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Chinese Journal of Chemistry 2015年第9期33卷 1041-1048页

作者： qian li junfeng xiang yalin tang Beijing National Laboratory for Molecular Sciences (BNLMS) Center for Molecular SciencesState Key Laboratory for Structural Chemistry of Unstable and Stable Species Institute of Chemistry Chinese Aeademy of Sciences Beijing 100190 China

Compounds selectively binding and stabilizing G-quadruplex structures could inhibit the telomerase or down- regulate the oncogenes and may act as anti-cancer drugs. An alkaloid with non-flat structure, fangchinoline, showed to strongly stabilize the intermolecular and intramolecular parallel stranded G-quadruplex structure, increasing melting temperature by 20 and 23℃, respectively. The binding mode was investigated by using NMR and molec- ular modelling methods. Four human cell lines （HL-60, BGC-823, Be1-7402 and KB） were taken to test the an- ti-proliferation effects of fangchinoline and the IC50 values were ranged from 16 to 32 μmol/L. These results showed that the fangchinoline or related moiety derivatives may represent a class of telomere-targeted agents as po- tential anti-cancer drugs.

关键词： G-quadruplex alkaloid non-flat anti-cancer drug

Kinetic characterization of a slow chemical exchange between two sites in N,N-dimethylacetylamide by CEST NMR spectroscopy

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Chinese Chemical Letters 2022年第9期33卷 4335-4338页

作者： lixia Wang Jikun li junfeng xiang Jie Cui yalin tang Beijing National Laboratory for Molecular Sciences(BNLMS) Center for Molecular SciencesInstitute of ChemistryChinese Academy of SciencesBeijing 100190China University of Chinese Academy of Sciences Beijing 100049China

Nuclear magnetic resonance(NMR)spectroscopy has provided many powerful tools for the study of dynamic *** the reported methods,chemical exchange saturation transfer(CEST)is more suitable for systems with slow exchange rates,and there will be promising in the detection and dynamic mechanism of metastable *** has been widely used in magnetic resonance imaging(MRI),however whether it is applicable in the field of chemical kinetics needs more *** we studied,as a proof of concept,the kinetics of the slow chemical exchange between the two N-methyl protons of N,N-dimethylacetylamide(DMA),exploiting QUantifying Exchange using Z-spectrum(QUEZS)and QUantifying Exchange using Saturation Time(QUEST)*** turned out that both of QUEZS and QUEST could give the corresponding exchange rates,showcasing the capability of this method to provide accurate kinetic data under a range of *** results clearly demonstrated the reliability of CEST-based techniques as a tool for dynamic kinetics by NMR.

关键词： Chemical exchange saturation transfer(CEST) Chemical exchange N,N-Dimethylacetylamid Bloch-Mc Connell equation Dynamic kinetics

Metabonomics analysis of the urine of rats with Qi deficiency and blood stasis syndrome based on NMR techniques

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Chinese Science Bulletin 2007年第22期52卷 3068-3073页

作者： li lin WANG JianNong REN JianXun xiang junfeng tang yalin liU JianXun HANDing State Key Laboratory for Structural Chemistry of Unstable and Stable Species Institute of Chemistry Chinese Academy of Sciences Beijing 100080 China Xi Yuan Hospital China Academy of Chinese Medical Sciences Beijing 100091 China

Metabonomics analysis of the urine of rats with Qi deficiency and blood stasis syndrome has been performed by comparison with those of normal rats based on NMR techniques. The relative contents of formate,creatinine,2-oxoglutarate(2-OG) ,citrate,taurine,trimethylamine-N-oxide(TMAO) ,succinate and hippurate in the urine of the rats with Qi deficiency and blood stasis syndrome have been changed. These results have provided evidence for understanding the mechanism and the therapy of Qi defi-ciency and blood stasis syndrome.

关键词：代谢组学尿大鼠血液核磁共振技术

Roles of flanking sequences in the binding between unimolecular parallel-stranded G-quadruplexes and ligands

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Science Bulletin 2013年第7期58卷 731-744页

作者： GAI Wei YANG qianFan xiang junfeng SUN HongXia SHANG qian li qian JIANG Wei GUAN AiJiao ZHANG Hong tang yalin XU GuangZhi Beijing National Laboratory for Molecular Sciences Center for Molecular SciencesState Key Laboratory for Structural Chemistry for Unstable and Stable SpeciesInstitute of ChemistryChinese Academy of Sciences Graduate University of Chinese Academy of Sciences

G-quadruplexes attract more and more attention in recent *** small molecules which can induce or stabilize the formation of G-quadruplexes have been investigated on the purpose of anticancer drug *** a motif existed in physiological condition,flanking sequences are an important part of G-quadruplexes but the study on the impact of flanking sequences on (G-quadruplex)-ligand binding is rarely *** this paper,the effects of flanking sequences on binding affinity between a series of unimolecular parallel-stranded G-quadruplex sequences derived from c-myc oncogene promoter (termed as c-myc G-quadruplexes) and their ligands are discussed in *** results showed that the flanking sequences on c-myc G-quadruplexes play key roles in (G-quadruplex)-ligand *** a c-myc G-quadruplex is bound to its ligands,the flanking sequences might form a binding cavity above the terminal G-quartet,which could provide a suitable site for ligands to dock ***,the bases on flanking sequences could interact with ligand through π-π stacking,and finally form a sandwich-stacking mode (terminal G-quartet,ligand and bases on the flanking sequence).This mode could stabilize the (G-quadruplex)-ligand complex effectively and enhance the binding affinity ***,flanking sequences are also found to exhibit steric hindrance effect which could impede the (G-quadruplex)-ligand binding.

