TEAD inhibitor SW-682
Term · Oncology and biomedicine · MLC-T-ONC-017005
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.
| Identifier | MLC-T-ONC-017005 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | Pan-TEAD inhibitor SW-682 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-017005",
"term": "TEAD inhibitor SW-682",
"field": "Oncology and biomedicine",
"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.",
"synonyms": [
"Pan-TEAD inhibitor SW-682"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/tead-inhibitor-sw-682/"
}
Record 16,057 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.