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. 2022 Apr;50(4):478–491. doi: 10.1124/dmd.121.000415

TABLE 1.

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)