Publications by authors named "Eddy J E Freyne"
ACS Med Chem Lett
January 2015
Article Synopsis
- A new Type II kinase inhibitor has been developed specifically for maternal embryonic leucine zipper kinase (MELK) using a method known as structure-based ligand design.
- This approach involved detailed structural analysis of the protein-ligand interactions through techniques like X-ray crystallography, which helped identify a unique pocket for the inhibitor to bind.
- The optimized inhibitor is highly effective, operating at low nanomolar concentrations and able to easily enter cells, making it a promising tool for researching MELK's biological functions.
ACS Med Chem Lett
January 2015
Article Synopsis
- Fragment-based drug design was used effectively to target maternal embryonic leucine zipper kinase (MELK).
- Researchers identified an initial low-affinity fragment that bound to MELK's hinge region in a unique way.
- This fragment was then optimized into a potent, cell-penetrating inhibitor with low nanomolar affinity, making it a valuable tool for studying MELK's biological roles.
