Preferred Label : AhR Inhibitor DA-4505;
NCIt synonyms : Aryl Hydrocarbon Receptor Inhibitor DA-4505; AhR Antagonist DA-4505;
NCIt 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.;
Molecule name : DA-4505; DA 4505;
Origin ID : C209753;
concept_is_in_subset
- has_target
