Okuyama, M. and Laman, H. and Kingsbury, S.R. and Visintin, C. and Leo, E. and Eward, K.L. and Stoeber, K. and Boshoff, C. and Williams, G.H. and Selwood, D.L. (2007) Small-molecule mimics of an α-helix for efficient transport of proteins into cells. Nature Methods , 4 (2) pp. 153-159. 10.1038/nmeth997.
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We designed and synthesized small-molecule mimics of an alpha-helical peptide protein transduction domain (PTD). These small-molecule carriers, which we termed SMoCs, are easily coupled to biomolecules, and efficiently deliver dye molecules and recombinant proteins into a variety of cell types. We designed the SMoCs using molecular modeling techniques. As an example of a protein cargo, we applied this new technology to the internalization of the DNA replication licensing repressor geminin, in vitro, providing evidence that extracellularly delivered SMoC-geminin can have an antiproliferative effect on human cancer cells. Uptake of SMoC-geminin was inhibited at 4 °C and by chlorpromazine, a compound that induces misassembly of clathrin-coated pits at the cell surface. Thus the mechanism of uptake is likely to be clathrin-mediated endocytosis.
|Title:||Small-molecule mimics of an α-helix for efficient transport of proteins into cells|
|UCL classification:||UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Wolfson Institute and Cancer Institute Administration > Wolfson Institute for Biomedical Research|
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