Design,synthesis and biological activity of cell‐penetrating peptide‐modified octreotide analogs |
| |
| Authors: | Wenlin Xie Jian Liu Minghua Qiu Jiancheng Yuan Anlong Xu |
| |
| Institution: | 1. School of Chemistry and Chemical Engineering, Hunan University of Science and Technology, Xiangtan 411201, China;2. Center of Biopharmaceutical Research, College of Life Science, Zhongshan University, Guangzhou 510275, China;3. Shenzhen Hanyu Pharmaceutical Co., Ltd., Shenzhen 518057, China |
| |
| 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. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd. |
| |
| Keywords: | anticancer activity cell‐penetrating peptide Octreotide peptide synthesis |
|
|
