23500-04-1Relevant articles and documents
Intramolecular long-distance nucleophilic reactions as a rapid fluorogenic switch applicable to the detection of enzymatic activity
Baba, Reisuke,Hori, Yuichiro,Kikuchi, Kazuya
, p. 4695 - 4702 (2015)
Long-distance intramolecular nucleophilic reactions are promising strategies for the design of fluorogenic probes to detect enzymatic activity involved in lysine modifications. However, such reactions have been challenging and hence have not been established. In this study, we have prepared fluorogenic peptides that induce intramolecular reactions between lysine nucleophiles and electrophiles in distal positions. These peptides contain a lysine and fluor-escence-quenched fluorophore with a carbonate ester, which triggers nucleophilic transesterification resulting in fluorogenic response. Transesterification occurred under mild aqueous conditions despite the presence of a long nine-amino-acid spacer between the lysine and fluorophore. In addition, one of the peptides showed the fastest reaction kinetics with a half-life time of 3.7 min. Furthermore, the incorporation of this fluorogenic switch into the probes allowed rapid fluorogenic detection of histone deacetylase (HDAC) activity. These results indicate that the transesterification reaction has great potential for use as a general fluorogenic switch to monitor the activity of lysine-targeting enzymes.
SPLICEOSTATIN ANALOGS
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Page/Page column 202; 203; 204, (2014/05/24)
The present invention is directed to novel cytotoxic spliceostatin analogs (I) and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.
A magnetic biomimetic nanocatalyst for cleaving phosphoester and carboxylic ester bonds under mild conditions
Zheng, Yan,Duanmu, Chuansong,Gao, Yong
, p. 3215 - 3217 (2007/10/03)
As a result of the unique surface structure of nanospheres, Asp and His residues supported on a 12 nm maghemite nanoparticle worked collaboratively as a biomimetic nanocatalyst for hydrolyzing paraoxon (phosphoester) and 4-nitrophenyl acetate (carboxylic ester) in Milli-Q water (pH 7.0) at 37 °C, without employing extremes of pH or heavy metals. Our nanocatalyst could be facilely recovered via magnetic concentration. The isolated catalyst exhibited long-term stability, showing no significant loss of its catalytic activity for repeated uses after 3 months.