PXR-modulating chemicals
| Chemical IDs | Activator/Repressor | Species | Reference | ||
|---|---|---|---|---|---|
| Exogenous molecules | Drugs | Rifampicin | Activator and ligand | Human | (Blumberg et al., 1998; Li and Chiang, 2005; Li and Chiang, 2006) |
| RU486 | Activator | Human | (Banerjee et al., 2015; Kliewer, 2015; | ||
| Etomidoline | Activator | Human | Lynch et al., 2021) | ||
| Clotrimazole | Activator | Human, weak activatorin rodent | (Jones et al., 2000; Lehmann et al., 1998; Banerjee et al., 2015; Kliewer, 2015) | ||
| Colfibrate | Activator and ligand | Rat | (Daujat-Chavanieu and Gerbal-Chaloin, 2020) | ||
| Phenobarbital | Activator | Human | (Li et al., 2019; Tamasi et al., 2009) | ||
| Dexamethasone | Activator | Human androdent | (Pascussi et al., 2001; Yueh et al., 2005; Pascussi et al., 2000; Shi et al., 2010) | ||
| Cyclophosphamide (CPA) | Activator | Human | (Lindley et al., 2002; Zhuo et al., 2014) | ||
| Ritanovir | Activator | Human | (Chang and Waxman, 2006; Shehu et al., 2019; Brewer and Chen, 2016) | ||
| Paclitaxel | Activator | Human | (Kostrubsky et al., 1998) | ||
| Felodipine | Activator | Human | (Dybdahl et al., 2012; Pinne et al., 2016) | ||
| Nifedipine | Activator | Human | (Bertilsson et al., 1998; Chang and Waxman, 2006; Lynch et al., 2021) | ||
| Bendipine | Activator | Human | (Bertilsson et al., 1998; Chang and Waxman, 2006; Lynch et al., 2021) | ||
| Carbamazepine | Activator | Human | (El-Sankary et al., 2001; Luo et al., 2002) | ||
| Bosentan | Activator | Human | (van Giersbergen et al., 2002) | ||
| Mevastatin | Activator | Human | (Raucy et al., 2002) | ||
| Tamoxifen | Activator | Human | (Desai et al., 2002; Zhuo et al., 2014) | ||
| Topotecan | Activator | Human | (Schuetz et al., 2002) | ||
| Lacidipine | Activator | Human | (Bertilsson et al., 1998; Chang and Waxman, 2006; Lynch et al., 2021) | ||
| Resveratrol | Inhibitor | Human | (Smutny and Pavek, 2014), (Deng et al., 2014) | ||
| Ketoconazole | Inhibitor | Human | (Mani et al., 2013; Huang et al., 2007) | ||
| Exogenous molecules | Drugs | ET-743 | Inhibitor | Human | (Synold et al., 2001) |
| SPA70 | Inhibitor | Human | (Lin et al., 2017) | ||
| Phytochemicals | St. John’s wort (hyperforin) | Activator | Human | (Watkins et al., 2003; Kliewer, 2015) | |
| Forskolin | Activator | Human, mouse | (Seamon et al., 1981; Ding and Staudinger, 2005a) | ||
| Guggulsterones | Activator | Human, mouse | (Chang and Waxman, 2006; Brobst et al., 2004; Ding and Staudinger, 2005b) | ||
| Artemisinin | Activator | Human | (Burk et al., 2005) | ||
| Kava extract | Activator | Human | (Raucy, 2003), (Ma et al., 2004) | ||
| Coumestrol | Repressor | Human and humanized mouse | (Wang et al., 2008) | ||
| Sulforaphane | Repressor | Human | (Zhou et al., 2007) | ||
| Schiandrol B (SolB) | Activator | Human | (Zeng et al., 2017) | ||
| Environmental chemicals | Bisphenol A (BPA) | Activator | Human | (Sui et al., 2012; Barrett, 2012) | |
| PBDEs | Activator | Human, rodents | (Pacyniak et al., 2007; Sueyoshi et al., 2014) | ||
