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How the exploration of the chemical space of cell-penetrating peptides helps to understand their functionality

Sofie Stalmans (UGent) , Evelien Wynendaele (UGent) and Bart De Spiegeleer (UGent)
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Abstract
Cell-penetrating peptides (CPPs) gained in recent years a lot of interest in the applied biomedical research field because of their ability to cross cellular barriers without causing significant lethal membrane damage. They have already been successfully applied to bring cell-impermeable cargoes into the cell interior. However, to date, only limited applications have reached the clinical phase of drug development. Currently, harmonization is needed in the cellular uptake studies of CPPs in order to efficiently draw reliable conclusions on their uptake mechanisms and structural properties. Therefore, we explored the chemical space of representative CPPs using chemo-molecular descriptors, which numerically express their chemical properties. Together with a newly defined cell-penetrating (CP) response for cellular influx, calculated using available quantitative cellular uptake data, the chemo-molecular descriptors were used to clarify which structural characteristics of the CPPs influence to what extent their cell-penetrating properties.[1] Our study indicated that CPPs are a chemically and CP-functionally diverse group of peptides.[1] Moreover, the newly defined CP-response and subgroups of CPPs help to select representative model peptides for further investigating their functionalities like e.g. uptake mechanisms and behaviour at different membrane interfaces, like the blood-brain barrier.[2] Another application of the exploration of the chemical space of the CPPs, is to investigate their chemical and functional relationship with the antimicrobial peptides, which are historically investigated as a separate peptide group.[3] References 1. S. Stalmans et al. Plos One. (2013), 8, e71752. 2. S. Stalmans et al. (submitted, 2014) 3. S. Stalmans et al. Protein Peptide Lett (2014), 21, 399-406.
Keywords
cellular uptake, Cell-penetrating peptides, multivariate data analysis, arginine, QSPR, lysine, unified response.

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Chicago
Stalmans, Sofie, Evelien Wynendaele, and Bart De Spiegeleer. 2014. “How the Exploration of the Chemical Space of Cell-penetrating Peptides Helps to Understand Their Functionality.” In Bioactive Peptides, 14th Naples Workshop, Abstracts.
APA
Stalmans, S., Wynendaele, E., & De Spiegeleer, B. (2014). How the exploration of the chemical space of cell-penetrating peptides helps to understand their functionality. Bioactive Peptides, 14th Naples workshop, Abstracts. Presented at the 14th Naples workshop on Bioactive Peptides.
Vancouver
1.
Stalmans S, Wynendaele E, De Spiegeleer B. How the exploration of the chemical space of cell-penetrating peptides helps to understand their functionality. Bioactive Peptides, 14th Naples workshop, Abstracts. 2014.
MLA
Stalmans, Sofie, Evelien Wynendaele, and Bart De Spiegeleer. “How the Exploration of the Chemical Space of Cell-penetrating Peptides Helps to Understand Their Functionality.” Bioactive Peptides, 14th Naples Workshop, Abstracts. 2014. Print.
@inproceedings{4418782,
  abstract     = {Cell-penetrating peptides (CPPs) gained in recent years a lot of interest in the applied biomedical research field because of their ability to cross cellular barriers without causing significant lethal membrane damage. They have already been successfully applied to bring cell-impermeable cargoes into the cell interior. However, to date, only limited applications have reached the clinical phase of drug development. Currently, harmonization is needed in the cellular uptake studies of CPPs in order to efficiently draw reliable conclusions on their uptake mechanisms and structural properties. Therefore, we explored the chemical space of representative CPPs using chemo-molecular descriptors, which numerically express their chemical properties. Together with a newly defined cell-penetrating (CP) response for cellular influx, calculated using available quantitative cellular uptake data, the chemo-molecular descriptors were used to clarify which structural characteristics of the CPPs influence to what extent their cell-penetrating properties.[1] 
Our study indicated that CPPs are a chemically and CP-functionally diverse group of peptides.[1] Moreover, the newly defined CP-response and subgroups of CPPs help to select representative model peptides for further investigating their functionalities like e.g. uptake mechanisms and behaviour at different membrane interfaces, like the blood-brain barrier.[2] Another application of the exploration of the chemical space of the CPPs, is to investigate their chemical and functional relationship with the antimicrobial peptides, which are historically investigated as a separate peptide group.[3]    
References
1. S. Stalmans et al.  Plos One. (2013), 8, e71752.
2. S. Stalmans et al. (submitted, 2014)
3. S. Stalmans et al.  Protein Peptide Lett (2014), 21, 399-406.},
  author       = {Stalmans, Sofie and Wynendaele, Evelien and De Spiegeleer, Bart},
  booktitle    = {Bioactive Peptides, 14th Naples workshop, Abstracts},
  keywords     = {cellular uptake,Cell-penetrating peptides,multivariate data analysis,arginine,QSPR,lysine,unified response.},
  language     = {eng},
  location     = {Naples, Italy},
  title        = {How the exploration of the chemical space of cell-penetrating peptides helps to understand their functionality},
  year         = {2014},
}