Potent pan-TEAD auto-palmitoylation inhibitor with anti-proliferation efficacy against mesothelioma with NF2 defect.
VT107 is a potent pan-TEAD auto-palmitoylation inhibitor (3 μM; using TEAD isotype-overexpressing HEK293T) that blocks TEAD-mediated gene transcription (IC50 = 4.93 nM) by preventing its association with YAP/TAZ. VT107 selectively inhibits the proliferation of mesothelioma cultures with NF2 mutation (NCI-H2051 IC50 = 20.4 nM), deletion (NCI-H2373 IC50 = 9.35 nM) or deficiency (NCI-H226 IC50 = 8.67 nM), but not those with wild-type NF2.
European journal of medicinal chemistry, 226, 113835-113835 (2021-09-13)
The Hippo pathway is involved in organ size control and tissue homeostasis by regulating cell growth, proliferation and apoptosis. It controls the phosphorylation of the transcription co-activator YAP (Yes associated protein) and TAZ (Transcriptional coactivator with PDZ-binding motif) in order
Molecular cancer therapeutics, 20(6), 986-998 (2021-04-15)
Mutations in the neurofibromatosis type 2 (NF2) gene that limit or abrogate expression of functional Merlin are common in malignant mesothelioma. Merlin activates the Hippo pathway to suppress nuclear translocation of YAP and TAZ, the major effectors of the pathway
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