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.
| Identifier | MLC-T-ONC-009733 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | aryl hydrocarbon receptor inhibitor DA-4505; AhR antagonist DA-4505 |
| References | National 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.