Table 3.
Chemical activators of DappuHR96 compared to mammalian CAR, PXR, and VDR.
| Chemical | HR96 | CAR# | PXR# | VDR# |
|---|---|---|---|---|
| Methyl farnesoate | ↔ | nd | nd | nd |
| Cortisol | ↔ | ↔ | ↑ | nd |
| Corticosterone | ↑ | ↑ | ↑ | nd |
| Androstanol | ↓ | ↓ | ↑ | nd |
| Estradiol | ↑ | ↑ | ↑ | nd |
| 20-hydroxyecdysone | ↔ | nd | nd | nd |
| Pyriproxyfen (JHA) | ↑ | nd | nd | nd |
| Triclosan | ↓ | ↑ | ↑ | nd |
| Atrazine | ↑ | nd | ↔ | nd |
| Chlorpyrifos | ↑ | ↑ | ↑ | nd |
| Parathion | ↔ | ↑ | nd** | nd |
| Bisphenol A | ↔ | ↑ | ↑ | nd |
| Lindane | ↔ | nd | ↑ | nd |
| M. Methyl Arsonate | ↑ | ↑ | nd | nd |
| Phenobarbital | ↓ | ↑ | ↑ | nd |
| 2,4-D | ↔ | nd | nd | nd |
| Fluoxetine | ↓ | nd | ↑ | nd |
| Methoxychlor | ↔ | ↑ | ↑ | nd |
| Nonylphenol | ↔ | ↑ | ↑ | nd |
| Cypermethrin | ↔ | ↑ | ↑ | nd |
| Cholesterol | ↔ | ↔ | ↔ | ↔ |
| Lithocholic acid | ↔ | ↑ | ↑ | ↑ |
| Chenodeoxycholic acid | ↔ | ↑ | ↑ | ↔ |
| Palmitic acid | ↔ | nd | nd | nd |
| Steric acid | ↔ | nd | nd | nd |
| Decanoic acid | ↓ | nd | nd | nd |
| Docosanoic acid | ↔ | nd | nd | nd |
| Linoleic acid (n-6) | ↑ | ↑ | ↔ | ↕** |
| Oleic acid (n-9) | ↑ | nd | nd | nd |
| Arachidonic acid (n-6) | ↔ | ? | ? | ↕** |
| Eicosapentaenoic acid (n-3) | ↓ | ? | ? | ↕** |
| Docasahexaenoic acid (n-3) | ↓ | ↓ | ↔ | ↕** |
| α-Linolenic acid (n-3) | ↓ | nd | nd | nd |
| Corn oil (n-6) | ↑ | nd$ | nd | nd |
Data compiled from the following references (Adachi et al., 2005; Antolino-Lobo et al., 2011; Baldwin and Roling, 2009; Haussler et al., 2008; Hernandez et al., 2009; Ishizawa et al., 2008; Kliewer et al., 1998; Kretschmer and Baldwin, 2005; Lemaire et al., 2004; Lemaire et al., 2006; Staudinger et al., 2001; Yu et al., 2011; Zhang et al., 2004)
nd = not determined or not determined based on our literature searches
↔ = no effect
↓ = inverse agonist, antagonist, or inhibitor of activity
↑ = activator
Data obtained from binding assays so the directional effects (agonists, inverse agonists, antagonists) of these unsaturated fatty acids on VDR activity are unknown (Haussler et al., 2008).
? Whether these polyunsaturated fatty acids activate or inactivate CAR and PXR is unknown; however, there is evidence that they modulate activity and expression (Kuan et al., 2011)
nd** Methyl parathion is not an activator of PXR (Lemaire et al., 2004)
nd$ Linoleic acid, the major PUFA in corn oil is an activator of CAR (Finn et al., 2009)