title: Design, synthesis and biological activity of cell-penetrating peptide-modified octreotide analogs.
abstract: Four novel octreotide analogs with cell-penetrating peptides (CPPs) at the N-terminus or C-terminus were synthesized by a stepwise Fmoc solid-phase synthesis strategy. The synthesized peptides were analyzed and characterized using reverse phase HPLC and MALDI-TOF mass spectrometry. The antiproliferative activity of the analogs was tested in vitro on human gastric (SGC-7901) and hepatocellular cancer (BEL7402) cell lines using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Interestingly, these analogs showed a higher anticancer activities than the parent octreotide except CMTPT03 analog. The results demonstrate that the designed octreotide analogs enhance their anticancer activity after linking together the CPPs to octreotide at the N-terminus, and are potential molecules for future use in cancer therapy and drug targeting.
authors.affiliation: School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, China. xwl2003zsu@yahoo.com.cn
authors.forename: Wenlin
authors.initials: W
authors.lastname: Xie
authors.forename: Jian
authors.initials: J
authors.lastname: Liu
authors.forename: Minghua
authors.initials: M
authors.lastname: Qiu
authors.forename: Jiancheng
authors.initials: J
authors.lastname: Yuan
authors.forename: Anlong
authors.initials: A
authors.lastname: Xu
mesh_terms: D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects*; D002851:Chromatography, High Pressure Liquid; D015195:Drug Design; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy; D009682:Magnetic Resonance Spectroscopy; D008969:Molecular Sequence Data; D015282:Octreotide / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D013274:Stomach Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D015282:Octreotide