title: Synthesis, characterization and anti-cancer activity of a peptide nucleolipid bioconjugate.
abstract: 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.
authors.affiliation: Department of Chemistry and Biochemistry, Seton Hall University, 400 South Orange Avenue, South Orange, NJ 07079, United States.
authors.forename: Niki
authors.initials: N
authors.lastname: Rana
authors.affiliation: Department of Chemistry, Queens College, City University of New York, 65-30 Kissena Blvd, Flushing, New York 11367, United States; The Ph.D. Programs in Chemistry and Biochemistry, The Graduate Center of the City University of New York, New York, NY 10016, United States.
authors.forename: Suiying
authors.initials: S
authors.lastname: Huang
authors.affiliation: Department of Chemistry and Biochemistry, Seton Hall University, 400 South Orange Avenue, South Orange, NJ 07079, United States.
authors.forename: Pradeepkumar
authors.initials: P
authors.lastname: Patel
authors.affiliation: Department of Chemistry, Queens College, City University of New York, 65-30 Kissena Blvd, Flushing, New York 11367, United States; The Ph.D. Programs in Chemistry and Biochemistry, The Graduate Center of the City University of New York, New York, NY 10016, United States.
authors.forename: Uri
authors.initials: U
authors.lastname: Samuni
authors.affiliation: Department of Chemistry and Biochemistry, Seton Hall University, 400 South Orange Avenue, South Orange, NJ 07079, United States. Electronic address: david.sabatino@shu.edu.
authors.forename: David
authors.initials: D
authors.lastname: Sabatino
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008055:Lipids / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D008055:Lipids; D010455:Peptides
keywords: Amphiphilic peptides; Anti-cancer activity; Nucleolipid; Peptide bioconjugate