improvedmethodforsynthesisoflowmolecularweightprotaminesirnaconjugate
文献类型：期刊论文
| 作者 | Yu Zhili1; Ye Junxiao2; Pei Xing1; Sun Lu1; Liu Ergang3; Wang Jianxin4; Huang Yongzhuo5 ; Lee Seung Jin6; He Huining1
|
| 刊名 | actapharmaceuticasinicab
 |
| 出版日期 | 2018 |
| 卷号 | 000期号:001页码:116 |
| 关键词 | Cell penetrating peptide siRNA Conjugate Conjugation yield Biomimetic delivery Crosslinker |
| ISSN号 | 2211-3835 |
| 英文摘要 | RNAi technology has aroused wide public interest due to its high efficiency and specificity to treat multiple types of diseases. However, the effective delivery of siRNA remains a challenge due to its large molecular weight and strong anionic charge. Considering their remarkable functions in vivo and features that are often desired in drug delivery carriers, biomimetic systems for siRNA delivery become an effective and promising strategy. Based on this, covalent attachment of synthetic cell penetrating peptides(CPP) to siRNA has become of great interest. We developed a monomeric covalent conjugate of low molecular weight protamine(LMWP, a well-established CPP) and siRNA via a cytosol-cleavable disulfide linkage using PEG as a crosslinker. Results showed that the conjugates didn’t generate coagulation, and exhibited much better RNAi potency and intracellular delivery compared with the conventional charge-complexed CPP/siRNA aggregates. Three different synthetic and purification methods were compared in order to optimize synthesis efficiency and product yield. The methodology using hetero-bifunctional NHS–PEG–OPSS as a crosslinker to synthesize LMWP–siRNA simplified the synthesis and purification process and produced the highest yield. These results pave the way towards siRNA biomimetic delivery and future clinical translation. |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/285000]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.天津医科大学 2.清华大学 3.天津大学 4.教育部 5.中国科学院上海药物研究所 6.梨花女子大学 |
| 推荐引用方式 GB/T 7714 | Yu Zhili,Ye Junxiao,Pei Xing,et al. improvedmethodforsynthesisoflowmolecularweightprotaminesirnaconjugate[J]. actapharmaceuticasinicab,2018,000(001):116. |
| APA | Yu Zhili.,Ye Junxiao.,Pei Xing.,Sun Lu.,Liu Ergang.,...&He Huining.(2018).improvedmethodforsynthesisoflowmolecularweightprotaminesirnaconjugate.actapharmaceuticasinicab,000(001),116. |
| MLA | Yu Zhili,et al."improvedmethodforsynthesisoflowmolecularweightprotaminesirnaconjugate".actapharmaceuticasinicab 000.001(2018):116. |
入库方式： OAI收割
来源：上海药物研究所
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