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Niklas Jänsch Wisely Oki Sugiarto Marius Muth Aleksandra Kopranovic Charlotte Desczyk Matthias Ballweg Frank Kirschhöfer Dr. Gerald Brenner-Weiss Prof. Dr. Franz-Josef Meyer-Almes 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(58):13249-13255
Human histone deacetylase 8 is a well-recognized target for T-cell lymphoma and particularly childhood neuroblastoma. PD-404,182 was shown to be a selective covalent inhibitor of HDAC8 that forms mixed disulfides with several cysteine residues and is also able to transform thiol groups to thiocyanates. Moreover, HDAC8 was shown to be regulated by a redox switch based on the reversible formation of a disulfide bond between cysteines Cys102 and Cys153. This study on the distinct effects of PD-404,182 on HDAC8 reveals that this compound induces the dose-dependent formation of intramolecular disulfide bridges. Therefore, the inhibition mechanism of HDAC8 by PD-404,182 involves both, covalent modification of thiols as well as ligand mediated disulfide formation. Moreover, this study provides a deep molecular insight into the regulation mechanism of HDAC8 involving several cysteines with graduated capability to form reversible disulfide bridges. 相似文献
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Lei Li Yunpeng Liu Cheng Ma Jingyao Qu Angie D. Calderon Baolin Wu Na Wei Xuan Wang Yuxi Guo Zhongying Xiao Jing Song Go Sugiarto Yanhong Li Hai Yu Xi Chen Peng George Wang 《Chemical science》2015,6(10):5652-5661
Quantification, characterization and biofunctional studies of N-glycans on proteins remain challenging tasks due to the complexity, diversity and low abundance of these glycans. The availability of structurally defined N-glycan (especially isomer) libraries is essential to help solve these tasks. We report herein an efficient chemoenzymatic strategy, namely Core Synthesis/Enzymatic Extension (CSEE), for rapid production of diverse N-glycans. Starting with 5 chemically prepared building blocks, 8 N-glycan core structures containing one or two terminal N-acetyl-d-glucosamine (GlcNAc) residue(s) were chemically synthesized via consistent use of oligosaccharyl thioethers as glycosylation donors in a convergent fragment coupling strategy. Each of these core structures was then extended to 5 to 15 N-glycan sequences by enzymatic reactions catalyzed by 4 robust glycosyltransferases. Success in synthesizing N-glycans with Neu5Gc and core-fucosylation further expanded the ability of the enzymatic extension. Meanwhile, high performance liquid chromatography with an amide column enabled rapid and efficient purification (>98% purity) of N-glycans in milligram scales. A total of 73 N-glycans (63 isomers) were successfully prepared and characterized by MS2 and NMR. In summary, the CSEE strategy provides a practical approach for “mass production” of structurally defined N-glycans, which are important standards and probes for glycoscience. 相似文献
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Dr. Hai Yu Kam Lau Dr. Vireak Thon Chloe A. Autran Dr. Evelyn Jantscher‐Krenn Mengyang Xue Dr. Yanhong Li Dr. Go Sugiarto Dr. Jingyao Qu Shengmao Mu Dr. Li Ding Prof. Dr. Lars Bode Prof. Dr. Xi Chen 《Angewandte Chemie (International ed. in English)》2014,53(26):6687-6691
Two novel synthetic α2–6‐linked disialyl hexasaccharides, disialyllacto‐N‐neotetraose (DSLNnT) and α2–6‐linked disialyllacto‐N‐tetraose (DS′LNT), were readily obtained by highly efficient one‐pot multienzyme (OPME) reactions. The sequential OPME systems described herein allowed the use of an inexpensive disaccharide and simple monosaccharides to synthesize the desired complex oligosaccharides with high efficiency and selectivity. DSLNnT and DS′LNT were shown to protect neonatal rats from necrotizing enterocolitis (NEC) and are good therapeutic candidates for preclinical experiments and clinical application in treating NEC in preterm infants. 相似文献
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