Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …

Cancer is one of the major healthcare challenges across the globe. Several anticancer
drugs are available on the market but they either lack specificity or have poor safety, severe …

Gliomas are the most common and challenging malignancies of the central nervous system
(CNS), due to their infiltrative nature, tendency to recurrence, and poor response to …

Background Glioblastoma (GBM) is a fatal brain tumor, lacking effective treatment.
Epidermal growth factor receptor (EGFR) is recognized as an attractive target for GBM …

Fragment based drug discovery has long been used for the identification of new ligands and
interest in targeted covalent inhibitors has continued to grow in recent years, with high …

Reactive oxygen species (ROS) are physiological mediators of cellular signaling and play
potentially damaging roles in human diseases. In this study, we found that the catalytic …

Once considered potential liabilities, the modern era witnesses a renaissance of interest in
covalent inhibitors in drug discovery. The available toolbox of electrophilic warheads is …

With a resurgence in interest in covalent drugs, there is a need to identify new moieties
capable of cysteine bond formation that are differentiated from commonly employed systems …

Cancer cells have the ability of dysregulation and autonomous proliferation due to
unchecked production of definite molecules. These molecules are involved in the cell growth …

Secondary acquired mutation in EGFR, ie. EGFR T790M and amplification of c-MET form the
two key components of resistant NSCLC. Thus, previously published pharmacophore …