Cell penetration properties

The lack of direct proportionality between the MIC values and the gyrase inhibition values is suggested reasonably to be related to varying relative cell-penetrating properties of the different agents. Thus, enoxacin would appear... 

Ruoslahti E, Duza T, Zhang L (2005) Vascular homing peptides with cell-penetrating properties. CurrPharm Des 11 3655-3660... 

A 27 amino acid chimeric peptide with cell-penetrating properties. See Cell-Penetrating Peptides. See Pooga, M., Hallbrink, M., Zorko, M., and Lan-gel, ti.. Cell penetration by transportan, FASEB J. 12, 67-77,1998 Padiri, K., Saalik, P, Hansen, M. et al.. Cell transduction pathways of transpor-tans, Biooconjugate Chem. 16, 1399-1410, 2005. 

The cellular membrane is a hydrophobic barrier that surrounds the cytoplasm of every cell and is involved in complex cellular processes, such as signaling and transport, which are essential to maintain the normal life cycle of a cell major components of this cellular membrane are lipids, proteins, peptides, and carbohydrates. Peptides that interact with cellular membranes are referred to as membrane-active peptides and can be broadly divided into three major classes antimicrobial, cell-penetrating, and fusogenic peptides. Any of these may have variable lengths, hydrophobicities, and secondary structures, but they often exhibit similar effects on membranes. For example, some antimicrobial peptides have cell-penetrating properties, and vice versa [23,24] these peptides usually cause some degree of membrane destabilization. 

The major difference between peptides and peptoids lies in the fact that the side chain substituents R -R in peptoids are attached to the amide nitrogens, thus avoiding the chiral a-centres of a peptide. There are no NH-bonds present in peptoids which has major implications on solubility, cell penetration properties and on the overall conformations which differ significantly from those of peptides. In addition, compared to peptides, peptoids show an increased protease stability due to the tertiary amide bond. 

Sisson, A. L., D. Steinhilber, et al. (2009). Biocompatible functionalized polyglycerol microgels with cell penetrating properties. Angew Chem IntEd Engl 48(41) 7540— 7545. 

The development of MRFT specific inhibitors faces immense problems as MRPl substrates and inhibitors show anionic properties, which lack good cell penetration properties (Schinkel Jonker, 2003). 

Polymers carrying a positively charged site and a lipophile may display antibacterial and cell penetration properties [87-93]. The present synthetic design... 

Phosphonium groups were also attached to a polypeptide. In particular, the synthesis, characterisation and cell-penetrating properties of a tributylphosphonium-tagged polymer were described by Cheng and co-workers. The preparation of a polysiloxane functionalised via a... 

Understanding the Cell Penetration Properties of Macrocyclic a-Helical Peptides... 

Unquestionably, there is significant interest in understanding the cell penetration properties of macrocyclic a-helical peptides. Such work is now the focus of ongoing basic research that will leverage sophisticated biochemical, cellular and biophysical methods to address the complexity of molecular mechanisms involved in cell penetration by stapled peptides. For example, highly potent macrocyclic a-helical peptides such as the stapled peptide ATSP-7041 provide opportunistic tool molecules to interrogate cell penetration relative to cellular uptake mechanisms and peptide biophysical properties, including the establishment of benchmarks and standardized procedures. 

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