Ligand-directed dibromophenyl benzoate chemistry for rapid and selective acylation of intracellular natural proteins† †Electronic supplementary information (ESI) available: Figures for eDHFR labeling in vitro and in cells, HPLC analyses of the stabilities of the reagents, CPK models of the reagents, and synthetic methods. See DOI: 10.1039/c5sc00190k Click here for additional data file.

نویسندگان

  • Yousuke Takaoka
  • Yuki Nishikawa
  • Yuki Hashimoto
  • Kenta Sasaki
  • Itaru Hamachi
چکیده

Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering Kyoto University, Katsura, Kyoto 615-8510, Japan. Present address: Department of Chemistry, Graduate School of Science, Tohoku University, Aramaki-aza Aoba 6-3, Aoba-ku, Sendai 980-8578, Japan. Core Research for Evolutional Science and Technology (CREST), Japan Science and Technology Agency, 5 Sanbancho, Chiyoda-ku, Tokyo 102-0075, Japan.

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منابع مشابه

Ligand-directed dibromophenyl benzoate chemistry for rapid and selective acylation of intracellular natural proteins.

A rapid and selective ligand-directed chemical reaction was developed for the acylation of proteins in living cells on the basis of ligand-directed chemistry. By fine tuning the reactivity and stability of the phenyl ester derivatives, we successfully identified ortho-dibromophenyl benzoate as the optimal reactive motif. It was sufficiently stable in an aqueous buffer, hydrolyzing less than 10%...

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Self-assembled micelles of amphiphilic PEGylated rapamycin for loading paclitaxel and resisting multidrug resistant cancer cells† †Electronic supplementary information (ESI) available: Chemicals and reagents, detailed experimental procedures for materials synthesis, characterization, cellular evaluations and supporting figures and tables. See DOI: 10.1039/c4tb01633e Click here for additional data file.

Self-assembled micelles of amphiphilic PEG-rapamycin conjugates loaded with paclitaxel have been developed for co-delivery and simultaneous intracellular release of paclitaxel and rapamycin, bypassing the cancer cell drug resistant mechanism and maximising the synergy of dual-drug combinational therapy. This novel nanomedicine offers 20-fold improved potency over free paclitaxel against a model...

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عنوان ژورنال:

دوره 6  شماره 

صفحات  -

تاریخ انتشار 2015