MLchartDataset catalogue

AhR inhibitor DA-4505

Term · Oncology and biomedicine · MLC-T-ONC-009733

An orally bioavailable small molecule inhibitor of the aryl hydrocarbon receptor (AhR; class E basic helix-loop-helix protein 76; bHLHe76), with potential immunomodulating and antineoplastic activities. Upon oral administration, AhR inhibitor DA-4505 specifically targets and binds to AhR, inhibits AhR activation, prevents AhR-mediated signaling, and AhR-dependent tumor cell proliferation. Abrogation of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs), regulatory T cells (Tregs) and decreases suppressive cytokines in the tumor microenvironment (TME). It stimulates cytotoxic T-cell activation and expansion. This may restore the immune response against tumor cells. AhR, a member of the basic helix-loop-helix/Per-Arnt-Sim (bHLH/PAS) family of transcription factors, plays key roles in regulating immunity and cellular differentiation. It mediates the expression of multiple immune related and tumor cell signal transduction and proliferation genes.

Table 1. Record
IdentifierMLC-T-ONC-009733
FieldOncology and biomedicine
Synonymsaryl hydrocarbon receptor inhibitor DA-4505; AhR antagonist DA-4505
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-009733",
  "term": "AhR inhibitor DA-4505",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable small molecule inhibitor of the aryl hydrocarbon receptor (AhR; class E basic helix-loop-helix protein 76; bHLHe76), with potential immunomodulating and antineoplastic activities. Upon oral administration, AhR inhibitor DA-4505 specifically targets and binds to AhR, inhibits AhR activation, prevents AhR-mediated signaling, and AhR-dependent tumor cell proliferation. Abrogation of AhR activation prevents the activation of immune-tolerant dendritic cells (DCs), regulatory T cells (Tregs) and decreases suppressive cytokines in the tumor microenvironment (TME). It stimulates cytotoxic T-cell activation and expansion. This may restore the immune response against tumor cells. AhR, a member of the basic helix-loop-helix/Per-Arnt-Sim (bHLH/PAS) family of transcription factors, plays key roles in regulating immunity and cellular differentiation. It mediates the expression of multiple immune related and tumor cell signal transduction and proliferation genes.",
  "synonyms": [
    "aryl hydrocarbon receptor inhibitor DA-4505",
    "AhR antagonist DA-4505"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/ahr-inhibitor-da-4505/"
}

Record 562 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.