Synthesis, characterization and anti-cancer activity of a peptide nucleolipid bioconjugate.


The synthesis, characterization and anti-cancer activity of a novel peptide nucleolipid bioconjugate is reported in this study. The prerequisite 5'-carboxy derived nucleolipid was synthesized following a five-step solution-phase approach and then coupled to the cytotoxic D-(KLAKLAK)2 sequence by solid-phase bioconjugation. The biophysical and structural properties of the peptide-nucleolipid bioconjugate were evaluated and compared to the peptide controls. These characterization studies revealed that the amphiphilic peptides favored helical-type secondary structures and well-defined nanoparticle formulations that were found to be contributive towards their biological activity. The peptide-nucleolipid bioconjugate displayed greater lethality in comparison to the native D-(KLAKLAK)2AK sequence when treated within the human A549 non-small cell lung carcinoma cell line. Thus, the amphiphilic peptide-nucleolipid forms a new class of anti-cancer peptides that may be developed into promising leads in the fight against cancer.

DOI: 10.1016/j.bmcl.2016.06.020

Cite this paper

@article{Rana2016SynthesisCA, title={Synthesis, characterization and anti-cancer activity of a peptide nucleolipid bioconjugate.}, author={Niki K Rana and Suiying Huang and Pradeepkumar L Patel and Uri Samuni and David Sabatino}, journal={Bioorganic & medicinal chemistry letters}, year={2016}, volume={26 15}, pages={3567-71} }