scholarly journals Cell-penetrating peptides containing 2,5-diketopiperazine (DKP) scaffolds as shuttles for anti-cancer drugs: conformational studies and biological activity

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.

2012 ◽  
Vol 20 (4) ◽  
pp. 695-697 ◽  
Author(s):  
Caroline Palm-Apergi ◽  
Peter Lönn ◽  
Steven F Dowdy

2010 ◽  
Vol 1 (2) ◽  
pp. 109-116 ◽  
Author(s):  
Jamie Brugnano ◽  
Brian C. Ward ◽  
Alyssa Panitch

AbstractCell penetrating peptides (CPPs) have been successful in delivering cargo into many different cell types and are an important alternative to other methods of permeation that might damage the integrity of the cell membrane. The traditional view of CPPs is that they are inert molecules that can be successfully used to deliver many cargos intracellularly. The goal of this review is to challenge this traditional understanding of CPPs. Recent literature has demonstrated that CPPs themselves can convey biological activity, including the alteration of gene expression and inhibition of protein kinases and proteolytic activity. Further characterization of CPPs is required to determine the extent of this activity. Research into the use of CPPs for intracellular delivery should continue with investigators being aware of these recent results.


Oncotarget ◽  
2017 ◽  
Vol 9 (5) ◽  
pp. 5944-5957 ◽  
Author(s):  
Xiguang Zhang ◽  
Jean Yves Brossas ◽  
Christophe Parizot ◽  
Jean Marc Zini ◽  
Angelita Rebollo

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3361 ◽  
Author(s):  
Teresa Glomb ◽  
Karolina Szymankiewicz ◽  
Piotr Świątek

Compounds containing 1,3,4-oxadiazole ring in their structure are characterised by multidirectional biological activity. Their anti-proliferative effects associated with various mechanisms, such as inhibition of growth factors, enzymes, kinases and others, deserve attention. The activity of these compounds was tested on cell lines of various cancers. In most publications, the most active derivatives of 1,3,4-oxadiazole exceeded the effect of reference drugs, so they may become the main new anti-cancer drugs in the future.


Molecules ◽  
2018 ◽  
Vol 23 (2) ◽  
pp. 295 ◽  
Author(s):  
Antonella Borrelli ◽  
Anna Tornesello ◽  
Maria Tornesello ◽  
Franco Buonaguro

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.


1993 ◽  
Vol 55 (1) ◽  
pp. 43-46
Author(s):  
Jun YOSHIDA ◽  
Juichiro NAKAYAMA ◽  
Nobuyuki SHIMIZU ◽  
Shonosuke NAGAE ◽  
Yoshiaki HORI

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