Abstract:
:Expression of various molecules on the surface of cancer cells compared to normal cells creates a platform for the generation of various drug vehicles for targeted therapy. Multiple interactions between ligands and their receptors mediated by targeting peptide-modified polymer could enable simultaneous delivery of a drug selectively to target tumor cells, thus limiting side effects resulting from non-specific drug delivery. In this study, we synthesized a novel tumor targeting system by using two key elements: (1) Bld-1 peptide (SNRDARRC), a recently reported bladder tumor targeting peptide identified by using a phage-displayed peptide library, and (2) ELP, a thermally responsive polypeptide. B5V60 containing five Bld-1 peptides and non-targeted ELP77 with a thermal phase-transition over 37 °C were analyzed to determine their bioactivities. Further studies confirmed the superior binding ability of B5V60 to bladder tumor cells and the cellular accumulation of B5V60 in cancer cells was dependent on the expression level of sialyl-Tn antigen (STn), a tumor-associated carbohydrate antigen. Additionally, B5V60 displayed excellent localization in bladder tumor xenograft mice after intravenous injection and was strictly confined to sialyl-Tn antigen-overexpressing tumor tissue. Thus, our newly designed B5V60 showed high potential as a novel carrier for STn-specific targeted cancer therapy or other therapeutic applications.
journal_name
Sci Repjournal_title
Scientific reportsauthors
Sarangthem V,Cho EA,Yi A,Kim SK,Lee BH,Park RWdoi
10.1038/s41598-018-21910-zsubject
Has Abstractpub_date
2018-03-01 00:00:00pages
3892issue
1issn
2045-2322pii
10.1038/s41598-018-21910-zjournal_volume
8pub_type
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