Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons, and regulates xenobiotic-metabolizing enzymes such as cytochrome P450s, most notably cyp 1A1.
Aryl Hydrocarbon Receptor is a member of the family of basic helix-loop-helix transcription factors. AhR binds several exogenous ligands including natural plant flavonoids, polyphenolics and indoles, as well as synthetic polycyclic aromatic hydrocarbons and dioxin-like compounds. AhR is a cytosolic transcription factor that is normally inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleus and dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.
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CH-223191 is a potent, specific antagonist of AhR (aryl hydrocarbon receptor), potently inhibits TCDD-induced AhR-dependent transcription with IC50 of 0.03 uM; shows more inhibitory potency and no agonist-like effect, compared with flavone, resveratrol, and α-naphthoflavone, as well as estrogenic potency; inhibits TCDD-AhR binding and TCDD-induced nuclear translocation and DNA binding of AhR, prevents the expression of cytochrome P450 enzymes, target genes of the AhR; potently prevents TCDD-elicited cytochrome P450 induction, liver toxicity, and wasting syndrome in mice
CAY10465 is an analog of resveratrol acting as a potent and selective aryl hydrocarbon receptor agonist, with a Ki of 0.2 nM. CAY10465 is inactive as a ligand for the estrogen receptor even at 100 µM.
PDM2 is a selective, high-affinity aryl hydrocarbon receptor (AhR) antagonist with an Ki of 1.2±0.4 nM.
FICZ is a high affinity aryl hydrocarbon receptor (AhR) agonist with Kd of 70 pM; induces transient expression of CYP1A1 in vitro, and potentiates NK cell IFN-γ production and cytolytic activity; enhances NK cell control of tumors in an NK cell- and AhR-dependent manner in vivo; an endogenous AhR ligand.
TCDD is a potent AHR (aryl hydrocarbon receptor) agonist that induces degradation of AhR by the ubiquitin-proteasome pathway; suppresses the transcription of PEPCK and decreases Sirtuin 1 activation of PGC1α; also blocks cNK development and supports group 3 innate lymphoid cell (ILC3) differentiation.
ITE is a endogenous ligand, potent aryl hydrocarbon receptor (AhR) agonist in vitro; activates the murine AhR in vivo, but does not induce toxicity; induces the differentiation of stem-like cancer cells and reduces their tumorigenic potential in both subcutaneous and orthotopic xenograft tumour models.
BAY-2335218 is an aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2017202816A1, example 23, has an IC50 of 39.9 nM in human cell line.
5F 203 is a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway; causes MCF-7 sensitive cells to arrest in G(1) and S phase, and induces DNA adduct formation, in contrast to AhR-deficient AH(R100) variant MCF-7 cells, induces CYP1A1 and CYP1B1 transcription; L-lysylamide prodrug Phortress (NSC 710305) demonstrats antitumor activity in vivo.
The L-lysylamide prodrug of 5F-203 (NSC703786), a potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway; causes MCF-7 sensitive cells to arrest in G(1) and S phase, and induces DNA adduct formation, in contrast to AhR-deficient AH(R100) variant MCF-7 cells, induces CYP1A1 and CYP1B1 transcription; demonstrats antitumor activity in vivo.
NK150460 is a potent and selective inhibitor of breast cancer cells via activation the aryl hydrocarbon receptor (AhR) pathway; inhibits growth of not only most ER-positive, but also some ER-negative breast cancer cell lines, while never inhibiting growth of non-breast cancer cell lines; inhibits 17β-estradiol (E2)-dependent transcription without affecting binding of E2 to ER; does not induce histone H2AX phosphorylation or p53 expression, is a a novel AhR agonist dependent on AhR/ARNT and cytochrome P450 CYP1A1.
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