Dynamic Amphiphile Libraries To Screen for the "Fragrant" Delivery of siRNA into HeLa Cells and Human Primary Fibroblasts

Article Article scientifique Article Dynamic Amphiphile Libraries To Screen for the "Fragrant" Delivery of siRNA into HeLa Cells and Human Primary Fibroblasts eng 2013 author Gehin Charlotte 685054 author Montenegro Garcia Javier 687118 author Bang Eun Kyoung 738959 author Cajaraville Leiro Ana 755877 author Takayama Shota author Hirose Hisaaki author Futaki Shiroh author Matile Stefan 0000-0002-8537-8349 129654 author Riezman Howard 134430 9295-9298 10.1021/ja404153m 0002-7863 Dynamic amphiphiles are amphiphiles with dynamic covalent bridges between their hydrophilic heads and their hydrophobic tails. Their usefulness to activate ion transporters, for odorant release, and for differential sensing of odorants and perfumes, has been demonstrated recently. Here, we report that the same “fragrant” dynamic amphiphiles are ideal to screen for new siRNA transfection agents. The advantages of this approach include rapid access to fairly large libraries of complex structures, and possible transformation en route to assist uptake and minimize toxicity. We report single-component systems that exceed the best commercially available multicomponent cocktails with regard to both efficiency and velocity of EGFP knockdown in HeLa cells. In human primary fibroblasts, siRNA-mediated enzyme knockdown nearly doubled from >30% for Lipofectamine to >60% for our best hit. The identified structures were predictable neither from literature nor from results in fluorogenic vesicles and thus support the importance of conceptually innovative screening approaches. Dewey 540 36 Département de chimie organique 141 false Journal of the American Chemical Society 135 25 e74df037-d3a5-46f1-8122-d3f22bbf8de3 Article (Published version) Restricted ja404153m (1).pdf 1210376 application/pdf 026164b7-321b-4b8d-b358-f6da1c7ac473 Article (Accepted version) Public 207.pdf 803073 application/pdf OA OTHER openAccess Faculté des sciences / Section de chimie et biochimie / Département de chimie organique

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Dynamic Amphiphile Libraries To Screen for the "Fragrant" Delivery of siRNA into HeLa Cells and Human Primary Fibroblasts	Journal of the American Chemical Society			2013	700	405

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Cajaraville Leiro, Ana