关键词： G-quadruplex flanking sequences interaction mechanism c-myc cyanine dye

An important functional group, benzo[1,3]dioxole, of alkaloids induces the formation of the human telomeric DNA G-quadruplex

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Chinese Science Bulletin 2011年第7期56卷 613-617页

作者： YANG Shu xiang junfeng YANG qianFan ZHOU QiuJu ZHANG XiuFeng li qian tang yalin XU GuangZhi Beijing National Laboratory for Molecular Sciences Centre for Molecular SciencesState Key Laboratory for Structural Chemistry for Unstable and Stable SpeciesInstitute of ChemistryChinese Academy of SciencesBeijing 100190China Graduate University of Chinese Academy of Sciences Beijing 100049China

Over the past few decades, numerous molecules have been discovered or designed to interact efficiently and selectively with a peculiar DNA structure named G-quadruplex. Some of these molecules have been developed as anticancer agents. To aid the design of anticancer agents, the ability of alkaloids possessing Protoberberine and Benzophenanthridine groups to induce the formation of G-quadruplexes were studied using CD spectroscopy. By careful examination of their structures, we found that a benzo[1,3]dioxole group plays an important role in influencing their inductive properties. The more functional groups the alkaloids have, the stronger their G-quadruplex inductive ability.

关键词：端粒DNA 生物碱诱导职能人类四链苯抗癌药物

Roles of flanking sequences in the binding between unimolecular parallel-stranded G-quadruplexes and ligands

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Science China(Technological Sciences) 2013年第3期56卷 731-740页

关键词： G-quadruplex flanking sequences interaction mechanism c-myc cyanine dye

HTG-四链体对甲基氮杂杯[6]吡啶的构象调控

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化学通报 2018年第9期81卷 828-833页

作者：李敬晨管爱娇向俊锋张恩选李骞齐伟孙红霞唐亚林曲阜师范大学化学与化工学院曲阜273100 中国科学院化学研究所分子动态与稳态结构国家重点实验室北京100190 中国科学院大学北京100049 凯莱英医药集团天津市药物绿色合成技术企业重点实验室天津300457

甲基氮杂杯[n]吡啶(MACPn)是一类柔性、多构象的新型杂杯杂芳烃化合物,溶液状态中对其构象的调控与分离一直是此类化合物研究的难点之一。我们将DNA G-四链体作为功能分子,调控甲基氮杂杯[6]吡啶(MACP6)在溶液态的构象,结果表明,HT序列... 详细信息

甲基氮杂杯[n]吡啶(MACPn)是一类柔性、多构象的新型杂杯杂芳烃化合物,溶液状态中对其构象的调控与分离一直是此类化合物研究的难点之一。我们将DNA G-四链体作为功能分子,调控甲基氮杂杯[6]吡啶(MACP6)在溶液态的构象,结果表明,HT序列在K^+条件下所形成的混合结构的G-四链体可以诱导MACP6的手性构象,而在Na^+条件下所形成的反平行结构不具备此功能。一维核磁共振氢谱、分子对接与碱基突变进一步揭示了HT G-四链体与MACP6以边沿loop为位点的构型匹配作用模式,loop区增长,有利于HT G-四链体对MACP6的调控作用。本研究再次拓展了G-四链体作为氮杂杯吡啶构象调控功能分子的应用。

关键词：甲基氮杂杯[n]吡啶 G-四链体手性诱导构象调控

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天然抗肿瘤分子筛选方法研究新进展

中国基础科学 2008年第4期10卷 13-14页

作者：周秋菊李林向俊锋唐亚林中科院化学研究所北京分子科学国家实验室(筹)分子动态与稳态结构国家重点实验室

The development of a simple and efficient method, which allows to fast screen compounds with high biological activity from natural plant extracts, is an attractive field in drug discovery. Our group propounded a novel method for fast screening and structural identification of antitumor agents from natural plant extracts by coupling the DNA target molecule’s recognition with NMR techniques. By introduction of DNA target molecule into natural plant extracts, the ligand(s) in the extracts will be recognized by target molecule and therefore can be monitored by NMR techniques. Our tactics includes the following three steps: judging the existence of G-quadruplex ligand(s) in the test extracts by 1H NMR spectra; detecting the characteristic peak(s) of G-quadruplex ligand(s) using DOSY NMR methods; and subsequently identifying the structure of G-quadruplex ligand(s) by 2D NMR experiments such as HSQC and HMBC. By the combination of G-quadruplex recognition and NMR methods, we have successfully obtained several active molecules stabilizing G-quadruplex with high cytotoxicity from two kinds of natural product extracts.

