Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1 It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km = 75 µM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2 In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transport via MRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) (E23G; Item No. 16155).2,3 E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2WARNING This product is not for human or veterinary use.
[1] D W LOE. ATP-dependent 17 beta-estradiol 17-(beta-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroids.[J]. The Journal of Biological Chemistry, 1996, 271 16: 9683-9689. DOI:
10.1074/jbc.271.16.9683[2] PHILLIP M GERK M V Wei Li. Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronide.[J]. ACS Applied Energy Materials, 2004: 1139-1145. DOI:
10.1124/dmd.104.000372[3] PHILLIP M GERK. Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholate.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 320 2: 893-899. DOI:
10.1124/jpet.106.106922
