<> "The repository administrator has not yet configured an RDF license."^^ . <> . . . "Synthesis and functionalization of protease-activated nanoparticles with tissue plasminogen activator peptides as targeting moiety and diagnostic tool for pancreatic cancer"^^ . "Background: Functionalized nanoparticles (NPs) are one promising tool for detecting specific molecular targets and combine molecular biology and nanotechnology aiming at modern imaging. We aimed at ligand-directed delivery with a suitable target-biomarker to detect early pancreatic ductal adenocarcinoma (PDAC). Promising targets are galectins (Gal), due to their strong expression in and on PDAC-cells and occurrence at early stages in cancer precursor lesions, but not in adjacent normal tissues. Results: Molecular probes (10-29 AA long peptides) derived from human tissue plasminogen activator (t-PA) were selected as binding partners to galectins. Affinity constants between the synthesized t-PA peptides and Gal were determined by microscale thermophoresis. The 29 AA-long t-PA-peptide-1 with a lactose-functionalized serine revealed the strongest binding properties to Gal-1 which was 25-fold higher in comparison with the native t-PA protein and showed additional strong binding to Gal-3 and Gal-4, both also over-expressed in PDAC. t-PA-peptide-1 was selected as vector moiety and linked covalently onto the surface of biodegradable iron oxide nanoparticles (NPs). In particular, CAN-doped maghemite NPs (CAN-Mag), promising as contrast agent for magnetic resonance imaging (MRI), were selected as magnetic core and coated with different biocompatible polymers, such as chitosan (CAN-Mag-Chitosan NPs) or polylactic co glycolic acid (PLGA) obtaining polymeric nanoparticles (CAN-Mag@PNPs), already approved for drug delivery applications. The binding efficacy of t-PA-vectorized NPs determined by exposure to different pancreatic cell lines was up to 90%, as assessed by flow cytometry. The in vivo targeting and imaging efficacy of the vectorized NPs were evaluated by applying murine pancreatic tumor models and assessed by 1.5 T magnetic resonance imaging (MRI). The t-PA-vectorized NPs as well as the protease-activated NPs with outer shell decoration (CAN-Mag@PNPs-PEG-REGAcp-PEG/tPA-pep1Lac) showed clearly detectable drop of subcutaneous and orthotopic tumor staining-intensity indicating a considerable uptake of the injected NPs. Post mortem NP deposition in tumors and organs was confirmed by Fe staining of histopathology tissue sections. Conclusions: The targeted NPs indicate a fast and enhanced deposition of NPs in the murine tumor models. The CAN-Mag@PNPs-PEG-REGAcp-PEG/tPA-pep1Lac interlocking steps strategy of NPs delivery and deposition in pancreatic tumor is promising."^^ . "2016" . . "14" . "81" . . "BioMed Central"^^ . . . "Journal of Nanobiotechnology"^^ . . . "14773155" . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . "Albert"^^ . "Strauß"^^ . "Albert Strauß"^^ . . "Jens"^^ . "Werner"^^ . "Jens Werner"^^ . . "Mauro Comes"^^ . "Franchini"^^ . "Mauro Comes Franchini"^^ . . "Christian"^^ . "Weis"^^ . "Christian Weis"^^ . . "Katya"^^ . "Kapilov-Buchman"^^ . "Katya Kapilov-Buchman"^^ . . "Jean-Paul"^^ . "Lellouche"^^ . "Jean-Paul Lellouche"^^ . . "Liron-Limor"^^ . "Israel"^^ . "Liron-Limor Israel"^^ . . "Aleko"^^ . "Kjaev"^^ . "Aleko Kjaev"^^ . . "Jennifer"^^ . "Vandooren"^^ . "Jennifer Vandooren"^^ . . "Sophie"^^ . "Dobiasch"^^ . "Sophie Dobiasch"^^ . . "Lars"^^ . "Grenacher"^^ . "Lars Grenacher"^^ . . "Klaus"^^ . "Felix"^^ . "Klaus Felix"^^ . . "Szilard"^^ . "Szanyi"^^ . "Szilard Szanyi"^^ . . "Erica"^^ . "Locatelli"^^ . "Erica Locatelli"^^ . . "Ghislain"^^ . "Opdenakker"^^ . "Ghislain Opdenakker"^^ . . . . . . "Synthesis and functionalization of protease-activated nanoparticles with tissue plasminogen activator peptides as targeting moiety and diagnostic tool for pancreatic cancer (PDF)"^^ . . . "12951_2016_Article_236.pdf"^^ . . . "Synthesis and functionalization of protease-activated nanoparticles with tissue plasminogen activator peptides as targeting moiety and diagnostic tool for pancreatic cancer (Other)"^^ . . . . . . "indexcodes.txt"^^ . . . "Synthesis and functionalization of protease-activated nanoparticles with tissue plasminogen activator peptides as targeting moiety and diagnostic tool for pancreatic cancer (Other)"^^ . . . . . . "lightbox.jpg"^^ . . . "Synthesis and functionalization of protease-activated nanoparticles with tissue plasminogen activator peptides as targeting moiety and diagnostic tool for pancreatic cancer (Other)"^^ . . . . . . "preview.jpg"^^ . . . 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