AI Summary
This article discusses the discovery of selective LATS inhibitors through scaffold hopping, aiming to improve drug-likeness and kinase selectivity for potential applications in regenerative medicine. The researchers identified an advanced LATS inhibitor with potent kinase activity, exceptional selectivity, and superior oral pharmacokinetic profiles.
Due to its essential roles in cell proliferation and apoptosis, the precise regulation of the Hippo pathway through LATS presents a viable biological target for developing new drugs for cancer and regenerative diseases. However, currently available probes for selective and highly drug-like inhibition of LATS require further improvement in terms of both activ-ity, selectivity and drug-like properties. Through scaffold hopping aided by docking studies and AI-assisted prediction of metabolic stabilities, we successfully identified an advanced LATS inhibitor demonstrating potent kinase activity, excep-tional selectivity against other kinases, and superior oral pharmacokinetic profiles.
This article is Open Access
Please wait while we load your content… Something went wrong. Try again?