The Transport of Choline

@article{Lockman2002TheTO,
  title={The Transport of Choline},
  author={Paul R. Lockman and David D. Allen},
  journal={Drug Development and Industrial Pharmacy},
  year={2002},
  volume={28},
  pages={749 - 771},
  url={https://api.semanticscholar.org/CorpusID:34402785}
}
This review article examines landmark and current choline transport studies, molecular mapping, and molecular identification of these carriers, and focuses on targeting the choline transporter in disease and use of this carrier as a drug delivery vector.
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163 Citations
Highly Influential Citations
6
Background Citations
61
Methods Citations
3
Results Citations
1

163 Citations

Cation Transport Specificity at the Blood–Brain Barrier

The molecular family of the blood–brain barrier (BBB) choline transporter may be elucidated in vitro by its interaction with physiologic thiamine levels, and two cationic transporters at the BBB may be responsible forThiamine brain uptake.

Inhibition of choline uptake by N-cyclohexylcholine, a high affinity ligand for the choline transporter at the blood–brain barrier

Five novel N-cycloalkyl derivatives of choline showed promising inhibition properties and a cyclohexyl moiety substituting one of the methyl groups attached to the cationic nitrogen in choline helped improve affinity for this transporter.

Impaired trafficking of choline transporter-like protein-1 at plasma membrane and inhibition of choline transport in THP-1 monocyte-derived macrophages.

Investigating choline transport processes and regulation of choline transporter-like protein-1 (CTL1) in human THP-1 monocytic cells and phorbol myristate 13-acetate (PMA)-differentiated macrophages reveals that CTL1 is the most plausible candidate that possesses the described kinetic and inhibitory properties.

Choline uptake in human intestinal Caco-2 cells is carrier-mediated.

Results indicate the presence of a carrier-mediated transport system for choline in Caco-2 cells, the substrate specificity of this carrier is unlike that seen in the rat intestinal epithelium, and the human transport protein is distinct from those for TEA and NMN.

The choline transporter-like family SLC44: properties and roles in human diseases.

Functional characterization of Na+-independent choline transport in primary cultures of neurons from mouse cerebral cortex

Functional expression of choline transporter like-protein 1 (CTL1) and CTL2 in human brain microvascular endothelial cells

Molecular and functional characterization of an Na+‐independent choline transporter in rat astrocytes

It is concluded that rat astrocytes express an intermediate‐affinity Na+‐independent choline transport system that seems to occur through a CTL1 and is responsible for the uptake of choline and organic cations in these cells.

Choline acetyltransferase and organic cation transporters are responsible for synthesis and propionate-induced release of acetylcholine in colon epithelium.

Active Transport of High-Affinity Choline and Nicotine Analogs into the Central Nervous System by the Blood-Brain Barrier Choline Transporter

It is hypothesized that the N-n-octyl group on the pyridinium nitrogen of NONI facilitates brain entry via the BBB choline transporter, and may have utility as a smoking cessation agent.
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173 References

Choline mustard: an irreversible ligand for use in studies of choline transport mechanisms at the cholinergic nerve terminal.

This mustard analogue did not inhibit synaptosomal uptake of 5-hydroxytryptamine, noradrenaline, or gamma-aminobutyric acid, thereby confirming further the specificity of this compound for the choline carrier.

Novel Choline Transport Characteristics in Caco-2 Cells

Choline transport across Caco-2 cells is demonstrated to be active and both pH- and Ca2+-dependent and has unique characteristics when compared to traditional choline transport models.

Choline transport into rat liver mitochondria. Characterization and kinetics of a specific transporter.

Characteristics of Choline Transport Across the Blood-Brain Barrier in Mice: Correlation with In Vitro Data

These in situ (in vivo) results corresponded well to the in vitro results and suggest that the choline transporter at the BBB is a member of the organic cation transporter (OCT) family.

Uptake and metabolism of [3H]choline mustard by cholinergic nerve terminals from rat brain

Transport of choline and its relationship to the expression of the organic cation transporters in a rat brain microvessel endothelial cell line (RBE4).

Pharmacological characteristics of choline transport system in mouse cerebral cortical neurons in primary culture.

The present results strongly suggest that the primary cultured neurons used in this study possess a sodium- and energy-dependent high-affinity choline uptake system as well as a synthesizing system for acetylcholine.

Inhibition of the rat blood–brain barrier choline transporter by manganese chloride

The results suggest that choline uptake into the CNS can be inhibited by divalent cationic metals and monovalent cations, and the choline transporter may be a means by which manganese enters the brain.

Blood–brain barrier choline transport in the senescent rat

Choline transport in rat liver basolateral plasma membrane vesicles

The findings demonstrate an electrogenic pathway on the sinusoidal membrane for the uptake of this essential nutrient and support the existence of multiple pathways for thesinusoidal uptake of endogenous and exogenous organic cations.
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