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.

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%...

Highly selective acylation of polyamines and aminoglycosides by 5-acyl-5-phenyl-1,5-dihydro-4H-pyrazol-4-ones† †Electronic supplementary information (ESI) available: Experimental procedures, kinetic data, UV/Vis spectra, NMR spectra, and HPLC traces. X-ray data for 44. CCDC 1563600. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c7sc03184j Click here for additional data file. Click here for additional data file.

Effects of reagent rotation on interferences in the product angular distributions of chemical reactions† †Electronic supplementary information (ESI) available: Additional figures. See DOI: 10.1039/c5sc03373j Click here for additional data file.

Broad substrate tolerance of tubulin tyrosine ligase enables one-step site-specific enzymatic protein labeling† †The technology described in this manuscript is part of a pending patent application. ‡ ‡Electronic supplementary information (ESI) available: Supporting figures, synthetic details, HPLC and MS spectra, ubiquitin labeling. See DOI: 10.1039/c7sc00574a Click here for additional data file.

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...