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. 2012 Spring;9(1):e49-e55.
doi: 10.1016/j.ddtec.2011.07.004.

Beyond Cell Penetrating Peptides: Designed Molecular Transporters

Paul A Wender  1 , Christina B Cooley, Erika I Geihe
Affiliations

Beyond Cell Penetrating Peptides: Designed Molecular Transporters

Paul A Wender et al. Drug Discov Today Technol. 2012 Spring.

Abstract

Inspired originally by peptides that traverse biological barriers, research on molecular transporters has since identified the key structural requirements that govern cellular entry, leading to new, significantly more effective and more readily available agents. These new drug delivery systems enable or enhance cellular and tissue uptake, can be targeted, and provide numerous additional advantages of significance in imaging, diagnostics and therapy.

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Figures

Figure 1
Figure 1
Representative examples of GR-MoTrs.
Figure 2
Figure 2
Schematic of synthetic approaches to GR-MoTrs and step count considerations. a) solid-phase synthesis, b) segment-doubling approach for homooligomers [41], c) oligomerization approach [46], d) table of step count comparison for the syntheses of different length oligomeric GR-MoTrs, G = guanidinium containing unit.
Figure 3
Figure 3
Syntheses and structures of oligomerization-based GR-MoTrs. a),b) ROMP oligomerizations [42, 44], c) organocatalytic carbonate oligomerization [46].
See this image and copyright information in PMC

References

    1. Wender PA, Galliher WC, Goun EA, Jones LR, Pillow TH. The design of guanidinium-rich transporters and their internalization mechanisms. Adv Drug Delivery Reviews. 2008;60:452–472. - PMC - PubMed
    1. Tung CH, Weissleder R. Arginine-containing peptides as delivery vectors. Adv Drug Delivery Reviews. 2003;55:281–294. - PubMed
    1. Wender PA, Mitchell DJ, Pattabiraman K, Pelkey ET, Steinman L, Rothbard JS. The design, synthesis, and evaluation of molecules that enable or enhance cellular uptake: peptoid molecular transporters. Proc Natl Acad Sci USA. 2000;97:13003–13008. - PMC - PubMed
    1. Wender PA, Verma VA, Paxton TJ, Pillow TH. Function oriented synthesis, step economy, and drug design. Acc Chem Res. 2008;41:40–49. - PubMed
    1. Torchilin VP. Tat peptide-mediated intracellular delivery of pharmaceutical nanocarriers. Adv Drug Delivery Reviews. 2008;60:548–558. - PubMed

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