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. 2019 Jan 4;10(2):203–208. doi: 10.1021/acsmedchemlett.8b00551

Figure 3.

Figure 3

(a) Structure and key properties of compound 28. (b,c) Selectivity profile of 3 and optimized derivative 28 on 12 nuclear receptors related to RXRs at 30 μM. Although 3 also activates RAR, 28 gained full RXR selectivity. n ≥ 3. (d, e) 28 activated permissive RXR heterodimers with (d) PPAR and (e) LXR in full-length assays showing synergistic effects with the respective partner agonists rosiglitazone (Rosi) and T0901317 (T090); (d) n = 3, (e) n = 4. (f) 28 induced RXR-regulated gene expression (qRT-PCR) of adiponectin (ADIPOQ), angiopoietin-like 4 (ANGPTL4), and apolipoprotein E (APOE) with similar efficacy as bexarotene (1, Bex). n = 4. All values are mean ± SEM; ∗ p < 0.05; ∗∗ p < 0.01; ∗∗∗ p < 0.001.