Despite the efforts of pharmaceutical companies to develop specific kinase modulators, few
drugs targeting kinases have been completely successful in the clinic. This is primarily due …

Neurological diseases share common neuroinflammatory and oxidative stress pathways.
Both phenotypic and molecular changes in microglia, astrocytes, and neurons contribute to …

The discovery of potent, peptide site directed, tyrosine kinase inhibitors has remained an
elusive goal. Herein we describe the discovery of two such clinical candidates that inhibit the …

In the kinase field, there are many widely held tenets about conformation-selective inhibitors
that have yet to be validated using controlled experiments. We have designed, synthesized …

Protein kinases are important mediators of cellular communication and attractive drug
targets for many diseases. Although success has been achieved with developing ATP …

Tyrosine kinases have been intensively investigated as drug targets for several decades,
since they regulate many cellular processes including cell growth, differentiation, and …

Phosphorylation is a post‐translational modification that is involved in many basic cellular
processes and diseases, but is difficult to detect in real time with existing technologies. A …

Human kinases are recognized as one of the most important drug targets associated with
cancer. There are> 80 FDA-approved kinase inhibitors to date, most of which work by …

The protein arginine deiminases (PADs) are a family of enzymes that catalyze the post-
translational hydrolytic deimination of arginine residues. Four different enzymologically …

We have developed a general methodology to produce bivalent kinase inhibitors for c-Src
that interact with the SH2 and ATP binding pockets. Our approach led to a highly selective …