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Discovery of a highly selective VEGFR2 kinase inhibitor CHMFL-VEGFR2-002 as a novel antiangiogenesis agent

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Acta Pharmaceutica Sinica B 2020年第3期10卷 488-497页

作者： Zongru Jiang li wang Xuesong liu cheng chen Beilei wang Wenliang wang chen Hu Kailin Yu Ziping Qi Qingwang liu Aoli wang Jing liu Guangchen Hong Wenchao wang Qingsong liu High Magnetic Field Laboratory Key Laboratory of High Magnetic Field and Ion Beam Physical BiologyHefei Institutes of Physical ScienceChinese Academy of SciencesHefei 230031China University of Science and Technology of china Hefei 230026China Precision Targeted Therapy Discovery Center Institute of Technology InnovationHefei Institutes of Physical ScienceChinese Academy of SciencesHefei 230088China Precision Medicine Research Laboratory of Anhui Province Hefei 230088China Qingdao Shinan District People's Hospital Qingdao 266002China Institutes of Physical Science and Information Technology Anhui UniversityHefei 230601China

Angiogenesis is an essential process in tumor growth,invasion and *** receptor 2(VEGFR2)inhibitors targeting tumor angiogenic pathway have been widely used in the clinical cancer ***,most of currently used VEGFR2 kinase inhibitors are multi-target inhibitors which might result in target-associated side effects and therefore limited clinical *** selective VEGFR inhibitors are still highly demanded from both basic research and clinical application point of *** we report the discovery and characterization of a novel VEGFR2 inhibitor(CHMFLVEGFR2-002),which exhibited high selectivity among structurally closed kinases including PDGFRs,FGFRs,CSF1 R,***-VEGFR2-002 displayed potent inhibitory activity against VEGFR2 kinase in the biochemical assay(IC50=66 nmol/L)and VEGFR2 autophosphorylation in cells(EC50s^100 nmol/L)as well as potent anti-proliferation effect against VEGFR2 transformed BaF3 cells(GI50=150 nmol/L).In addition,CHMFL-VEGFR2-002 also displayed good anti-angiogenesis efficacy in vitro and exhibited good in vivo PK(pharmacokinetics)profile with bioavailability over 49%and antiangiogenesis efficacy in both zebrafish and mouse models without apparent *** results suggest that CHMFL-VEGFR2-002 might be a useful research tool for dissecting new functions of VEGFR2 kinase as well as a potential anti-angiogenetic agent for the cancer therapy.

关键词： Cancer VEGFR2 kinase Kinase inhibitor Angiogenesis Inhibitor selectivity

基于测试系统柔度分析的水压致裂法确定最大水平主应力误差分析与讨论

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岩石力学与工程学报 2024年第S1期43卷 3385-3396页

作者：杨跃辉孙东生秦向辉李阿伟孙炜锋张重远李冉孟文陈群策中国地质科学院地质力学研究所北京100081 自然资源部地应力工程技术创新中心北京100081

最大水平主应力测量结果误差较大是水压致裂地应力测量方法中存在的突出问题。在梳理国内外水压致裂地应力测量规程或建议方法的基础上,对比分析用于计算最大水平主应力的几个主要公式之间的差异及其适用性,并以测试系统柔度为主要影响... 详细信息

最大水平主应力测量结果误差较大是水压致裂地应力测量方法中存在的突出问题。在梳理国内外水压致裂地应力测量规程或建议方法的基础上,对比分析用于计算最大水平主应力的几个主要公式之间的差异及其适用性,并以测试系统柔度为主要影响因素,较为细致和深入地分析影响最大水平主应力计算精度的误差来源及其物理机制。在此基础上,以甘肃北山花岗岩钻孔获取的深孔水压致裂实测数据为例,基于KGD理论模型对裂缝重张过程进行数值分析,定量研究系统柔度对最大水平主应力计算结果的影响。以剔除柔度影响因素的理论计算值为“修正值”,给出孔深18~930m深度范围共计6个测段的实测数据和“理论修正值”,结果表明,受系统柔度影响,随测试深度增加,最大水平主应力测试结果误差逐渐增加。当测试深度为930 m时,测量结果的相对误差为24.55%。研究结果可为相关工程应用中最大水平主应力测量结果误差问题提供参考,也为开展水压致裂地应力测量的误差分析,以及进一步提升测量结果的可靠性提供一种新的研究思路和技术途径。

