One of the hottest topics in epileptology: ABC proteins. Their inhibition may be the future for patients with intractable seizures

Neurol Res. 2008 Nov;30(9):920-5. doi: 10.1179/174313208X319116. Epub 2008 Jun 30.

Abstract

One of the new topics in epileptology is the ABC proteins, which seem to control whether or not anti-epileptic drugs (AEDs) can come in contact with and affect the epileptogenic areas that cause seizures. The goal of this report is to simplify the concepts involved in these proteins and then to review the progress made in the field, especially of one protein called P-glycoprotein (P-gp). First, the ABC proteins are reviewed, mainly P-gp, which appears to alter drug permeability (like an extra blood-brain barrier). The possibility is discussed that changes in P-gp are the result of many seizures; are caused by the AEDs, or truly reflect pharmacoresistance. The different locations where these changes can be seen include the endothelial cells, glia and also neurons. The polymorphism of P-gp, called C3435T, probably has little functional significance and finally the importance of inhibitors of P-g to reverse pharmacoresistance is emphasized. Tariquidar (XR9576) is likely to be a good candidate that appears to inhibit these proteins and therefore to allow the AEDs to control the intractable seizures that may account for nearly 40% of our patients.

Publication types

  • Review

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / physiology*
  • ATP-Binding Cassette Transporters / antagonists & inhibitors
  • ATP-Binding Cassette Transporters / genetics
  • ATP-Binding Cassette Transporters / physiology*
  • Animals
  • Blood-Brain Barrier / drug effects
  • Blood-Brain Barrier / metabolism
  • Brain / drug effects
  • Brain / metabolism
  • Brain / physiopathology
  • Drug Resistance, Multiple / genetics
  • Epilepsy / drug therapy
  • Epilepsy / genetics
  • Epilepsy / physiopathology*
  • Humans
  • Polymorphism, Single Nucleotide
  • Quinolines / therapeutic use

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • ATP-Binding Cassette Transporters
  • Quinolines
  • tariquidar