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.
['Rana|Niki|N|', 'Huang|Suiying|S|', 'Patel|Pradeepkumar|P|', 'Samuni|Uri|U|', 'Sabatino|David|D|']
D000970:Antineoplastic Agents D016923:Cell Death D045744:Cell Line, Tumor D049109:Cell Proliferation D004305:Dose-Response Relationship, Drug D004354:Drug Screening Assays, Antitumor D006801:Humans D008055:Lipids D015394:Molecular Structure D010455:Peptides D013329:Structure-Activity Relationship
Anti-cancer activity Nucleolipid Amphiphilic peptides Peptide bioconjugate