关键词：岩石力学水压致裂法系统柔度重张压力最大水平主应力误差分析

HMGB1参与人参皂苷Rg1改善糖尿病大鼠缺血性脑卒中的作用

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药学学报 2018年第6期53卷 958-965页

作者：楚世峰周欣张钊陈晨罗飘陈乃宏中国医学科学院、北京协和医学院药物研究所神经科学中心北京100050 湖南中医药大学药学院湖南长沙410208

人参皂苷Rg1是多种脑卒中和糖尿病治疗药物的共有成分,但是Rg1对糖尿病合并脑卒中的治疗作用尚不清楚。本文旨在观察Rg1对糖尿病大鼠缺血性脑卒中的治疗作用,并观察Rg1对糖尿病大鼠卒中后神经炎症及高迁移率族蛋白1(high mobility group... 详细信息

人参皂苷Rg1是多种脑卒中和糖尿病治疗药物的共有成分,但是Rg1对糖尿病合并脑卒中的治疗作用尚不清楚。本文旨在观察Rg1对糖尿病大鼠缺血性脑卒中的治疗作用,并观察Rg1对糖尿病大鼠卒中后神经炎症及高迁移率族蛋白1(high mobility group box1,HMGB1)信号分子的变化。结果显示,Rg1可显著缩小糖尿病大鼠卒中后大脑梗死率,降低行为学评分,减轻脑水肿系数,具有治疗糖尿病大鼠脑卒中的功效。进一步研究发现,Rg1可缓解卒中后炎症反应,降低卒中后HMGB1蛋白的表达,而外源性增加HMGB1可显著抑制Rg1的神经保护作用,表明HMGB1参与了Rg1抗脑卒中作用。

关键词：人参皂苷Rg1 缺血性脑卒中糖尿病高迁移率族蛋白神经炎症

Syntheses of Novel Macrocyclic Polyarylate Oligomers Based on Phenolphthalein and m-Phthaloyl dichloride

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Chemical Research in chinese Universities 1999年第4期15卷 350-353页

作者： gao Jun-bo wang Jun-zuo SUN Hui li Ke ZHANG Wan-jin chen chun-hai WU Zhong-wen JI Yi-ping Department of Chemistry Jilin UniverstryChangchun 130023P.R.China Changchun Institute of Applied Chemistry Chinese Academy of SciencesChangchun 130021P.R.China

Novel macrocyclic oligomers were synthesized through the condensation of phenolphthalein and m phthaloyl dichloride with triethylamine as catalyst in the mixed solution of methylene chloride and THF via pseudo high dilution technique. The oligomers were characterized by IR, 1H NMR , MS, WAXD, TGA and DSC. It was found that the 3∶3 adduct(molar ratio of phenolphthalein to m phthaloyl dichloride) and the 4∶4 adduct were the main products and there was a small amount of crystalline in the macrocyclic mixtures. When the mixtures were heated to 360 ℃ , the crystalline disappeared.

关键词： macrocyclic oligomer pseudo high dilution technique polycondensation ring opening polymerization thermal behavior.

Design of antibacterial peptide-like conjugated molecule with broad spectrum antimicrobial ability

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Science china Chemistry 2018年第1期61卷 113-117页

作者： Hui chen Meng li Zhang liu Rong Hu Shengliang li Yuan Guo Fengting Lv libing liu Yilin wang Yuanping Yi Shu wang Key Laboratory of Organic Solids Institute of Chemistry Chinese Academy of Sciences Key Laboratory of Colloid Interface and Chemical Thermodynamics Institute of ChemistryChinese Academy of Sciences

