A Disulfide Intercalator Toolbox for the Site‐Directed Modification of Polypeptides

A disulfide intercalator toolbox was developed for site‐specific attachment of a broad variety of functional groups to proteins or peptides under mild, physiological conditions. The peptide hormone somatostatin (SST) served as model compound for intercalation into the available disulfide functionalization schemes starting from the intercalator or the reactive SST precursor before or after bioconjugation. A tetrazole–SST derivative was obtained that undergoes photoinduced cycloaddition in mammalian cells, which was monitored by live‐cell imaging.     

铜基/氧化锆催化剂的应用及改性研究进展

ZrO2具有弱酸碱性、氧化还原性、良好的热稳定性和机械强度,在催化领域得到广泛应用。以Zr O2为载体的铜基催化剂因其活性高,选择性好,性能稳定,受到越来越多的关注。本文介绍了Cu/Zr O2催化剂在醇类的水蒸气重整制氢、CO/CO2加氢合成低碳醇、二乙醇胺脱氢、乙醇直接合成乙酸乙酯和低温水煤气变换方面的应用。综述了添加不同助剂对Cu/Zr O2催化剂物化及催化性能的影响。     

Protein Staining Agents from Cationic and Neutral Luminescent Iridium(III) Complexes

Seven luminescent iridium(III) complexes were prepared to investigate the relationships between chemical structures and properties of protein staining. For the first time, the effect of the main ligand, the π conjugation effect of the ancillary ligand, and the charge effect of organometallic complexes on protein staining has been revealed. Most importantly, this study gives the first experimental evidence of the potential applications of charge‐neutral organometallic complexes in protein staining, which could open an avenue of exploiting novel protein staining agents in the future.     

Gold‐Catalyzed Tandem Cycloisomerization–Halogenation of Chiral Homopropargyl Sulfonamides

Two new gold‐catalyzed tandem cycloisomerization–halogenation reactions of chiral homopropargyl sulfonamides have been developed. Various enantioenriched 3,3‐diiodopyrrolidin‐2‐ols and 3‐fluoropyrrolidin‐2‐ols were obtained in moderate‐to‐good yields with excellent enantio‐ and diastereoselectivity.     

Redox‐responsive core cross‐linked micelles of poly(ethylene oxide)‐b‐poly(furfuryl methacrylate) by Diels‐Alder reaction for doxorubicin release

Redox‐responsive core cross‐linked (CCL) micelles of poly(ethylene oxide)‐b‐poly(furfuryl methacrylate) (PEO‐b‐PFMA) block copolymers were prepared by the Diels‐Alder click‐type reaction. First, the PEO‐b‐PFMA amphiphilic block copolymer was synthesized by the reversible addition‐fragmentation chain transfer polymerization. The hydrophobic blocks of PFMA were employed to encapsulate the doxorubicin (DOX) drug, and they were cross‐linked using dithiobismaleimidoethane at 60 °C without any catalyst. Under physiological circumstance, the CCL micelles demonstrated the enhanced structural stability of the micelles, whereas dissociation of the micelles took place rapidly through the breaking of disulfide bonds in the cross‐linking linkages under reduction environment. The core‐cross‐linked micelles showed fine spherical distribution with hydrodynamic diameter of 68 ± 2.9  nm. The in vitro drug release profiles presented a slight release of DOX at pH 7.4, while a significant release of DOX was observed at pH 5.0 in the presence of 1,4‐dithiothreitol. MTT assays demonstrated that the block copolymer did not have any practically cytotoxicity against the normal HEK293 cell line while DOX‐loaded CCL micelles exhibited a high antitumor activity towards HepG2 cells. © 2016 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2016 , 54, 3741–3750