Kinase inhibitors effectively illustrate the success of molecular targeted therapeutics, most dramatically as therapies for several types of cancer. To date, the US FDA has approved more than 50 small molecule kinase inhibitors¹⁾. In general, most kinase inhibitors have low selectivity, attributed to their interactions with the ATP-binding pocket, a...
Newsletter
Kinase Inhibitors in the Fight against COVID-19～
4/24/20
Worldwide efforts to develop preventative and therapeutic treatments for coronavirus associated disease of 2019 (COVID-19), caused by SARS-CoV-2 (Severe Acute Respiratory Syndrome Coronavirus 2), are intensely focused on identification of potential targets based on its molecular virology and disease biology. Given it could be a considerable time before an effective...
The significance of ATP concentration in cell-free and cell-based assays
10/ 8/193 comments
ATP concentration greatly affects the determination of kinase inhibitory activity, given most kinase inhibitors bind to the ATP binding site of the kinase. Cell free (biochemical) assays typically utilize ATP concentrations approximating the ATP Km, however this is frequently far lower than the mM ATP concentrations found in cells. ...
Targeted Protein Degraders
6/30/19
This year marked the exciting start of clinical trials for a first in class protein degrader targeting androgen receptor for the treatment of prostate cancer. Arvinas, Inc., is now set to initiate the second clinical program of their PROTAC™ (proteolysis-targeting chimaera) protein degrader for the treatment of patients with locally...
Residence time and compound selectivity
5/25/19
Human kinases are well-studied targets and have extensive involvement in a variety of diseases. More than 50 registered small molecule drugs target this enzyme class, and more than 250 kinase inhibitors are being actively evaluated in clinical trials. Most kinase inhibitors are classified as Type I, which act by binding...