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Chinese Journal of Chemistry 2021年第3期39卷 671-676页

作者： Chen-Xi Yu Bing-Yan Wei xue-qing kong Cai-Guang Yang Fa-Jun Nan State Key Laboratory of Drug Research the National Center for Drug ScreeningShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced StudyUCASHangzhouZhejiang 310024China Yantai Key Laboratory of Nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaYantaiShandong 264000China

Main observation and conclusion Methicillin-resistant Staphylococcus aureus(MRSA)has become a major threat on public health because of the increase of clinically isolated strains that exhibit resistance to many ***,development of new antibiotics for the treatment of MRSA in-fection is a sustained *** have previously identified a ring-opened bengamide analogue L472-2 that displays moderate ac-tivity against the growth of *** our previous work,we started from L472-2 and identified a class of analogues containing al-kynyl groups which have the potential to activate SaCIpP activity but moderate antibacterial ***,we focused on the anti-bacterial activity of L472-2,and a novel series of ring-opened bengamide analogues were synthesized and their activities were evalu-ated against *** conducting a compact analysis of the structure-activity relationships(SAR)of these analogues,we found that an adamantane ethanol ester bengamide 2j showed excellent antibacterial activity towards six *** strains,including MRSA,while it does not activate ***,these bengamide analogues represent a new class of candidates that suppress MRSA via-bility..

关键词： Bengamides Staphylococcus aureus Antibiotics Structure-activity relationships Pharmacokinetic

Design,Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators

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Chinese Journal of Chemistry 2020年第10期38卷 1111-1115页

作者： xue-qing kong Bing-Yan Wei Chen-Xi Yu Xiang Na Guan Wei-Ping Ma Gang Liu Cai-Guang Yang Fa-Jun Nan Chinese National Center for Drug Screening CAS Key Laboratory of Receptor ResearchStote Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China Yantai Key Laboratory of Nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaNo.39Science and Technology AvenueHigh-tech Industrial Development ZoneYantaiShandong 264000China

Summary of main observation and conclusion To combat multidrug-resistant Gram-positive bacteria,new antimicrobials particularly those with novel mechanism of action are badly *** with conventional antibiotics which are typical inhibitors,small-molecule activators of bacterial CIpP represent a new class of *** ClpP activator has been developed for clinical ***,we conducted a screening on our library of benga-mide-like ring opened analogues and found that L472-2 possesses a low minimum inhibitory concentration(MIC)against *** and shows no activity for ClpP activation in vitro,but it displayed reduced antibacterial activity against *** with clpP *** order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity,we perform further structural modifications starting from *** 37 re-mains the antimicrobial activity and activation of ClpP protein in vitro,which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.

关键词： analogues activation starting

Lightweight Malicious Code Classification Method Based on Improved Squeeze Net

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Computers, Materials & Continua 2024年第1期78卷 551-567页

作者： Li Li Youran kong qing Zhang School of Computer and Control Engineering Northeast Forestry UniversityHarbin150040China

With the growth of the Internet,more and more business is being done online,for example,online offices,online education and so *** this makes people’s lives more convenient,it also increases the risk of the network being attacked by malicious ***,it is important to identify malicious codes on computer systems ***,most of the existing malicious code detection methods have two problems:(1)The ability of the model to extract features is weak,resulting in poor model performance.(2)The large scale of model data leads to difficulties deploying on devices with limited ***,this paper proposes a lightweight malicious code identification model Lightweight Malicious Code Classification Method Based on Improved SqueezeNet(LCMISNet).In this paper,the MFire lightweight feature extraction module is constructed by proposing a feature slicing module and a multi-size depthwise separable convolution *** feature slicing module reduces the number of parameters by grouping *** multi-size depthwise separable convolution module reduces the number of parameters and enhances the feature extraction capability by replacing the standard convolution with depthwise separable convolution with different convolution kernel *** addition,this paper also proposes a feature splicing module to connect the MFire lightweight feature extraction module based on the feature reuse and constructs the lightweight model *** malicious code recognition accuracy of LCMISNet on the BIG 2015 dataset and the Malimg dataset reaches 98.90% and 99.58%,*** proves that LCMISNet has a powerful malicious code recognition *** addition,compared with other network models,LCMISNet has better performance,and a lower number of parameters and computations.

