Newsletter

The significance of ATP concentration in cell-free and cell-based assays

10/21/19

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

8/ 7/19

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

7/17/19

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...

A story about biotin-avidin affinity and how it accelerate small molecule drug discovery

5/20/19

Biotin is a type of water soluble vitamin, also called vitamin B7. Although it's an essential substance for all species, only baceria, yeast, mold, algae and certain plants are capable of producing it, leaving the mammalian species depend on external sources. Did you know that biotin deficiency attributes to congenital...