MLchartDataset catalogue

PRC2 inhibitor ORIC-944

Term · Oncology and biomedicine · MLC-T-ONC-016208

An orally bioavailable allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. Upon oral administration, PRC2 inhibitor ORIC-944 targets and binds to the regulatory embryonic ectoderm development (EED) subunit of PRC2. This prevents the methyltransferase activity of PRC2, spefifically the methylation of histone 3 at lysine27 (H3K27). This depletes H3K27 trimethylation (H3K27me3) and modulates the expression of target genes. This may inhibit tumor cell proliferation. PRC2 is dysregulated in a variety of cancer cell types and is associated with poor prognosis. It is responsible for the methylation of H3K27 leading to transcriptional silencing. EED is essential for the histone methyltransferase activity of PRC2.

Table 1. Record
IdentifierMLC-T-ONC-016208
FieldOncology and biomedicine
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-016208",
  "term": "PRC2 inhibitor ORIC-944",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. Upon oral administration, PRC2 inhibitor ORIC-944 targets and binds to the regulatory embryonic ectoderm development (EED) subunit of PRC2. This prevents the methyltransferase activity of PRC2, spefifically the methylation of histone 3 at lysine27 (H3K27). This depletes H3K27 trimethylation (H3K27me3) and modulates the expression of target genes. This may inhibit tumor cell proliferation. PRC2 is dysregulated in a variety of cancer cell types and is associated with poor prognosis. It is responsible for the methylation of H3K27 leading to transcriptional silencing. EED is essential for the histone methyltransferase activity of PRC2.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/prc2-inhibitor-oric-944/"
}

Record 13,563 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.