TY - JOUR
T1 - Aryl hydrocarbon receptor agonists directly activate estrogen receptor α in MCF-7 breast cancer cells
AU - Liu, Shengxi
AU - Abdelrahim, Maen
AU - Khan, Shaheen
AU - Ariazi, Eric
AU - Jordan, V. Craig
AU - Safe, Stephen
N1 - Funding Information:
The financial assistance of the National Institutes of Health (ES04917, ES04176 and ES09106), Specialized Program of Research Excellence in Breast Cancer (P50-CA89018), and the Texas Agriculture Experiment Station are gratefully acknowledged.
PY - 2006/9/1
Y1 - 2006/9/1
N2 - The aryl hydrocarbon receptor (AhR) binds with high affinity to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and related halogenated aromatics, but also binds with lower affinity to structurally diverse exogenous and endogenous chemicals. One study reported that 3-methylcholanthrene (3MC) activated the estrogen receptor (ER) through the AhR, which acts as co-regulatory protein, whereas a recent report showed that 3MC directly bound and activated ERα. This study also shows that the AhR agonists benzo[a]pyrene, 3,3′,4,4′-tetrachlorobiphenyl, chrysin, 6-methyl-1,3,8-trichlorodibenzofuran, and 3,3′-diindolylmethane also induce ERα-dependent transactivation. Moreover, in chromatin immunoprecipitation assays, these compounds induce binding of AhR and ERα to the CYP1A1 and pS2 gene promoters, which is consistent with their activities as both selective AhR modulators (SAhRMs) and selective ER modulators (SERMs).
AB - The aryl hydrocarbon receptor (AhR) binds with high affinity to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and related halogenated aromatics, but also binds with lower affinity to structurally diverse exogenous and endogenous chemicals. One study reported that 3-methylcholanthrene (3MC) activated the estrogen receptor (ER) through the AhR, which acts as co-regulatory protein, whereas a recent report showed that 3MC directly bound and activated ERα. This study also shows that the AhR agonists benzo[a]pyrene, 3,3′,4,4′-tetrachlorobiphenyl, chrysin, 6-methyl-1,3,8-trichlorodibenzofuran, and 3,3′-diindolylmethane also induce ERα-dependent transactivation. Moreover, in chromatin immunoprecipitation assays, these compounds induce binding of AhR and ERα to the CYP1A1 and pS2 gene promoters, which is consistent with their activities as both selective AhR modulators (SAhRMs) and selective ER modulators (SERMs).
KW - AhR
KW - Estrogenicity
KW - Selective AhR modulators
KW - Transactivation
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U2 - 10.1515/BC.2006.149
DO - 10.1515/BC.2006.149
M3 - Article
C2 - 16972788
AN - SCOPUS:33748806035
SN - 1431-6730
VL - 387
SP - 1209
EP - 1213
JO - Biological Chemistry
JF - Biological Chemistry
IS - 9
ER -