Liver transporters play an important role in the pharmacokinetics and disposition of
pharmaceuticals, environmental contaminants, and endogenous compounds. Among them, the
family of ATP-Binding Cassette (ABC) transporters is the most important due to its role in
the transport of endo- and xenobiotics. The ABCC sub-family is the largest one, consisting of
13 members that include the cystic fibrosis conductance regulator (CFTR/ABCC7); the sulfonylurea
receptors (SUR1/ABCC8 and SUR2/ABCC9) and the multidrug resistanceassociated
proteins (MRPs). The MRP-related proteins can collectively confer resistance to
natural, synthetic drugs and their conjugated metabolites, including platinum-containing compounds,
folate anti-metabolites, nucleoside and nucleotide analogs, among others. MRPs can
be also catalogued into "long" (MRP1/ABCC1, -2/C2, -3/C3, -6/C6, and -7/C10) and "short"
(MRP4/C4, -5/C5, -8/C11, -9/C12, and -10/C13) categories. While MRP2/ABCC2 is expressed
in the canalicular pole of hepatocytes, all others are located in the basolateral membrane.
In this review, we summarize information from studies examining the changes in expression
and regulation of the basolateral hepatic transporter MPR3/ABCC3 by xenobiotics
and during various pathophysiological conditions. We also focus, primarily, on the consequences
of such changes in the pharmacokinetic, pharmacodynamic and/or toxicity of different
drugs of clinical use transported by MRP3.