Protein kinase C restricts transport of carnitine by amino acid transporter ATB(0,+) apically localized in the blood-brain barrier

Arch Biochem Biophys. 2014 Jul 15:554:28-35. doi: 10.1016/j.abb.2014.05.006. Epub 2014 May 10.

Abstract

Carnitine (3-hydroxy-4-trimethylammoniobutyrate) is necessary for transfer of fatty acids through the inner mitochondrial membrane. Carnitine, not synthesized in the brain, is delivered there through the strongly polarized blood-brain barrier (BBB). Expression and presence of two carnitine transporters - organic cation/carnitine transporter (OCTN2) and amino acid transporter B(0,+) (ATB(0,+)) have been demonstrated previously in an in vitro model of the BBB. Due to potential protein kinase C (PKC) phosphorylation sites within ATB(0,+) sequence, the present study verified effects of this kinase on transporter function and localization in the BBB. ATB(0,+) can be regulated by estrogen receptor α and up-regulated in vitro, therefore its presence in vivo was verified with the transmission electron microscopy. The analyses of brain slices demonstrated ATB(0,+) luminal localization in brain capillaries, confirmed by biotinylation experiments in an in vitro model of the BBB. Brain capillary endothelial cells were shown to control carnitine gradient. ATB(0,+) was phosphorylated by PKC, what correlated with inhibition of carnitine transport. PKC activation did not change the amount of ATB(0,+) present in the apical membrane of brain endothelial cells, but resulted in transporter exclusion from raft microdomains. ATB(0,+) inactivation by a lateral movement in plasma membrane after transporter phosphorylation has been postulated.

Keywords: Amino acid transporter (ATB(0,+)); Blood–brain barrier; Organic cation transporter (OCTN2); Protein kinase C; l-Carnitine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Transport, Active
  • Blood-Brain Barrier / metabolism*
  • Brain / blood supply
  • Brain / metabolism
  • Brain / ultrastructure
  • Carnitine / metabolism*
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism
  • Male
  • Membrane Microdomains / metabolism
  • Microscopy, Electron, Transmission
  • Models, Neurological
  • Neurotransmitter Transport Proteins / metabolism*
  • Organic Cation Transport Proteins / metabolism
  • Phosphorylation
  • Protein Kinase C / metabolism*
  • Rats
  • Rats, Wistar
  • Solute Carrier Family 22 Member 5
  • Tetradecanoylphorbol Acetate / pharmacology

Substances

  • Neurotransmitter Transport Proteins
  • Organic Cation Transport Proteins
  • Slc22a5 protein, rat
  • Slc6a14 protein, rat
  • Solute Carrier Family 22 Member 5
  • Protein Kinase C
  • Tetradecanoylphorbol Acetate
  • Carnitine