Preferred Label : Pan-TEAD Inhibitor ISM6331;
NCIt synonyms : TEAD Inhibitor ISM6331;
NCIt definition : An orally bioavailable non-covalent small molecule inhibitor of the TEA domain (TEAD)
family of transcription factors, including TEAD1, TEAD2, TEAD3 and TEAD4, with potential
antineoplastic activity. Upon oral administration, pan-TEAD inhibitor ISM6331 reversibly
binds to the TEAD palmitoylation site and inhibits TEAD, thereby disrupting the interaction
between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional
coactivator with PDZ-binding motif (TAZ) and TEAD. This may inhibit YAP/TAZ-TEAD-promoted
transcription of multiple genes involved in tumor cell proliferation, progression
and survival, and may result in enhanced apoptosis in TEAD-dependent cancers. Hippo
pathway alterations, as seen in tumors with neurofibromatosis type 2 (NF2)-deficiency,
large tumor suppressor 1 (LATS1) and 2 (LATS2) mutations and YAP/TAZ fusions, lead
to Hippo pathway activation, hyperactivation of YAP/TAZ and activation of TEAD. It
plays a key role in cancer initiation, progression, and cancer cell resistance to
various therapies.;
Molecule name : ISM-6331; ISM 6331;
Origin ID : C210651;
concept_is_in_subset
- has_target
