Preferred Label : TEAD Inhibitor IK-930;
NCIt definition : An orally bioavailable, small molecule inhibitor of the transcription factor TEAD
(TEA domain), with potential antineoplastic activity. Upon oral administration, TEAD
inhibitor IK-930 targets, binds to 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. The
Hippo-YAP/TAZ-TEAD signaling pathway is dysregulated in certain cancers and diseases,
including mesothelioma, neurofibromatosis type 2 (NF2)/large tumor suppressor 1 (LATS1)/
large tumor suppressor 2 (LATS2) mutated tumors and tumors with functional YAP/TAZ
fusions. It plays a key role in cancer initiation, progression, and cancer cell resistance
to various therapies. Mutations in the NF2 gene, common in malignant mesothelioma,
limits the expression of Merlin, which is an activator of the Hippo pathway and suppresses
the nuclear translocation of YAP and TAZ. LATS1/LATS2 are serine/threonine-protein
kinases involved in the kinase cascade of the Hippo pathway; their activation leads
to the inactivation of YAP/TAZ.;
Molecule name : IK-930; IK 930;
NCI Metathesaurus CUI : CL1792194;
Origin ID : C187365;
UMLS CUI : C5706417;
Semantic type(s)
- concept_is_in_subset