Increasing multidrug-resistant （MDR） superbugs emerge worldwide causing a public health crisis. Consequently, it is urgent to find new antibiotics with efficient broad-spectrum antimicrobial activity. By virtue of versatility in molecular design, a new peptide-like cell membrane-broken molecule, oligo-（7,7＇-bifluoren-benzo[c][1,2,5]thiadiazole）（OFBT） possessing a conjugated backbone and eight pendant guanidyl moieties was designed and synthesized. OFBT exhibits favorable broad-spectrum of antirnicrobial activity to pathogens including Gram-negative and Gram-positive bacteria, and fungi with the minimum inhibitory concentration （MIC） below 3.0 μM. Moreover, OFBT exhibits high selectivity for pathogens over human cells to make it a promising broad spectrum antimicrobial agent.

关键词： OFBT broad spectrum antimicrobial activity

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雅万高铁自动售票机软件研究

铁路计算机应用 2024年第6期33卷 40-45页

作者：李士达张曦李男陈晨尹伊伊中国铁道科学研究院集团有限公司电子计算技术研究所北京100081 北京经纬信息技术有限公司北京100081 北京勤实信息技术有限公司北京100089

印尼雅加达—万隆高速铁路(简称:雅万高铁)自动售票服务在售票规则、票务系统对接方式上与国内铁路自动售票系统存在较大差异。针对以上问题,结合国内自动售票的成熟技术经验,研究雅万高铁自动售票机(TVM,Ticket Vending Machine)机内... 详细信息

印尼雅加达—万隆高速铁路(简称:雅万高铁)自动售票服务在售票规则、票务系统对接方式上与国内铁路自动售票系统存在较大差异。针对以上问题,结合国内自动售票的成熟技术经验,研究雅万高铁自动售票机(TVM,Ticket Vending Machine)机内软件。在机内软件的结构上,将其分为通信控制进程、人机交互进程、机内维护进程和硬件控制进程,由通信控制进程负责其他各进程间的数据交互;人机交互进程基于***框架开发,实现TVM与旅客的友好交互、与票务系统的高效对接,以及便捷的升级服务。通过在雅万高铁的实际应用表明,该软件可很好地满足旅客的出行需要。

关键词：自动售票系统雅万高铁 NW.js框架自动售票机(TVM) 机内软件

Machine learning modeling identifies hypertrophic cardiomyopathy subtypes with genetic signature

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Frontiers of Medicine 2023年第4期17卷 768-780页

作者： Jiaqi Dai Tao wang Ke Xu Yang Sun Zongzhe li Peng chen Hong wang Dongyang Wu Yanghui chen Lei Xiao Hao liu Haoran Wei Rui li liyuan Peng Ting Yu Yan wang Zhongsheng Sun Dao Wen wang Division of Cardiology Department of Internal MedicineTongji HospitalTongji Medical CollegeHuazhong University of Science and TechnologyWuhan 430030China beijing Institutes of life Science Chinese Academy of SciencesBeijing 100101China Hubei Key Laboratory of Genetics and Molecular Mechanism of Cardiologic Disorders Huazhong University of Science and TechnologyWuhan 430030China

Previous studies have revealed that patients with hypertrophic cardiomyopathy(HCM)exhibit differences in symptom severity and prognosis,indicating potential HCM subtypes among these ***,793 patients with HCM were recruited at an average follow-up of 32.78±27.58 months to identify potential HCM subtypes by performing consensus clustering on the basis of their echocardiography ***,we proposed a systematic method for illustrating the relationship between the phenotype and genotype of each HCM subtype by using machine learning modeling and interactome network detection techniques based on whole-exome sequencing *** independent cohort that consisted of 414 patients with HCM was recruited to replicate the ***,two subtypes characterized by different clinical outcomes were identified in *** with subtype 2 presented asymmetric septal hypertrophy associated with a stable course,while those with subtype 1 displayed left ventricular systolic dysfunction and aggressive *** learning modeling based on personal whole-exome data identified 46 genes with mutation burden that could accurately predict subtype ***,the patients in another cohort predicted as subtype 1 by the 46-gene model presented increased left ventricular end-diastolic diameter and reduced left ventricular ejection *** employing echocardiography and genetic screening for the 46 genes,HCM can be classified into two subtypes with distinct clinical outcomes.

