Amphipathicity Determines Different Cytotoxic Mechanisms of Lysine- or Arginine-Rich Cationic Hydrophobic Peptides in Cancer Cells
文献类型：期刊论文
| 作者 | Liu, XL(刘晓丽); Cao, R; Wang, S(汪莎); Jia, JL(贾俊丽); Fei, H(费浩) |
| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2016 |
| 卷号 | 59期号:11 |
| 通讯作者 | Fei, H(费浩) |
| 英文摘要 | Cationic amphipathic peptides (CAPs) are known to be able to cause membrane destabilization and induce cell death, yet how the hydrophobicity, amphipathicity, and lysine (K)/arginine (R) composition synergistically affect the peptide activity remains incompletely understood. Here, we designed a panel of peptides based on the well-known anticancer peptide KLA. Increasing hydrophobicity enhanced the cytotoxicities of both the K- and R-rich peptides. Peptides with an intact amphipathic helical interface can cause instant cell death through a membrane lysis mechanism. Interestingly, rearranging the residue positions to minimize amphipathicity caused a great decrease of cytotoxicity to the K-rich peptides but not to the R-rich peptides. The amphipathicity-minimized R-rich peptide 6 (RL2) (RLLRLLRLRRLLRL-NH2) penetrated the cell membrane and induced caspase-3-dependent apoptotic cell death. We found that the modulation of hydrophobicity, amphipathicity, and K/R residues leads to distinct mechanisms of action of cationic hydrophobic peptides. Amphipathicity-reduced, arginine-rich cationic hydrophobic peptides (CHPs) may represent a new class of peptide therapeutics. |
| 关键词[WOS] | ANTIMICROBIAL PEPTIDES ; PROAPOPTOTIC PEPTIDE ; LYTIC PEPTIDES ; IRIDIUM(III) COMPLEX ; AMPHIPHILIC PEPTIDES ; MEMBRANES ; STRESS ; APOPTOSIS ; TOXICITY ; PROTEINS |
| 收录类别 | SCI ; EI |
| 语种 | 英语 |
| WOS记录号 | WOS:000377842500008 |
| 源URL | [http://ir.sinano.ac.cn/handle/332007/4764]  |
| 专题 | 苏州纳米技术与纳米仿生研究所_纳米生物医学与安全研究部_费浩团队 |
| 推荐引用方式 GB/T 7714 | Liu, XL,Cao, R,Wang, S,et al. Amphipathicity Determines Different Cytotoxic Mechanisms of Lysine- or Arginine-Rich Cationic Hydrophobic Peptides in Cancer Cells[J]. JOURNAL OF MEDICINAL CHEMISTRY,2016,59(11). |
| APA | Liu, XL,Cao, R,Wang, S,Jia, JL,&Fei, H.(2016).Amphipathicity Determines Different Cytotoxic Mechanisms of Lysine- or Arginine-Rich Cationic Hydrophobic Peptides in Cancer Cells.JOURNAL OF MEDICINAL CHEMISTRY,59(11). |
| MLA | Liu, XL,et al."Amphipathicity Determines Different Cytotoxic Mechanisms of Lysine- or Arginine-Rich Cationic Hydrophobic Peptides in Cancer Cells".JOURNAL OF MEDICINAL CHEMISTRY 59.11(2016). |
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