Preferred Label : YAP/TEAD Interaction Inhibitor IAG933;
NCIt synonyms : YAP/TEAD Inhibitor IAG933;
NCIt definition : An orally bioavailable inhibitor of the interaction between the transcription coactivator
yes-associated protein 1 (YAP) and the transcription factor TEAD (TEA domain), with
potential antineoplastic activity. Upon oral administration, YAP/TEAD inhibitor IAG933
disrupts the interaction between YAP and TEAD, thereby disrupting the interaction
between the transcription coactivators YAP/transcriptional coactivator with PDZ-binding
motif (TAZ) and TEAD. This may inhibit YAP/TAZ-TEAD promoted gene transcription involved
in tumor cell proliferation and survival. The Hippo-YAP/TAZ-TEAD 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. 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 : IAG 933; IAG-933;
NCI Metathesaurus CUI : CL1773758;
Origin ID : C185454;
UMLS CUI : C5667001;
Semantic type(s)
- concept_is_in_subset
