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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: https://doi.org/10.1021/acs.jmedchem.3c01319