Organic anion transporting polypeptide 1A2 (OATP1A2)

Organic anion transporting polypeptide 1A2 (OATP1A2) is a membrane transporter belonging to the solute carrier organic anion transporter family. It mediates sodium-independent cellular uptake of a broad range of endogenous compounds—including bile acids, conjugated steroids, thyroid hormones—and many xenobiotics such as statins and antihistamines. Expressed widely across tissues including the intestine, liver cholangiocytes, brain, kidney, lung, testis and placenta, it plays a key role in drug absorption from the gut as well as hormone regulation at barrier sites like the blood-brain barrier and placenta. Its activity can be modulated by genetic variation, nuclear receptors such as PXR, bile acid levels, pH conditions, food components like fruit juice, and various drugs that act as substrates or inhibitors. Altered expression has been linked to cancer progression—especially breast cancer—and fetal-maternal transport disorders such as intrahepatic cholestasis of pregnancy.

Other names

OATPOATP-ASLC21A3SLCO1A2

Drugs interact with OATP1A2 primarily by being transported into cells via this protein or by inhibiting its function, thereby altering drug absorption, distribution, or elimination. Inhibition can reduce oral bioavailability for some drugs.