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991.
Diaminodiacid Bridges to Improve Folding and Tune the Bioactivity of Disulfide‐Rich Peptides
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Ye Guo De‐Meng Sun Feng‐Liang Wang Yao He Prof. Lei Liu Prof. Chang‐Lin Tian 《Angewandte Chemie (International ed. in English)》2015,54(48):14276-14281
Disulfide‐rich peptides containing three or more disulfide bonds are promising therapeutic and diagnostic agents, but their preparation is often limited by the tedious and low‐yielding folding process. We found that a single cystine‐to‐diaminodiacid replacement could significantly increase the folding efficiency of disulfide‐rich peptides and thus improve their production yields. The practicality of this strategy was demonstrated by the synthesis and folding of derivatives of the μ‐conotoxin SIIIA, the preclinical hormone hepcidin, and the trypsin inhibitor EETI‐II. NMR and X‐ray crystallography studies confirmed that these derivatives of disulfide‐rich peptide retained the correct three‐dimensional conformations. Moreover, the cystine‐to‐diaminodiacid replacement enabled structural tuning, thereby leading to an EETI‐II derivative with higher bioactivity than the native peptide. 相似文献
992.
Far‐Red and Near‐IR AIE‐Active Fluorescent Organic Nanoprobes with Enhanced Tumor‐Targeting Efficacy: Shape‐Specific Effects
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Andong Shao Prof. Dr. Yongshu Xie Shaojia Zhu Dr. Zhiqian Guo Shiqin Zhu Dr. Jin Guo Prof. Dr. Ping Shi Prof. Dr. Tony D. James Prof. Dr. He Tian Prof. Dr. Wei‐Hong Zhu 《Angewandte Chemie (International ed. in English)》2015,54(25):7275-7280
The rational design of high‐performance fluorescent materials for cancer targeting in vivo is still challenging. A unique molecular design strategy is presented that involves tailoring aggregation‐induced emission (AIE)‐active organic molecules to realize preferable far‐red and NIR fluorescence, well‐controlled morphology (from rod‐like to spherical), and also tumor‐targeted bioimaging. The shape‐tailored organic quinoline–malononitrile (QM) nanoprobes are biocompatible and highly desirable for cell‐tracking applications. Impressively, the spherical shape of QM‐5 nanoaggregates exhibits excellent tumor‐targeted bioimaging performance after intravenously injection into mice, but not the rod‐like aggregates of QM‐2. 相似文献
993.
Fluorescent In Situ Targeting Probes for Rapid Imaging of Ovarian‐Cancer‐Specific γ‐Glutamyltranspeptidase
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Feiyi Wang Prof. Ying Zhu Li Zhou Liang Pan Zhifen Cui Qiang Fei Sihang Luo Dr. Dun Pan Prof. Rui Wang Prof. Chunchang Zhao Prof. He Tian Prof. Chunhai Fan 《Angewandte Chemie (International ed. in English)》2015,54(25):7349-7353
γ‐Glutamyltranspeptidase (GGT) is a tumor biomarker that selectively catalyzes the cleavage of glutamate overexpressed on the plasma membrane of tumor cells. Here, we developed two novel fluorescent in situ targeting (FIST) probes that specifically target GGT in tumor cells, which comprise 1) a GGT‐specific substrate unit (GSH), and 2) a boron–dipyrromethene (BODIPY) moiety for fluorescent signalling. In the presence of GGT, sulfur‐substituted BODIPY was converted to amino‐substituted BODIPY, resulting in dramatic fluorescence variations. By exploiting this enzyme‐triggered photophysical property, we employed these FIST probes to monitor the GGT activity in living cells, which showed remarkable differentiation between ovarian cancer cells and normal cells. These probes represent two first‐generation chemodosimeters featuring enzyme‐mediated rapid, irreversible aromatic hydrocarbon transfer between the sulfur and nitrogen atoms accompanied by switching of photophysical properties. 相似文献
994.
Dr. Chun Zhang Zhen Wang Liangxiao Tan Tian‐Long Zhai Dr. Sheng Wang Prof. Bien Tan Prof. Yan‐Song Zheng Prof. Xiang‐Liang Yang Prof. Hui‐Bi Xu 《Angewandte Chemie (International ed. in English)》2015,54(32):9244-9248
A quadrangular prismatic tricyclooxacalixarene cage 1 based on tetraphenylethylene (TPE) was efficiently synthesized by a one‐pot SNAr condensation reaction. As a result of the porous internal structure in the solid state, cage 1 exhibited a good CO2 uptake capacity of 12.5 wt % and a high selectivity for CO2 over N2 adsorption of 80 (273 K, 1 bar) with a BET surface area of 432 m2 g?1. Formation of cage 1 led to the fluorescence of TPE being switched on in solution. The system was employed as a single‐molecule platform to study the mechanism of aggregation‐induced emission (AIE) by examining the restriction of intramolecular rotation (RIR). 相似文献
995.
