Preferred Label : TEAD Inhibitor SW-682;
NCIt synonyms : Pan-TEAD Inhibitor SW-682;
NCIt definition : An orally bioavailable inhibitor of the transcription factor TEAD (TEA domain), with
potential antineoplastic activity. Upon oral administration, TEAD inhibitor SW-682
targets and binds to the TEAD palmitoylation pocket all TEAD isoforms, thereby disrupting
the interaction between the transcription co-activators yes-associated protein 1 (YAP)/transcriptional
coactivator with PDZ-binding motif (TAZ) and TEAD and inhibiting TEAD auto-palmitoylation.
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.;
Molecule name : SW-682; SW 682;
NCI Metathesaurus CUI : CL1928921;
Origin ID : C206390;
concept_is_in_subset
- has_target
