期刊
PEPTIDES
卷 32, 期 9, 页码 1934-1941出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.peptides.2011.07.018
关键词
Cell penetrating peptide; Structure-activity relationship; Uptake selectivity; Molecular dynamics simulations
资金
- National Natural Science Foundation of China [20932003, 90813012]
- Ministry of Science and Technology of China [2007AA02Z321, 2009ZX09503-017]
Transportan 10 (TP10) is an amphipathic cell-penetrating peptide with high translocation ability. In order to obtain more details of structure-activity relationship of TP10, we evaluated the effects of structure and charge on its translocation ability. Our results demonstrated that disrupting the helical structure or Arg substitution could remarkably decrease the cellular uptake of TP10. However, increasing the number of positive charge was an effective strategy to enhance translocation ability of TP10. Furthermore, the molecular dynamics simulation supported the results derived from experiments, suggesting that higher membrane disturbance leads to higher cellular uptake of peptides. In addition, our study also demonstrated TP10 and its analogs preferentially entered cancer cells rather than normal cells. The uptake selectivity toward cancer cells makes TP10 and its analogs as potent CPPs for drug delivery. (C) 2011 Elsevier Inc. All rights reserved.
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