GSPT1 MGD MRT-2359
Term · Oncology and biomedicine · MLC-T-ONC-014041
An orally bioavailable selective molecular glue degrader (MGD) of the translational termination factor GSPT1, with potential antineoplastic activity. Upon oral administration, MRT-2359 targets and binds to GSPT1, thereby promoting complex formation between the E3 ubiquitin ligase component cereblon (CRBN) and GSPT1, and inducing GSPT1 degradation in a CRBN- and degron-dependent manner. This downregulates L-MYC and N-MYC, thereby disrupting MYC-driven protein translation and reducing MYC-oncogenic signaling. This inhibits proliferation in MYC-driven tumors. The translation termination factor GSPT1, a G-loop degron-containing protein, plays a key role in protein translation in MYC-driven cancers.
| Identifier | MLC-T-ONC-014041 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | GSPT1-directed MGD MRT-2359; GSPT1-directed molecular glue degrader MRT-2359 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-014041",
"term": "GSPT1 MGD MRT-2359",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable selective molecular glue degrader (MGD) of the translational termination factor GSPT1, with potential antineoplastic activity. Upon oral administration, MRT-2359 targets and binds to GSPT1, thereby promoting complex formation between the E3 ubiquitin ligase component cereblon (CRBN) and GSPT1, and inducing GSPT1 degradation in a CRBN- and degron-dependent manner. This downregulates L-MYC and N-MYC, thereby disrupting MYC-driven protein translation and reducing MYC-oncogenic signaling. This inhibits proliferation in MYC-driven tumors. The translation termination factor GSPT1, a G-loop degron-containing protein, plays a key role in protein translation in MYC-driven cancers.",
"synonyms": [
"GSPT1-directed MGD MRT-2359",
"GSPT1-directed molecular glue degrader MRT-2359"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/gspt1-mgd-mrt-2359/"
}
Record 8,212 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.