Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

In aerobic organisms, oxygen is essential for efficient energy production but paradoxically,
produces chronic toxic stress in cells. Diverse protective systems must exist to enable …

In the relatively young but expanding field of irreversible kinase inhibitor drug discovery,
there are two main developments that are of central importance. First, the patients have …

The post-translational modification (PTM) of proteins (eg, phosphorylation, acetylation,
ubiquitinylation, SUMOylation) is a fundamental mechanism of cell signaling that modulates …

Leptin is highly expressed in the placenta, mainly by trophoblastic cells, where it has an
important autocrine trophic effect. Moreover, increased leptin levels are found in the most …

OBJECTIVE—Sulforaphane is an activator of transcription factor NF-E2–related factor-2
(nrf2) that regulates gene expression through the promoter antioxidant response element …

BACKGROUND: Isothiocyanates are phytochemicals with a broad array of effects in
biological systems. Bioactivity includes the stimulation of cellular antioxidant systems …

Brassicales contain a myrosinase enzyme that hydrolyzes glucosinolates to form toxic
isothiocyanates (ITC), as a defense against bacteria, fungi, insects and herbivores including …

Organic isothiocyanates (ITCs), which are characterized by the presence of an–N= C= S
group, are among the most extensively studied cancer chemopreventive agents and show …