Retinoid X Receptor-Antagonistic Diazepinylbenzoic Acids.

Efficient Induction of CCR9 on T Cells Requires Coactivation of Retinoic Acid Receptors and Retinoid X Receptors (RXRs): Exaggerated T Cell Homing to the Intestine by RXR Activation with Organotins

“…Thus, we tried to test the possibility that these DCs might also provide RXRactivating signals by using RXR antagonists. The potent RXR antagonist HX531 (1 mM) significantly suppressed CCR9 expression, but it is also known to inhibit RAR activation at high concentrations (51). In contrast, the specific, but relatively weak, RXR antagonist PA452 (52) did not significantly suppress CCR9 expression, even at 10 mM (Supplemental Fig.…”

N-(4-hydroxyphenyl) retinamide (4HPR) enhances TRAIL-mediated apoptosis through enhancement of a mitochondrial-dependent amplification loop in ovarian cancer cell lines

“…To investigate if the enhancement of TRAIL-mediated apoptosis requires retinoid receptor activation, two pan-antagonists, one blocking the RAR receptors (LE540) and the other blocking the RXR receptors (HX531), were tested in the A547 and AD10 cell lines. 36,37 Preincubation with these antagonists did not inhibit the enhancement in TRAIL-mediated apoptosis induced by 4HPR in the cell lines tested (A547 shown in Figure 3b and AD10 not shown). To demonstrate that the inhibitors block RAR-or RXR-mediated effects, we treated the A547 cell line with ATRA plus TRAIL in the presence or absence of both inhibitors.…”

Docosahexaenoic Acid Induces Adipose Differentiation-Related Protein through Activation of Retinoid X Receptor in Human Choriocarcinoma BeWo Cells

“…complexes with BSA as previously described. 9) To examine the effect of nuclear receptors, PA024 and HX630 (RXR agonist), 21,22) PA452 and HX531 (RXR antagonist), 23,24) GW1929 (PPARg agonist; Sigma), and GW9662 (PPARg antagonist; Alexis) were used. These reagents dissolved in dimethylsufoxide were added to the cells (10 ml DMSO/5 ml cell culture dish).…”