Universität zu Köln

Gronewold, Anja, Horn, Mareike and Neundorf, Ines ORCID: 0000-0001-6450-3991 (2018). Design and biological characterization of novel cell-penetrating peptides preferentially targeting cell nuclei and subnuclear regions. Beilstein J. Org. Chem., 14. S. 1378 - 1389. FRANKFURT AM MAIN: BEILSTEIN-INSTITUT. ISSN 1860-5397

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Abstract

Within this study, we report about the design and biological characterization of novel cell-penetrating peptides (CPPs) with selective suborganelle-targeting properties. The nuclear localization sequence N50, as well as the nucleoli-targeting sequence NrTP, respectively, were fused to a shortened version of the cell-penetrating peptide sC18. We examined cellular uptake, subcellular fate and cytotoxicity of these novel peptides, N50-sC18* and NrTP-sC18*, and found that they are nontoxic up to a concentration of 50 or 100 mu M depending on the cell lines used. Moreover, detailed cellular uptake studies revealed that both peptides enter cells via energy-independent uptake, although endocytotic processes cannot completely excluded. However, initial drug delivery studies demonstrated the high versatility of these new peptides as efficient transport vectors targeting specifically nuclei and nucleoli. In future, they could be further explored as parts of newly created peptide-drug conjugates.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Gronewold, Anja UNSPECIFIED UNSPECIFIED UNSPECIFIED Horn, Mareike UNSPECIFIED UNSPECIFIED UNSPECIFIED Neundorf, Ines UNSPECIFIED orcid.org/0000-0001-6450-3991 UNSPECIFIED
URN:	urn:nbn:de:hbz:38-182996
DOI:	10.3762/bjoc.14.116
Journal or Publication Title:	Beilstein J. Org. Chem.
Volume:	14
Page Range:	S. 1378 - 1389
Date:	2018
Publisher:	BEILSTEIN-INSTITUT
Place of Publication:	FRANKFURT AM MAIN
ISSN:	1860-5397
Language:	English
Faculty:	Faculty of Mathematics and Natural Sciences
Divisions:	Faculty of Mathematics and Natural Sciences > Department of Chemistry > Institute of Biochemistry
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language POTENTIAL ANTICANCER ACTIVITY; DRUG-DELIVERY; MECHANISM; INTERNALIZATION; DOXORUBICIN; DYNAMICS; LEADS Multiple languages Chemistry, Organic Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/18299