关键词： Lightweight neural network malicious code classification feature slicing feature splicing multi-size depthwise separable convolution

Open-Shell Oligomers and Polymers: Theory, Characterization Methods, Molecular Design, and Applications

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Chinese Journal of Polymer Science 2024年第4期42卷 417-436页

作者： xue-qing Wang Cheng Song Ting Lei Key Laboratory of Polymer Chemistry and Physics(Ministry of Education) School of Materials Science and EngineeringPeking UniversityBeijing100871China

Open-shell oligomers and polymers have exhibited intriguing electronic and magnetic properties, making them highly desirable for a wide range of applications, including ambipolar organic field-effect transistors (OFETs), photodetectors, organic thermoelectrics, and spintronics. Although open-shell ground states have been observed in certain small molecules and doped organic semiconductors, the exploration of open-shell ground-state conjugated polymers is still limited, and the strategies for designing these polymers remain obscure. This review aims to briefly introduce the theory and characterization methods of open-shell conjugated polymers, along with an overview of recent progress and applications. The objective is to stimulate further advancements and investigations in this promising area by shedding light on the potential of open-shell conjugated polymers and the challenges that lie ahead.

关键词： Conjugated polymers Open-shell molecules High-spin ground state Donor-acceptor(D-A)polymers Optoelectronic and magnetic properties

All types of base conversions allowed by base editors

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Science China(Life Sciences) 2024年第2期67卷 431-433页

作者： Shun-qing Liang Wen xue RNA Therapeutics Institute UMass Chan Medical SchoolWorcester 01655USA Department of Molecular Cell and Cancer BiologyUMass Chan Medical SchoolWorcester 01655USA Department of Molecular Medicine UMass Chan Medical SchoolWorcester 01655USA Li Weibo Institute for Rare Diseases Research UMass Chan Medical SchoolWorcester 01655USA

Base editors(BEs) hold great promise as tools for introducing single-base-pair changes in both basic research and therapeutic applications(Rees and Liu,2018).Base editors are composed of a Cas9 nickase fused to a DNA-modifying enzyme,which chemically modifies nucleobases within a specific targeting window near the Cas9-binding site.

关键词： base bases allowed

A GAN-EfficientNet-Based Traceability Method for Malicious Code Variant Families

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Computers, Materials & Continua 2024年第7期80卷 801-818页

作者： Li Li qing Zhang Youran kong School of Computer and Control Engineering Northeast Forestry UniversityHarbin150040China

Due to the diversity and unpredictability of changes in malicious code,studying the traceability of variant families remains *** this paper,we propose a GAN-EfficientNetV2-based method for tracing families of malicious code *** method leverages the similarity in layouts and textures between images of malicious code variants from the same source and their original family of malicious code *** method includes a lightweight classifier and a *** classifier utilizes the enhanced EfficientNetV2 to categorize malicious code images and can be easily deployed on mobile,embedded,and other *** simulator utilizes an enhanced generative adversarial network to simulate different variants of malicious code and generates datasets to validate the model’s *** process helps identify model vulnerabilities and security risks,facilitating model enhancement and *** classifier achieves 98.61%and 97.59%accuracy on the MMCC dataset and Malevis dataset,*** simulator’s generated image of malicious code variants has an FID value of 155.44 and an IS value of 1.72±*** classifier’s accuracy for tracing the family of malicious code variants is as high as 90.29%,surpassing that of mainstream neural network *** meets the current demand for high generalization and anti-obfuscation abilities in malicious code classification models due to the rapid evolution of malicious code.

关键词： Malicious code variant traceability feature reuse lightweight neural networks code visualization attention mechanism

Modulation of starch synthesis in Arabidopsis via phytochrome B-mediated light signal transduction

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Journal of Integrative Plant Biology 2024年第5期66卷 973-985页

作者： qingbiao Shi Ying Xia Na xue Qibin Wang qing Tao Mingjing Li Di Xu Xiaofei Wang Fanying kong Haisen Zhang Gang Li National Key Laboratory of Wheat Improvement College of Life SciencesShandong Agricultural UniversityTai'an 271018China National Key Laboratory of Wheat Improvement College of AgronomyShandong Agricultural UniversityTai'an 271018China

