Fu-Bao Huang

Discovery of Highly Potent and Selective, Orally Bioavailable BTK-Targeting PROTACs Featuring Novel CRBN-Binding Warheads.

Drugs targeting Bruton's tyrosine kinase (BTK) are recognized as key tools in hematological oncology. The clinical efficacy of BTK inhibitors is limited, however, by the emerging resistance driven by BTK mutations and the severe toxicity attributed to off-target kinase inhibition. PROteolysis TArgeting Chimeras (PROTAC...