Story on discovery of Pi3K-C2α-selective inhibitors

out now in Journal of Medicinal Chemistry!

Find out how we developed isoform-selective Class II phosphoinositide-3-kinases (PI3K) C2α inhibitors. Starting from a high-throughput screening hit, we optimized pteridone-based inhibitors into the first isoform-selective chemical probes for Pi3K-C2α. Structure-activity relationship studies complemented by computational modeling revealed the structural basis for their outstanding selectivity.

Read our paper here: