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131.
Frontispiece: Irreversible Denaturation of Proteins through Aluminum‐Induced Formation of Backbone Ring Structures 下载免费PDF全文
132.
In Situ Proteome Profiling and Bioimaging Applications of Small‐Molecule Affinity‐Based Probes Derived From DOT1L Inhibitors 下载免费PDF全文
Biwei Zhu Dr. Hailong Zhang Sijun Pan Chenyu Wang Dr. Jingyan Ge Prof. Dr. Jun‐Seok Lee Prof. Dr. Shao Q. Yao 《Chemistry (Weinheim an der Bergstrasse, Germany)》2016,22(23):7824-7836
DOT1L is the sole protein methyltransferase that methylates histone H3 on lysine 79 (H3K79), and is a promising drug target against cancers. Small‐molecule inhibitors of DOT1L such as FED1 are potential anti‐cancer agents and useful tools to investigate the biological roles of DOT1L in human diseases. FED1 showed excellent in vitro inhibitory activity against DOT1L, but its cellular effect was relatively poor. In this study, we designed and synthesized photo‐reactive and “clickable” affinity‐based probes (AfBPs), P1 and P2 , which were cell‐permeable and structural mimics of FED1 . The binding and inhibitory effects of these two probes against DOT1L protein were extensively investigated in vitro and in live mammalian cells (in situ). The cellular uptake and sub‐cellular localization properties of the probes were subsequently studied in live‐cell imaging experiments, and our results revealed that, whereas both P1 and P2 readily entered mammalian cells, most of them were not able to reach the cell nucleus where functional DOT1L resides. This offers a plausible explanation for the poor cellular activity of FED1 . Finally with P1 / P2 , large‐scale cell‐based proteome profiling, followed by quantitative LC‐MS/MS, was carried out to identify potential cellular off‐targets of FED1 . Amongst the more than 100 candidate off‐targets identified, NOP2 (a putative ribosomal RNA methyltransferase) was further confirmed to be likely a genuine off‐target of FED1 by preliminary validation experiments including pull‐down/Western blotting (PD/WB) and cellular thermal shift assay (CETSA). 相似文献
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Zhenbei Zhang Tong-Xin Liu Qingfeng Liu Zhiguo Zhang Guisheng Zhang 《Tetrahedron: Asymmetry》2013,24(24):1591-1597
An alternative and efficient method to stereoselectively synthesize oxazolo[3,4-b]tetrahydroisoquinolin-3-ones via a Pictet–Spengler reaction promoted by Lewis acid TMSOTf from readily available (S)-4-benzyl-2-oxazolidinone with various aromatic, aliphatic, and cyclic aldehydes under room temperature is described. 相似文献
135.
An enantioselective hydrogenolysis of 3-aryl-3-hydroxyisoindolin-1-ones under H2 has been developed by using Ir(I)/(R)-MeO-Biphep complex as a catalyst. Cyclic diaryl methylamides were obtained in moderate to excellent yields and up to 92% ee. 相似文献
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Yunxia Huang Shuaipeng Ge Xiaojuan Chen Zhongcheng Xiang Xinran Zhang Ruoxuan Zhang Yimin Cui 《Chemistry (Weinheim an der Bergstrasse, Germany)》2019,25(62):14117-14122
The design of electrode materials with rational core/shell structures is promising for improving the electrochemical properties of supercapacitors. Hence, hierarchical FeCo2S4@FeNi2S4 core/shell nanostructures on Ni foam were fabricated by a simple hydrothermal method. Owing to their structure and synergistic effect, they deliver an excellent specific capacitance of 2393 F g−1 at 1 A g−1 and long cycle lifespan as positive electrode materials. An asymmetric supercapacitor device with FeCo2S4@FeNi2S4 as positive electrode and graphene as negative electrode exhibited a specific capacitance of 133.2 F g−1 at 1 A g−1 and a high energy density of 47.37 W h kg−1 at a power density of 800 W kg−1. Moreover, the device showed remarkable cycling stability with 87.0 % specific-capacitance retention after 5000 cycles at 2 A g−1. These results demonstrate that the hierarchical FeCo2S4@FeNi2S4 core/shell structures have great potential in the field of electrochemical energy storage. 相似文献
138.
Tian‐Jun Yue Ming‐Chao Zhang Ge‐Ge Gu Li‐Yang Wang Wei‐Min Ren Xiao‐Bing Lu 《Angewandte Chemie (Weinheim an der Bergstrasse, Germany)》2019,131(2):628-633
The precise synthesis of poly(thioester)s with diverse structures is still a significant challenge in the polymeric materials field. Herein, we report a novel approach to the synthesis of well‐defined poly(thioester)s by the controlled alternating copolymerization of cyclic thioanhydrides and episulfides induced by simple organic ammonium salts. Both the cation and anion have strong effects on the copolymerization. [PPN]OAc ([PPN]=bis(triphenylphosphine)iminium) with a bulky cation was proven to be efficient in initiating this polymerization, yielding poly(thioester)s with a completely alternating structure, controlled molecular weight, and narrow polydispersity. The poly(thioester) obtained from succinic thioanhydride and propylene sulfide is a typical semicrystalline material, possessing a high refractive index of up to 1.78. Because it uses readily available monomers, this method is expected to open up a new route to poly(thioester)s with diverse structures and properties. 相似文献
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Nan Jiang Xiao-Yu Yang Guo-Liang Ying Ling Shen Jing Liu Wei Geng Ling-Jun Dai Shao-Yin Liu Jian Cao Ge Tian Tao-Lei Sun Shi-Pu Li Bao-Lian Su 《Chemical science》2015,6(1):486-491
Self-repair is nature''s way of protecting living organisms. However, most single cells are inherently less capable of self-repairing, which greatly limits their wide applications. Here, we present a self-assembly approach to create a nanoshell around the cell surface using nanoporous biohybrid aggregates. The biohybrid shells present self-repairing behaviour, resulting in high activity and extended viability of the encapsulated cells (eukaryotic and prokaryotic cells) in harsh micro-environments, such as under UV radiation, natural toxin invasion, high-light radiation and abrupt pH-value changes. Furthermore, an interaction mechanism is proposed and studied, which is successful to guide design and synthesis of self-repairing biohybrid shells using different bioactive molecules. 相似文献