Preferred Label : Aryl Hydrocarbon Receptor Inhibitor IK-175;
NCIt synonyms : AhR Inhibitor IK-175; Aryl Hydrocarbon Receptor Antagonist IK-175; AhR Antagonist IK-175; AhRi KYN-175; Aryl Hydrocarbon Receptor Antagonist KYN-175; AhRi IK-175;
NCIt definition : An orally bioavailable selective 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 IK-175 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 : KYN 175; KYN-175; IK-175; IK 175;
NCI Metathesaurus CUI : CL1405381;
Origin ID : C171151;
UMLS CUI : C5417847;
Semantic type(s)
- concept_is_in_subset
- has_target
