The role of OATP1A1 in cholestasis and drug-induced toxicity: a systematic review

Abstract OATP1A1 is the first and founding member of the Organic anion transporting polypeptides (OATPs) family. OATP1A1 is usually considered to mediate the cellular uptake of endogenous and xenobiotics, such as bile acids, drugs and environmental toxins. However, some new research indicated that the decrease of Oatp1a1 expression can result in the cholestasis, which was confirmed by clinic case of drug-induced cholestatic liver injury and bile duct ligation surgery or Oatp1a1-null mice models. These results suggested that Oatp1a1 does not simply transport bile acids to hepatocytes, as is commonly believed. In this overview, we summarized the advances of OATP1A1 in drug induced toxicity, cholestasis and other pathological states as well as the differences of Oatp1a1 in different gender and age.