Monitoring of Endogenous Hydrogen Sulfide in Living Cells Using Surface‐Enhanced Raman Scattering
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Dr. Da‐Wei Li Lu‐Lu Qu Kai Hu Prof. Dr. Yi‐Tao Long Prof. Dr. He Tian 《Angewandte Chemie (International ed. in English)》2015,54(43):12758-12761
Hydrogen sulfide (H2S) has emerged as an important gasotransmitter in diverse physiological processes, although many aspects of its roles remain unclear, partly owing to a lack of robust analytical methods. Herein we report a novel surface‐enhanced Raman scattering (SERS) nanosensor, 4‐acetamidobenzenesulfonyl azide‐functionalized gold nanoparticles (AuNPs/4‐AA), for detecting the endogenous H2S in living cells. The detection is accomplished with SERS spectrum changes of AuNPs/4‐AA resulting from the reaction of H2S with 4‐AA on AuNPs. The SERS nanosensor exhibits high selectivity toward H2S. Furthermore, AuNPs/4‐AA responds to H2S within 1 min with a 0.1 μM level of sensitivity. In particular, our SERS method can be utilized to monitor the endogenous H2S generated in living glioma cells, demonstrating its great promise in studies of pathophysiological pathways involving H2S. 相似文献
996.
Gold(I)‐Catalyzed Tandem Transformation with Diynes: Rapid Access to Linear Cyclopentenone‐Fused Polycyclic Molecules
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Congjun Yu Bin Chen Tian Zhou Qingshan Tian Prof. Dr. Guozhu Zhang 《Angewandte Chemie (International ed. in English)》2015,54(37):10903-10907
An efficient and convenient synthesis of useful linear cyclopentenone‐fused polycyclic compounds has been achieved through a novel gold(I)‐catalyzed transformation of diynes. The method demonstrates high product yields and tolerates of a wide variety of important functional groups. Gold‐vinylidene formation, methoxy group migration, and Nazarov‐type cyclization are proposed to be the key steps in the reaction pathway. The synthetic utility of this method is demonstrated by converting the product to eight‐membered‐ring‐fused compound. 相似文献
997.
Isomerization of Secondary Phosphirane into Terminal Phosphinidene Complexes: An Analogy between Monovalent Phosphorus and Transition Metals
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Jonathan Wong Yongxin Li Yanwei Hao Rongqiang Tian François Mathey 《Angewandte Chemie (International ed. in English)》2015,54(44):12891-12893
Secondary phosphirane complexes isomerize above 100 °C to give the corresponding terminal phosphinidene complexes, which can be trapped by alkenes and alkynes. This reaction is a rare instance of the isomerization of a PIII derivative into a PI derivative. It appears to mimic the reductive elimination of alkanes from transition‐alkylmetal hydrides. 相似文献
998.
Wrinkled Graphene Monoliths as Superabsorbing Building Blocks for Superhydrophobic and Superhydrophilic Surfaces
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Li‐Bing Lv Tian‐Lu Cui Bing Zhang Hong‐Hui Wang Prof. Xin‐Hao Li Prof. Jie‐Sheng Chen 《Angewandte Chemie (International ed. in English)》2015,54(50):15165-15169
Superhydrophobic and superhydrophilic surfaces are of great interest because of a large range of applications, for example, as antifogging and self‐cleaning coatings, as antibiofouling paints for boats, in metal refining, and for water–oil separation. An aqueous ink based on three‐dimensional graphene monoliths (Gr) can be used for constructing both superhydrophobic and superhydrophilic surfaces on arbitrary substrates with different surficial structures from the meso‐ to the macroscale. The surface wettability of a Gr‐coated surface mainly depends on which additional layers (air for a superhydrophobic surface and water for a superhydrophilic surface) are adsorbed on the surface of the graphene sheets. Switching a Gr‐coated surface between being superhydrophobic and superhydrophilic can thus be easily achieved by drying and prewetting with ethanol. The Gr‐based superhydrophobic membranes or films should have great potential as efficient separators for fast and gravity‐driven oil–water separation. 相似文献
999.
1000.
Cheng-Fang Wang Li Fan Mei Tian Shu-Shan Du Zhi-Wei Deng Jiang-Bin Feng 《Natural product research》2015,29(14):1380-1383
This work aimed to investigate benzophenanthridine from the roots of Zanthoxylum nitidum (Roxb.) DC. var. fastuosum How ex Huang for the first time. Thirteen benzophenanthridines were isolated, and our results of the cytotoxic activities indicated that compound 6 exhibited the best potency against A549, Hela, SMMC-7721 and EJ, with the IC50 values of 27.50, 37.50, 16.95 and 60.42 μM, respectively. Compounds 7 and 11 also showed strong cytotoxicity when tested against the four human cancer cell lines (A549, Hela, SMMC-7721 and EJ), while only compounds 12 and 13 displayed cytotoxicity in inhibiting BALL-1 proliferation among all the compounds. These results suggested that benzophenanthridines may become a valid alternative of potential basis for new anti-proliferative agents. 相似文献