MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-014041
FieldOncology and biomedicine
SynonymsGSPT1-directed MGD MRT-2359; GSPT1-directed molecular glue degrader MRT-2359
ReferencesNational 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.