| PCBs | Activator | Human, rodents | (Egusquiza et al., 2020; Wahlang et al., 2014; Jacobs et al., 2005) | ||
| PFOA | Activator | Rodents | (Bjork et al., 2011; Ren et al., 2009) | ||
| PFOS | Activator | Human, rodents | (Bjork et al., 2011; Ren et al., 2009) | ||
| Phthalate monoesters | Activator | Human, rodents | (Hurst and Waxman, 2004; Cooper et al., 2008) | ||
| Metal ions (Pb+, Ag+), As | Activator | Zebrafish, humanized mouse | (Liu et al., 2019; Medina-Diaz et al., 2009) | ||
| Uranium | Activator | Rat | (Souidi et al., 2005) | ||
| Exogenous molecules | Pesticides | Chlordane (trans-nonachlor) | Activator | Human | (Jacobs et al., 2005) |
| Alachlor | Activator | Human, rat | (Mikamo et al., 2003; Lemaire et al., 2006) | ||
| Nonylphenol | Activator | Fish | (Meucci and Arukwe, 2006) | ||
| Cis-bifenthrin | Activator | Human | (Xiang et al., 2018) | ||
| DDT | Activator | Human, mouse | (Lemaire et al., 2004) | ||
| Dieldrin | Activator | Human | (Milnes et al., 2008) | ||
| Cholpyrifos | Activator | Mouse | (Lemaire et al., 2004) | ||
| Cypermethrine | Activator | Human | (Lemaire et al., 2004; Abass et al., 2012) | ||
| Endosulfan | Activator | Human | (Lemaire et al., 2004; Coumoul et al., 2002) | ||
| Dane | Activator | Human, rat | (Lemaire et al., 2004; Mikamo et al., 2003) | ||
| Methoxychlor | Activator | Human, rat | (Lemaire et al., 2004; Mikamo et al., 2003; Lemaire et al., 2006) | ||
| Miscellaneous | CITCO | Activator | Humans | (Lin et al., 2020) | |
| SR12813 | Activator | Human, rabbit, canine | (Jones et al., 2000; Pinne et al., 2016) | ||
| Pregnenolone 16Chlorpyrifosile (PCN) | Activator and ligand | Rodents | (Ma et al., 2008; Marek et al., 2005) | ||
| FKK6 | Activator and ligand | Human, mouse | (Dvořák et al., 2020) | ||
| Food components | Aflatoxin B1 | Activator | Human | (Ayed-Boussema et al., 2012a; Daujat-Chavanieu and Gerbal-Chaloin, 2020) | |
| Patulin | Activator | Human | (Ayed-Boussema et al., 2012b) | ||
| Isorhamnetin | Activator and ligand | Mouse | (Dou et al., 2014) | ||
| High fat diet | Activator | Mouse | (Saraswathi et al., 2017) | ||
| Alpha-ketoglutarate | Activator | Pig | (He et al., 2017) | ||
| Ochratoxin A | Inhibitor | Human | (Doricakova and Vrzal, 2015; Daujat-Chavanieu and Gerbal-Chaloin, 2020) | ||
| Vitamins | Vit K | Activator and ligand | Mouse | (Sultana et al., 2018; Tabb et al., 2003; Avior et al., 2015) | |
| Vit E | Activator | Human | (Landes et al., 2003) | ||
| Endogenous molecules | Microbial metabolites | Lithocholic acid (LCA) | Activator | Human, rodents | (Wistuba et al., 2007; Staudinger et al., 2001) |
| 3-keto LCA | Activator | Human, rodents | (Xie et al., 2001; Staudinger et al., 2001) | ||
| Deoxycholic acid (DCA) | Activator | Mouse | (Xie et al., 2001) | ||
| Indole-3-propionic acid | Ligand and activator | Human, mouse | (Venkatesh et al., 2014) | ||
| Skatole (3-methyl-indole) | Partial agonist and low affinity ligand | Human | (Vyhlidalova et al., 2020) | ||
| Lipopolysaccharides (LPS) | Inhibitor | Mouse | (Xu et al., 2004; Xu et al., 2005) |