关键词： machine learning methods hypertrophic cardiomyopathy genetic risk

玉米抗南方锈病种质资源初步鉴定及遗传多样性分析

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植物遗传资源学报 2018年第2期19卷 225-231,242页

作者：陈文娟李万昌杨知还孙素丽王晓鸣朱振东段灿星河南师范大学生命科学学院新乡453007 中国农业科学院作物科学研究所/国家农作物基因资源与基因改良重大科学工程北京100081

南方锈病是玉米生产上的重要病害。2013-2015年在广西南宁和北京昌平对903份玉米种质资源进行了抗南方锈病的初步鉴定与评价,并利用SSR标记对筛选出的部分抗性材料进行了遗传多样性分析。结果表明,在903份种质中,8份自交系在广西南宁和... 详细信息

南方锈病是玉米生产上的重要病害。2013-2015年在广西南宁和北京昌平对903份玉米种质资源进行了抗南方锈病的初步鉴定与评价,并利用SSR标记对筛选出的部分抗性材料进行了遗传多样性分析。结果表明,在903份种质中,8份自交系在广西南宁和北京昌平均对南方锈病表现高抗(HR),占总鉴定种质的0.9%;29份材料表现为抗病(R),占比3.2%,包括27份自交系和2份农家种;中抗种质(MR)100份,占比11.1%;感病(S)和高感(HS)种质分别为181和585份,占鉴定材料的20.0%和64.8%。由此可见,玉米资源中高抗南方锈病的种质较为匮乏,在不同地点均表现高抗的材料是难得的抗源。不同地理来源的玉米种质对南方锈病的抗性水平存在较大差异,其中抗性资源较为丰富的是源自内蒙古和山西的种质。42对多态性SSR引物在50份抗锈病材料中,共扩增出141个条带,多态性条带139个,多态位点百分率(PPB)为98.58%。平均等位基因数(Na)1.98,平均有效等位基因数(Ne)1.59,平均Nei's基因多样性(H)0.34,平均多态性信息含量(PIC)0.78,平均Shannon's信息指数(I)0.51;通过UPGMA聚类分析,50份抗病材料被划分为2个类群,其中,第Ⅰ类群又可划分为5个亚类,表现出较高的遗传多样性,为抗病育种中抗源的选择和利用提供参考信息。

关键词：玉米南方锈病抗性鉴定 SSR标记遗传多样性

Influence of North Pacific SST on heavy precipitation events in autumn over North china

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Atmospheric and Oceanic Science Letters 2017年第1期10卷 21-28页

作者： li Hui-Xin chen Huo-Po wang Hui-Jun International Research Center Institute of Atmospheric PhysicsChinese Academy of SciencesCollege of Earth ScienceGraduate University of Chinese Academy of SciencesCollaborative Innovation Center on Forecast and Evaluation of Meteorological DisastersNanjing University of Information Science ＆ Technologylntemational Joint Laboratory on Climate and Environment ChangeClimate Change Research CenterChinese Academy of Science

The characteristics of heavy precipitation occurrence in autumn（the month of September） over North china are investigated using daily observational *** indicate that heavy precipitation events experienced a significant decadal increase in 2000/*** investigation reveals a close connection between heavy precipitation occurrence and simultaneous North Pacific *** SST anomaly over the North Pacific can result in intensification of the western North Pacific subtropical high and increased water vapor transport from the tropical ocean,which benefits the occurrence of heavy precipitation over North ***,the key region of North Pacific SST influencing heavy precipitation events over North china was different in the periods 1960-2000 and 2001-2014,being located over the eastern Ocean to china in the first period but more eastward in the second *** drift in the key region of SST is partly responsible for the decadal increase in heavy precipitation events over North china since 2000/***,the changes in SST variability（a decrease in the eastern Ocean to china and an increase to its east） may have been the main reason for the eastward movement of the key region in the latter ***,more work is needed in the future to verify the findings of this study.

关键词： Heavy precipitation autumn North china sea surface temperature North Pacific