"Expression versus Function of ABC Transporters at the Blood-Brain Barrier".
I am Jean-Michel Scherrmann,
I am professor of Pharmacokinetics at
the Faculty of Pharmacie of Paris Descartes University.
During my presentation, I will give
some general properties on the ABC transporters and on the blood-brain barrier.
I will describe P-glycoprotein or ABCB1, BCRP,
or ABCG2, and the multi-drug resistant proteins,
the MRPs at the level of the blood-brain barrier.
In the last part, I will report our data on the gene and
protein expression of this ABC in the human brain microvessels.
And finally, I will conclude my presentation by
the impact that these ABC transporters in the blood-brain barrier can have,
in the research and development of central nervous system drugs.
The ABC transporters belong to a superfamily with 48 reported genes in humans.
Four subfamilies, A, B, C,
and G contain several isoforms,
which are implied in drug transport.
The most known is a full transporters ABCB1 or P-glycoprotein,
which is mostly expressed in the plasma membrane,
but also in some sub-cellular sites,
like other ABC proteins.
This raises the question of
the ABC transporter role in the intracellular drug disposition.
Nevertheless, the subfamily D, E,
and F do not seem involved in
the transport and expressed at the level of the blood-brain barrier.