Preferred Label : TEAD Inhibitor BPI-460372;
NCIt synonyms : TEAD-targeted Agent BPI-460372;
NCIt definition : An orally bioavailable, small molecule inhibitor of the transcription factor TEAD
(TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD
inhibitor BPI-460372 targets and covalently binds to the cysteine residue in the TEAD
palmitoylation pocket, thereby disrupting the interaction between the transcription
co-activators yes-associated protein 1 (YAP)/transcriptional coactivator with PDZ-binding
motif (TAZ) and TEAD and irreversibly 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 : BPI 460372; BPI-460372;
NCI Metathesaurus CUI : CL1907560;
Origin ID : C200564;
concept_is_in_subset
