Newsletter

The simplest and most straightforward way to evaluate a kinase inhibitor is to look at its inhibitory effect on the enzyme activity response. For this to be most useful and accurate, it is critical to establish the appropriate assay condition like ATP concentration and substrate¹）. Issues can exist such as the...

The announcement that Kymera Therapeutics, a company pioneering targeted protein degradation, entered into a strategic collaboration with Sanofi to develop and commercialize first-in-class protein degrader therapies targeting IRAK4 in patients with immune-inflammatory diseases highlights the growing interest in clinical applications of small molecule mediated kinase degradation. Kymera received $150 million...

Since the clinical introduction of imatinib as a cancer therapeutic in 2001, the development of kinase inhibitors has focused on identification of first-in-class drugs for specific targets. Additionally, the search for next generation drugs targeting drug resistant kinase mutants has greatly expanded, initiating a focus on personalized medicine, particularly in...

Covalent inhibitors generally contain electrophiles that interact covalently with nucleophilic residues such as serine, lysine, histidine and cysteine in enzymes1). Penicillin, discovered in 1928 as the first effective treatment for bacterial infections, is one of the best known examples of a covalent inhibitor. The β-lactam present in penicillin binds covalently to...