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Showing posts with the label TEAD

Etern Therapeutics Ready for YAP/TEAD Inhibitor ETS-006

Etern Therapeutics announced that the U.S. FDA has granted orphan drug designation to the YAP/TEAD inhibitor ETS-006 for treating patients with malignant mesothelioma. Etern has not yet submitted the IND application in either China or the U.S. Hippo pathway dysregulation can lead to diseases like cancer. Drug development focuses on targeting Hippo kinases, YAP/TAZ levels, and YAP-TEAD interactions, aiming to disrupt YAP-TEAD activity and inhibit disease progression. The core Hippo pathway ETS-006 ETS-006, an orally available YAP/TEADs PPI inhibitor, is discovered by Etern Therapeutics. YAP, with TEAD transcription factors, drives Hippo pathway signaling and regulates cancer progression. Its overactivation promotes metastasis, immune evasion, and drug resistance. Inhibiting YAP/TEAD interactions effectively suppresses YAP’s transcriptional activity. In 2022, Etern filed a patent (WO2023155927) for the YAP/TEAD inhibitors. The structure of example 124 is shown below. Structures ...