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Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

Published on: January 26, 2016

Antimicrobial cyclic decapeptides with anticancer activity.

Lidia Feliu1, Glòria Oliveras, Anna D Cirac

  • 1LIPPSO, Department of Chemistry, University of Girona, Campus Montilivi, E-17071 Girona, Spain.

Peptides
|August 17, 2010
PubMed
Summary
This summary is machine-generated.

Cyclic decapeptides show potent anticancer activity, inducing apoptosis and targeting key cell signaling proteins. These antimicrobial peptides offer a promising new strategy for cancer therapy with low toxicity to normal cells.

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Last Updated: Jun 10, 2026

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
08:48

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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
10:12

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

Published on: September 19, 2022

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Antimicrobial peptides (AMPs) are explored for cancer therapy.
  • Cyclic decapeptides are investigated for their cytotoxic potential.

Purpose of the Study:

  • To evaluate the cytotoxicity of 66 cyclodecapeptides against human carcinoma cell lines.
  • To assess their effects on apoptosis and cell signaling proteins.
  • To identify peptides with high anticancer activity and specificity.

Main Methods:

  • Cytotoxicity assays on multiple human carcinoma cell lines.
  • Apoptosis assessment via poly(ADP-ribose) polymerase (PARP) cleavage.
  • Analysis of p53 and ERK1/2 signaling protein levels.
  • Design of experiments approach for activity rule definition.
  • Hemolytic activity and fibroblast cytotoxicity assays.
  • Protease stability in human serum assessment.
  • Synergy studies with cisplatin.

Main Results:

  • Eight peptides exhibited IC(50) values between 18.5–57.5 μM against tested cell lines.
  • HeLa cells showed the highest sensitivity.
  • Peptides BPC88, BPC96, BPC98, and BPC194 demonstrated specific cytotoxicity against HeLa cells (IC(50) 22.5–38.5 μM).
  • These selected peptides had low hemolytic activity and low cytotoxicity to fibroblasts.
  • They were stable to human serum proteases.
  • Apoptosis induction was observed, with BPC88 and BPC96 decreasing activated ERK1/2 and increasing p53.
  • BPC96 showed synergistic effects with cisplatin.

Conclusions:

  • Cyclic decapeptides are effective anticancer agents.
  • They induce apoptosis and modulate cancer cell signaling pathways.
  • Selected peptides demonstrate specificity and stability, suggesting therapeutic potential.
  • These peptides represent a novel strategy for cancer treatment.