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Adenosine triphosphate-dependent transport of estradiol-17?(?-d-glucuronide) in membrane vesicles by MDR1 expressed in insect cells by Liyue Huang; Tim Hoffman; Dr. Mary Vore is a Medicine article available to read on EtoBox.

What is Adenosine triphosphate-dependent transport of estradiol-17?(?-d-glucuronide) in membrane vesicles by MDR1 expressed in insect cells about?

MDR1, an ABC transporter that confers multidrug resistance in tumor cells, is constitutively expressed in normal liver canalicular membrane. Human MDR1-expressing multidrug-resistant cells display increased resistance to estradiol-17beta(beta-D-glucuronide) (E217G). MDR1 substrates/modulators inhibit adenosine triphosphate (ATP)-dependent transport of E217G in the rat canalicular membrane and protect against E217G-mediated cholestasis in isolated perfused rat liver. The present studies were designed to determine if E217G is a substrate for MDR1 using a baculovirus expression system and if other estrogen glucuronides interact with MDR1. ATP-dependent transport of E217G (10 micromol/L) was linear for up to 2 minutes and yielded a rate of 45.6 pmol/min/mg protein in membrane vesicles from Sf9 cells infected with MDR1-baculovirus. This transport was saturable (Km = 62 micromol/L) and occurred into an osmotically sensitive space. ATP-dependent transport of E217G (10 micromol/L) was inhibited 63% by 10 micromol/L daunomycin, but not by 100 micromol/L S-(2,4-dinitrophenyl)glutathione (GS-DNP) (a substrate for canalicular multispecific organic anion transporter [cMOAT]). Glucuronide conjug

Who reads Adenosine triphosphate-dependent transport of estradiol-17?(?-d-glucuronide) in membrane vesicles by MDR1 expressed in insect cells?

Author

Liyue Huang; Tim Hoffman; Dr. Mary Vore

Publisher

Ovid Technologies (Wolters Kluwer Health)

Published

1998

Language

EN

Field

Medicine (Health Sciences)