关键词：现代分子生物学技术天然产物抗肿瘤活性筛选方法抗癌药物药物研发活性筛选高等植物

Safety and efficacy of meplazumab in healthy volunteers and COVID-19 patients: a randomized phase 1 and an exploratory phase 2 trial

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Signal Transduction and Targeted Therapy 2021年第6期6卷 1845-1855页

作者： Huijie Bian Zhao-Hui Zheng Ding Wei Aidong Wen Zheng Zhang Jian-Qi lian Wen-Zhen Kang Chun-Qiu Hao Jing Wang Rong-Hua Xie Ke Dong Jie-Lai Xia Jin-lin Miao Wen Kang Guoquan li Di Zhang Mingru Zhang Xiu-Xuan Sun likun Ding Kui Zhang junfeng Jia Jin Ding Zhiqin li Yanyan Jia lin-Na liu Zhe Zhang Zhao-Wei Gao Hong Du Na Yao Qing Wang Ke Wang Jie-Jie Geng Bin Wang Ting Guo Ruo Chen Yu-Meng Zhu li-Juan Wang qian He Rui-Rui Yao Ying Shi xiang-Min Yang Jian-Sheng Zhou Yi-Nan Ma Ya-Tao Wang Xue liang Fei Huo Zhe Wang Yang Zhang Xu Yang Ye Zhang Lu-Hua Gao ling Wang Xiao-Chun Chen Hao tang Shuang-Shuang liu Qing-Yi Wang Zhi-Nan Chen Ping Zhu National Translational Science Center for Molecular Medicine and Department of Cell Biology Fourth Military Medical UniversityXi'anChina Department of Clinical Immunology Xijing HospitalFourth Military Medical UniversityXi'anChina Department of Pharmacy Xijing HospitalFourth Military Medical UniversityXi'anChina Center for Infectious Diseases Tangdu HospitalFourth Military Medical UniversityXi'anChina Department of Nuclear Medicine Xijing HospitalFourth Military Medical UniversityXi'anChina department of Clinical Diagnosis Tangdu HospitalFourth Military Medical UniversityXKanChina College of Military Preventive Medicine Fourth Military Medical UniversityXi'anChina Department of Pharmaceutics Tangdu HospitalFourth Military Medical UniversityXi'anChina Department of Pathology Fourth Military Medical UniversityXi'anChina Jiangsu Pacific Meinuoke Biopharmaceutical Co.Ltd ChangzhouChina Department of Foreign Languages Fourth Military Medical UniversityXi'anChina

Recent evidence suggests that CD147 serves as a novel receptor for severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)*** CD147 via anti-CD147 antibody could suppress the in vitro SARS-CoV-2 *** is a humanized anti-CD147 IgG_(2) monoclonal antibody,which may effectively prevent SARS-CoV-2 infection in coronavirus disease 2019(COVID-19)***,we conducted a randomized,double-blinded,placebo-controlled phase 1 trial to evaluate the safety,tolerability,and pharmacokinetics of meplazumab in healthy subjects,and an open-labeled,concurrent controlled add-on exploratory phase 2 study to determine the efficacy in COVID-19 *** phase 1 study,59 subjects were enrolled and assigned to eight cohorts,and no serious treatment-emergent adverse event(TEAE)or TEAE grade≥3 was *** serum and peripheral blood Cmax and area under the curve showed non-linear pharmacokinetic *** obvious relation between the incidence or titer of positive anti-drug antibody and dosage was observed in each *** biodistribution study indicated that meplazumab reached lung tissue and maintained>14 days stable with the lung tissue/cardiac blood-pool ratio ranging from 0.41 to *** the exploratory phase 2 study,17 COVID-19 patients were enrolled,and 11 hospitalized patients were involved as concurrent *** meplazumab treatment significantly improved the discharged(P=0.005)and case severity(P=0.021),and reduced the time to virus negative(P=0.045)in comparison to the control *** results show a sound safety and tolerance of meplazumab in healthy volunteers and suggest that meplazumab could accelerate the recovery of patients from COVID-19 pneumonia with a favorable safety profile.

关键词： patients dosage phase

An important functional group, benzo[1,3]dioxole, of alkaloids induces the formation of the human telomeric DNA G-quadruplex

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Science Bulletin 2011年第7期 611-617页

作者： YANG Shu1,2, xiang junfeng1, YANG qianFan1,2, ZHOU QiuJu1,2, ZHANG XiuFeng1, li qian1,2, tang yalin1 & XU GuangZhi1 1 Beijing National Laboratory for Molecular Sciences, Centre for Molecular Sciences, State Key Laboratory for Structural Chemistry for Unstable and Stable Species Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China 2 Graduate University of Chinese Academy of Sciences, Beijing 100049, China

关键词： benzo[1 3]dioxole group telomeric DNA G-quadruplex alkaloids Protoberberine Benzophenanthridine