Hepatic uptake of estradiol-3-glucuronide and estradiol-3-sulfate-17β-glucuronide by human organic anion transporting polypeptides 1B1, 1B3, and 2B1.

ABSTRACT: Estradiol is the most potent and biologically active form of estrogen, with glucuronide as its predominant conjugation form. Major estradiol glucuronides include estradiol-3-glucuronide (E₂3G), estradiol-17β-glucuronide, and estradiol-3-sulfate-17β-glucuronide (E₂3S17βG). Hepatic disposition of estradiol-17β-glucuronide involves basolateral uptake transporters organic anion transporting polypeptide (OATP) 1B1/1B3 and apical efflux transporters multidrug resistance-associated protein 2 (MRP2)/breast cancer resistance protein (BCRP). In addition, E₂3G and E₂3S17βG are substrates for MRP2/BCRP. However, whether E₂3G and E₂3S17βG across the basolateral membrane of hepatocytes are transporter-mediated and which transporters play

SUBMITTER: Li L 

PROVIDER: S-EPMC12597597 | biostudies-literature | 2025 Sep

REPOSITORIES: biostudies-literature