scholarly journals Cell Penetrating Peptides as Molecular Carriers for Anti-Cancer Agents

Molecules ◽  
2018 ◽  
Vol 23 (2) ◽  
pp. 295 ◽  
Author(s):  
Antonella Borrelli ◽  
Anna Tornesello ◽  
Maria Tornesello ◽  
Franco Buonaguro
Oncotarget ◽  
2017 ◽  
Vol 9 (5) ◽  
pp. 5944-5957 ◽  
Author(s):  
Xiguang Zhang ◽  
Jean Yves Brossas ◽  
Christophe Parizot ◽  
Jean Marc Zini ◽  
Angelita Rebollo

2020 ◽  
Vol 56 (42) ◽  
pp. 5685-5688
Author(s):  
Lucia Feni ◽  
Linda Jütten ◽  
Sara Parente ◽  
Umberto Piarulli ◽  
Ines Neundorf ◽  
...  

Cargo-peptides approaching cellular membranes: influence of cyclization and stereochemistry on cellular translocation activity of a novel group of cell-penetrating peptides containing bifunctional diketopiperazine.


Cancers ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 2504
Author(s):  
Qing Zhou ◽  
Xiotian Sun ◽  
Nicolas Pasquier ◽  
Parvaneh Jefferson ◽  
Trang T. T. Nguyen ◽  
...  

Transcription factors are key players underlying cancer formation, growth, survival, metastasis and treatment resistance, yet few drugs exist to directly target them. Here, we characterized the in vitro and in vivo anti-cancer efficacy of novel synthetic cell-penetrating peptides (Bpep and Dpep) designed to interfere with the formation of active leucine-zipper-based dimers by CEBPB and CEBPD, transcription factors implicated in multiple malignancies. Both peptides similarly promoted apoptosis of multiple tumor lines of varying origins, without such effects on non-transformed cells. Combined with other treatments (radiation, Taxol, chloroquine, doxorubicin), the peptides acted additively to synergistically and were fully active on Taxol-resistant cells. The peptides suppressed expression of known direct CEBPB/CEBPD targets IL6, IL8 and asparagine synthetase (ASNS), supporting their inhibition of transcriptional activation. Mechanisms by which the peptides trigger apoptosis included depletion of pro-survival survivin and a required elevation of pro-apoptotic BMF. Bpep and Dpep significantly slowed tumor growth in mouse models without evident side effects. Dpep significantly prolonged survival in xenograft models. These findings indicate the efficacy and potential of Bpep and Dpep as novel agents to treat a variety of cancers as mono- or combination therapies.


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