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...
Newsletter
Drug-resistant EGFR mutations in lung cancer
7/29/21
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...
Kinetic analysis of covalent and irreversible inhibitors
11/27/20
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...
Carna Tech Note No.2: The importance of assessing intrinsic target kinase activity
9/18/20
Carna Biosciences’ long standing commitment to manufacture highly active protein kinases is based on our belief that drugs designed to inhibit disease related protein dysregulation should be evaluated in activity- based enzyme assays usingthe most active kinases. Nearly all kinases produced at Carna are expressed in insect cells, purified, and...
Carna Tech Note No.1 : Production of Highly Active Protein Kinases for Drug Discovery Applications
6/28/20
Carna Biosciences’ long standing commitment to manufacture highly active protein kinases is based on our belief that drugs designed to inhibitdisease related protein dysregulation should be evaluated in activity- based enzyme assays using the most active kinases. Production of proteinkinases meeting these standards is not always an easy task. Despite use...