic drugs, clinical candidates, and the recent
literature to understand how macrocycles are used in drug discovery. Current drugs are …

The transcription factor nuclear factor erythroid 2‐related factor 2 (NRF2) is considered the
master regulator of the phase II antioxidant response. It controls a plethora of cytoprotective …

Targeted therapy is a groundbreaking innovation for cancer treatment. Among the receptor
tyrosine kinases, the fibroblast growth factor receptors (FGFRs) garnered substantial …

Targeting the protein–protein interaction (PPI) between the transcription factor nuclear factor
erythroid 2-related factor 2 (Nrf2) and its repressor, Kelch-like ECH-associated protein 1 …

Covering: 1981 to 2019 Natural products continue to play a major role in drug discovery,
with half of new chemical entities based structurally on a natural product. Herein, we report a …

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.• …

The development of simplified synthetic strategy to create structurally and functionally
diverse pseudo‐natural macrocyclic molecules is highly appealing but poses a marked …

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 …