Kwok A Eggimann GA Heitz M Reymond JL Hollfelder F Darbre T 2016 Efficient delivery of small interfering RNA (siRNA) into cells is the basis of target-gene-specific silencing and, ultimately, gene therapy. However, current transfection reagents are relatively inefficient, and very few studies provide the sort of systematic understanding based on structure-activity relationships that would provide rationales for their improvement. This work established peptide dendrimers (administered with cationic lipids) as siRNA transfection reagents and recorded structure-activity relationships that highlighted the importance of positive charge distribution in the two outer layers and a hydrophobic core as key features for efficient performance. These dendrimer-based transfection reagents work as well as highly optimised commercial reagents, yet show less toxicity and fewer off-target effects. Additionally, the degrees of freedom in the synthetic procedure will allow the placing of decisive recognition features to enhance and fine-tune transfection and cell specificity in the future. application/pdf https://sonar.ch/global/documents/263731 eng info:eu-repo/semantics/altIdentifier/doi/10.1002/cbic.201600485 info:eu-repo/semantics/altIdentifier/pmid/27862758 info:eu-repo/semantics/openAccess Chembiochem : a European journal of chemical biology. - 2016 RNA interference gene knockdown peptide dendrimers siRNA transfection Dendrimers Humans Lipids Peptides RNA, Small Interfering Transfection Efficient Transfection of siRNA by Peptide Dendrimer-Lipid Conjugates. http://purl.org/coar/resource_type/c_6501