Advanced search
1 file | 661.54 KB

Do cell-penetrating peptides cross the blood-brain barrier

Sofie Stalmans (UGent) , Evelien Wynendaele (UGent) , Nathalie Bracke (UGent) and Bart De Spiegeleer (UGent)
(2014) JOURNAL OF PEPTIDE SCIENCE. 20(suppl. 1). p.S211-S212
Author
Organization
Abstract
Cell-penetrating peptides (CPPs) are a chemically diverse group of peptides, able to cross cell membranes. In literature, several studies are available describing a successful coupling of a brain-impermeable compound to a CPP to transport the molecule across the blood-brain barrier (BBB). Quantitative kinetic BBB transport studies of cell-penetrating peptides are however not yet available. To characterize quantitatively the BBB behavior of CPPs, the in vivo BBB transport and the in vitro metabolic stability of a diverse set of CPPs was determined. The chemical-functional space of the CPPs was first explored using chemo-molecular descriptors and a newly defined cell-penetrating response [1]. Then, five chemically and functionally diverse CPPs were selected representing the CPP space. Their BBB influx and efflux was quantified, as well as their distribution to the brain capillaries and parenchyma. Furthermore, the in vitro metabolic stability of these CPPs in mouse serum and brain was determined to ensure the reliability of our BBB transport conclusions. Finally, preliminary results of the in-brain region distribution will be presented. Our results indicate that the investigated CPPs show divergent BBB transport kinetics, which may be explained by their structural difference and their mechanism of cellular influx.
Keywords
in vivo blood-brain barrier transport, QSPR., Cell-penetrating peptides, in vitro metabolic stability

Downloads

  • 2014-358c Poster Do CPPs cross the BBB - 33rd EPS Sofia 2014.pdf
    • full text
    • |
    • open access
    • |
    • PDF
    • |
    • 661.54 KB

Citation

Please use this url to cite or link to this publication:

Chicago
Stalmans, Sofie, Evelien Wynendaele, Nathalie Bracke, and Bart De Spiegeleer. 2014. “Do Cell-penetrating Peptides Cross the Blood-brain Barrier.” In Journal of Peptide Science, 20:S211–S212.
APA
Stalmans, S., Wynendaele, E., Bracke, N., & De Spiegeleer, B. (2014). Do cell-penetrating peptides cross the blood-brain barrier. JOURNAL OF PEPTIDE SCIENCE (Vol. 20, pp. S211–S212). Presented at the 33rd European Peptide Symposium.
Vancouver
1.
Stalmans S, Wynendaele E, Bracke N, De Spiegeleer B. Do cell-penetrating peptides cross the blood-brain barrier. JOURNAL OF PEPTIDE SCIENCE. 2014. p. S211–S212.
MLA
Stalmans, Sofie, Evelien Wynendaele, Nathalie Bracke, et al. “Do Cell-penetrating Peptides Cross the Blood-brain Barrier.” Journal of Peptide Science. Vol. 20. 2014. S211–S212. Print.
@inproceedings{5703199,
  abstract     = {Cell-penetrating peptides (CPPs) are a chemically diverse group of peptides, able to cross cell membranes. In literature, several studies are available describing a successful coupling of a brain-impermeable compound to a CPP to transport the molecule across the blood-brain barrier (BBB). Quantitative kinetic BBB transport studies of cell-penetrating peptides are however not yet available. To characterize quantitatively the BBB behavior of CPPs, the in vivo BBB transport and the in vitro metabolic stability of a diverse set of CPPs was determined.
The chemical-functional space of the CPPs was first explored using chemo-molecular descriptors and a newly defined cell-penetrating response [1]. Then, five chemically and functionally diverse CPPs were selected representing the CPP space. Their BBB influx and efflux was quantified, as well as their distribution to the brain capillaries and parenchyma. Furthermore, the in vitro metabolic stability of these CPPs in mouse serum and brain was determined to ensure the reliability of our BBB transport conclusions. Finally, preliminary results of the in-brain region distribution will be presented.
Our results indicate that the investigated CPPs show divergent BBB transport kinetics, which may be explained by their structural difference and their mechanism of cellular influx.},
  articleno    = {abstract P163},
  author       = {Stalmans, Sofie and Wynendaele, Evelien and Bracke, Nathalie and De Spiegeleer, Bart},
  booktitle    = {JOURNAL OF PEPTIDE SCIENCE},
  issn         = {1075-2617},
  keywords     = {in vivo blood-brain barrier transport,QSPR.,Cell-penetrating peptides,in vitro metabolic stability},
  language     = {eng},
  location     = {Sofia, Bulgaria},
  number       = {suppl. 1},
  pages        = {abstract P163:S211--abstract P163:S212},
  title        = {Do cell-penetrating peptides cross the blood-brain barrier},
  volume       = {20},
  year         = {2014},
}