Reposted by Picotti Lab
Out now: ATP-competitive inhibitors lock kinases in a pseudo-active conformation and modulate their non-catalytic functions.
We show that these on-target, off-machanism effects can cause unexpected phenotypes and how to screen for these effects.
Read more at link.springer.com/article/10.1...
link.springer.com
Paradoxical non-catalytic kinase functions are driven by inhibitor-induced displacement of autoinhibitory domains - Molecular Systems Biology
ATP-competitive kinase inhibitors represent one of the largest classes of targeted anti-cancer drugs. While their primary mechanism is to block catalytic activity, they can also trigger paradoxical ph...
