The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Photodynamic therapy (PDT) has been extensively investigated for decades for tumor
treatment because of its non-invasiveness, spatiotemporal selectivity, lower side-effects, and …

Sulfoximines have been largely disregarded in medicinal chemistry for a long time.
However, recently, they have risen to the apparent level of stardom on the drug discovery …

Sensing invasive cytosolic DNA is an integral component of innate immunity. cGAS was
identified in 2013 as the major cytosolic DNA sensor that binds dsDNA to catalyze the …

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 …

A large proportion of biomedical research and the development of therapeutics is focused
on a small fraction of the human genome. In a strategic effort to map the knowledge gaps …

There are several challenges towards the development and clinical use of small molecule
inhibitors, which are currently the main type of targeted therapies towards intracellular …

Protein phosphorylation is a major regulator of protein function and biological outcomes.
This was first recognized through functional biochemical experiments, and in the past …

Opportunistic infections caused by Pneumocystis jirovecii, Cryptococcus neoformans, and
ubiquitous airborne filamentous fungi have been recently reported in patients with …

For kinase inhibitors, intracellular target selectivity is fundamental to pharmacological
mechanism. Although a number of acellular techniques have been developed to measure …