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  CPP or cholesterol conjugation to antisense PNA for cellular delivery

Joshi, R., Mishra, R., Su, W., & Engelmann, J. (2008). CPP or cholesterol conjugation to antisense PNA for cellular delivery. In H. Lankinen, J. Vallivirta, T. Strandin, & J. Hepojoki (Eds.), Peptides 2008: Chemistry of Peptides in Life Science Technology and Medicine (pp. 550-551). Helsinki, Finland: FIPS.

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http://www.5z.com/30EPS/30EPS.pdf (Publisher version)
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 Creators:
Joshi, R1, 2, Author           
Mishra, R1, 2, Author           
Su, W1, 2, Author           
Engelmann, J1, 2, Author           
Affiliations:
1Former Department MRZ, Max Planck Institute for Biological Cybernetics, Max Planck Society, Spemannstrasse 38, 72076 Tübingen, DE, ou_2528700              
2Max Planck Institute for Biological Cybernetics, Max Planck Society, Spemannstrasse 38, 72076 Tübingen, DE, ou_1497794              

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 Abstract: Peptide nucleic acids (Proc Nat Acad Sci USA) are DNA
mimics consisting of the four common bases as in DNA
on a pseudopeptide backbone that makes them extremely
stable in biological fluids. Antisense PNA can be targeted
to mRNA in the cytoplasm in a complementary base
pairing manner. In order to achieve efficient mRNA based
targeting, endosomal release or direct uptake of
Proc Nat Acad Sci USA into the cytosol is mandatory. However,
relatively poor internalization of these agents is reported
for most cells.
1 Several reports suggested cell penetrating
peptide (CPP) based delivery systems for PNA delivery
into cells.
2 Unfortunately, endosomal capture seems to
be a major challenge in these approaches restricting the
ability of PNA to bind with mRNA. Recent studies have
explored the use of cholesterol-siRNA conjugates to
enhance cellular import.
3 In order to attain efficient PNA
internalization into cells, we synthesized two different
sequences of cholesterol coupled antisense PNA and
evaluated their uptake efficacy in comparison to a PNA-CPP conjugate previously reported by our group.

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 Dates: 2008-09
 Publication Status: Published in print
 Pages: -
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 Table of Contents: -
 Rev. Type: -
 Identifiers: BibTex Citekey: 6760
 Degree: -

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Title: Thirtieth European Peptide Symposium (Peptides 2008)
Place of Event: Helsinki, Finland
Start-/End Date: 2008-08-31 - 2008-09-05

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Title: Peptides 2008: Chemistry of Peptides in Life Science Technology and Medicine
Source Genre: Proceedings
 Creator(s):
Lankinen, H, Editor
Vallivirta, J, Editor
Strandin, T, Editor
Hepojoki, J, Editor
Affiliations:
-
Publ. Info: Helsinki, Finland : FIPS
Pages: 719 Volume / Issue: - Sequence Number: 4-19-122 Start / End Page: 550 - 551 Identifier: ISBN: 978-952-92-7697-4