KG-FP-003

KG-FP-003 is a potent and selective pan-TEAD proteolysis-targeting chimera (PROTAC) designed to directly target the TEAD-YAP interaction. Developed by Kygent Therapeutics, it utilizes the CRBN E3 ubiquitin ligase to induce the degradation of TEAD transcription factors, specifically TEAD1 and TEAD4. This degradation results in the disruption of downstream Hippo pathway signaling, leading to durable antiproliferative effects in various cancer models, including mesothelioma (NF2-deficient or LATS1/2-deficient) and other solid tumors. Preclinical data indicates that KG-FP-003 provides more effective inhibition of YAP target genes compared to traditional TEAD lipid-binding pocket (LBP) or protein-protein interaction (PPI) inhibitors.