2021
DOI: 10.3390/nano11030772
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Peptide-Functionalized Nanoparticles-Encapsulated Cyclin-Dependent Kinases Inhibitor Seliciclib in Transferrin Receptor Overexpressed Cancer Cells

Abstract: Seliciclib, a broad cyclin-dependent kinases (CDKs) inhibitor, exerts its potential role in cancer therapy. For taking advantage of overexpressive transferrin receptor (TfR) on most cancer cells, T7 peptide, a TfR targeting ligand, was selected as a targeting ligand to facilitate nanoparticles (NPs) internalization in cancer cells. In this study, poly(d,l-lactide-co-glycolide) (PLGA) was conjugated with maleimide poly(ethylene glycol) amine (Mal-PEG-NH2) to form PLGA-PEG-maleimide copolymer. The synthesized co… Show more

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Cited by 21 publications
(12 citation statements)
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“…The higher expression of Tf receptors on U87 cells enables a much greater proportion of targeted niosomes to enter the cells via receptor-mediated endocytosis, in comparison to non-targeted niosomes. We verified this Tf-receptor-mediated endocytosis of Tf-functionalized PEGNIO formulations by Tf-receptor-expressing U87 glioma cells via performing flow-cytometric cellular uptake measurements of fluorescence-labeled PEGNIO/Tf in Tf-receptor negative cells (A549, which expresses hardly any Tf-receptors [ 49 ]) ( Figure S7 ). Because, in this case, the internalization of PEGNIO and PEGNIO/Tf was shown to be almost uniform and therefore independent of Tf-functionalization, the presented enhanced internalization of Tf-labeled PEGNIO/QDs/MIONs by U87 cells can be attributed to a Tf-based endocytosis.…”
Section: Resultsmentioning
confidence: 83%
“…The higher expression of Tf receptors on U87 cells enables a much greater proportion of targeted niosomes to enter the cells via receptor-mediated endocytosis, in comparison to non-targeted niosomes. We verified this Tf-receptor-mediated endocytosis of Tf-functionalized PEGNIO formulations by Tf-receptor-expressing U87 glioma cells via performing flow-cytometric cellular uptake measurements of fluorescence-labeled PEGNIO/Tf in Tf-receptor negative cells (A549, which expresses hardly any Tf-receptors [ 49 ]) ( Figure S7 ). Because, in this case, the internalization of PEGNIO and PEGNIO/Tf was shown to be almost uniform and therefore independent of Tf-functionalization, the presented enhanced internalization of Tf-labeled PEGNIO/QDs/MIONs by U87 cells can be attributed to a Tf-based endocytosis.…”
Section: Resultsmentioning
confidence: 83%
“…Cell Cultures. Human breast cancer cells MDA-MB-231 (TfR1 highly overexpressed) and lung carcinoma cells A549 (TfR1 expressed, lower level than MDA-MB-231 cells) 32 were provided by the Cell Bank of Type Culture Collection of Chinese Academy of Sciences (Shanghai, China). Cells were cultured in Dulbecco's modified Eagle's medium supplemented with 10% (v/v) FBS and 1% penicillin−streptomycin at 37 °C in a humidified atmosphere containing 5% CO 2 .…”
Section: Methodsmentioning
confidence: 99%
“…Cellular targeting and uptake of the bioconjugates were also investigated using the MDA-MB-231 breast cancer cell line, which overexpresses the Tf receptor. 50 Most importantly, when investigated in a healthy mouse model, Tf-PMSEA 16.2k was able to significantly improve the in vivo pharmacokinetics and bioavailability of the native protein compared to Tf-POEGA 16.2k and native Tf due to its lowfouling nature. Moreover, when tested in mice bearing subcutaneous MDA-MB-231 breast tumors, a remarkably high tumor accumulation of Tf-PMSEA 16.2k was observed compared to the other groups, and hence the conjugate is expected to perform favorably for therapeutic delivery.…”
Section: ■ Introductionmentioning
confidence: 97%