RRC ID 53861
Author Toyama K, Nomura W, Kobayakawa T, Tamamura H.
Title Delivery of a Proapoptotic Peptide to EGFR-Positive Cancer Cells by a Cyclic Peptide Mimicking the Dimerization Arm Structure of EGFR.
Journal Bioconjug. Chem.
Abstract ) has limited use due to a deficiency of cell membrane permeability resulting from cationic sequences and lack of specificity for cancer cells. As a proof-of-concept study, the cellular delivery of the PAD peptide was challenged by conjugation with peptide 1. The cellular uptake of a conjugated peptide 2, which was composed of peptide 1, the PAD peptide, and a linker cleavable with a protease, was evaluated by treatment of an EGFR-positive lung carcinoma cell line, A549. Significant suppression of proliferation by peptide 2 was shown in the results of a cell viability assay. The PAD peptide alone had no effect on the cells. The results suggest that peptide 1 is a promising lead compound as a new intracellular delivery vehicle for therapeutically effective peptides.
Volume 29(6)
Pages 2050-2057
Published 2018-6-20
DOI 10.1021/acs.bioconjchem.8b00250
PMID 29763296
MeSH A549 Cells Adenocarcinoma of Lung / drug therapy Adenocarcinoma of Lung / metabolism Amino Acid Sequence Antineoplastic Agents / administration & dosage* Antineoplastic Agents / chemistry Antineoplastic Agents / pharmacokinetics Antineoplastic Agents / pharmacology* Apoptosis / drug effects* Cell Proliferation / drug effects Drug Delivery Systems ErbB Receptors / chemistry ErbB Receptors / metabolism Humans Lung Neoplasms / drug therapy Lung Neoplasms / metabolism Models, Molecular Peptides / administration & dosage* Peptides / chemistry Peptides / pharmacokinetics Peptides / pharmacology* Peptides, Cyclic / administration & dosage Peptides, Cyclic / chemistry Peptides, Cyclic / pharmacokinetics Peptides, Cyclic / pharmacology Protein Multimerization
IF 4.485
Human and Animal Cells A431(RCB0202), A549(RCB0098), 293(RCB1637)