Increased expression and elevated levels of matrix metalloproteinase-2 (MMP-2) and MMP-9 play a role in impaired cardiac function. These MMPs make for essential targets in the treatment of heart failure, specifically heart failure with preserved ejection fraction (HFpEF).
HER2 is a receptor tyrosine kinase and well-established oncogenic driver with mutations present in various types of tumors such as bladder urothelial carcinoma, uterine corpus endometrial carcinoma, stomach adenocarcinoma and breast cancer.
Targeting TEAD with small-molecule inhibitors is an emerging therapeutic strategy for YAP/TAZ-dependent human cancers with Hippo pathway alterations. Bridgene Biosciences Inc. identified three hits with the Isobaric Mass Tagged Affinity Characterization (IMTAC) screening platform that covalently bound to TEAD1 with the binding site being cysteine 359, which led to the BGI-9004 compound.