Starch is a major storage carbohydrate in plants and is critical in crop yield and *** synthesis is intricately regulated by internal metabolic processes and external environmental cues;however,the precise molecular mechanisms governing this process remain largely *** this study,we revealed that high red to far-red(high R:FR)light significantly induces the synthesis of leaf starch and the expression of synthesis-related genes,whereas low R:FR light suppress these *** phytochrome B(phyB),the primary R and FR photoreceptor,was identified as a critical positive regulator in this *** of phyB,basic leucine zipper transcription factor ELONGATED HYPOCOTYL5(HY5)was found to enhance starch synthesis,whereas the basic helix-loop-helix transcription factors PHYTOCHROME INTERACTING FACTORs(PIF3,PIF4,and PIF5)inhibit starch synthesis in Arabidopsis ***,HY5 and PIFs directly compete for binding to a shared G-box cis-element in the promoter region of genes encoding starch synthases GBSS,SS3,and SS4,which leads to antagonistic regulation of their expression and,consequently,starch *** findings highlight the vital role of phyB in enhancing starch synthesis by stabilizing HY5 and facilitating PIFs degradation under high R:FR light ***,under low R:FR light,PIFs predominantly inhibit starch *** study provides insight into the physiological and molecular functions of phyB and its downstream transcription factors HY5 and PIFs in starch synthesis regulation,shedding light on the regulatory mechanism by which plants synchronize dynamic light signals with metabolic cues to module starch synthesis.

关键词： Arabidopsis thaliana HY5 light signal phyB PIFs starch synthesis

Loss of GATA6-mediated up-regulation of UTX promotes pancreatic tumorigenesis and progression

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Genes & Diseases 2024年第2期11卷 921-934页

作者： Hui-qing Zhang Fanyang kong Xiangyu kong Tingting Jiang Muyuan Ma Shaojiang Zheng Junli Guo Keping Xie The Third Department of Medical Oncology Jiangxi Cancer HospitalNanchangJiangxi 330006China Departments of Gastroenterology Changhai HospitalSecond Military Medical UniversityShanghai 200433China Center for Pancreatic Cancer Research The South China University of Technology School of MedicineGuangzhouGuangdong 510006China Hainan Clinical Medical Research Center of the First Affiliated Hospital Hainan Women and Children's Medical CenterHainan Medical UniversityHaikouHainan 570102China Key Laboratory of Tropical Cardiovascular Diseases Research of Hainan Province Key Laboratory of Emergency and Trauma of Ministry of EducationHainan Medical UniversityHaikouHainan 571199China

Ubiquitously transcribed tetratricopeptide repeat on chromosome X(UTX),also known as lysine(K)-specific demethylase 6A(KDM6A),functions as a tumor suppressor gene or oncogene depending on the tumor type and ***,its tumor-suppressive mechanisms remain largely ***,we investigated the clinical significance and biological effects of UTX expression in pancreatic ductal adenocarcinoma(PDA)and determined the potential mechanisms of its *** expression and its association with clinicopathologic characteristics of PDA patients were analyzed using *** mRNA and protein expression and their regulation in PDA cell lines were measured using quantitative polymerase chain reaction and Western blot *** biological functions of UTX in PDA cell growth,migration,and invasion were determined using gain-and loss-of-function assays with both in vitro and in vivo animal *** expression was reduced in human PDA cell lines and *** UTX expression was associated with poor differentiation and prognosis in *** UTX expression inhibited PDA proliferation,migration,and invasion in vitro and PDA growth and metastasis in vivo,whereas knockdown of UTX expression did the ***,UTX expression was trans-activated by GATA6 ***6-mediated PDA progression could be blocked,at least partially,by silencing UTX *** conclusion,loss of GATA6-mediated UTX expression was evident in human PDA and restored UTX expression suppressed PDA growth and ***,UTX is a tumor suppressor in PDA and may serve as a prognostic biomarker and therapeutic target.

关键词： Growth Invasion Metastasis Pancreatic cancer UTX

ATM Activation is Key in Vasculogenic Mimicry Formation by Glioma Stem-like Cells

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Biomedical and Environmental Sciences 2024年第8期37卷 834-849页

作者： Jing Xie Jiaxin Tang Yuan Li xue kong Wei Wang Haibo Wu Department of Pathology the First Affiliated Hospital of USTCDivision of Life Sciences and MedicineUniversity of Science and Technology of ChinaHefei 230036AnhuiChina Intelligent Pathology Institute Division of Life Sciences and MedicineUniversity of Science and Technology of ChinaHefei 230036AnhuiChina

Objective Vasculogenic mimicry(VM)is a novel vasculogenic process integral to glioma stem cells(GSCs)in glioblastoma(GBM).However,the relationship between VM and ataxia-telangiectasia mutated(ATM)serine/threonine kinase activation,which confers chemoradiotherapy resistance,remains *** We investigated VM formation and phosphorylated ATM(pATM)levels by CD31/GFAPperiodic acid-Schiff dual staining and immunohistochemical staining in 145 GBM *** stem-like cells(GSLCs)derived from the formatted spheres of U87 and U251 cell lines and their pATM level and VM formation ability were examined using western blot and three-dimensional *** the examination of the function of pATM in VM formation by GSLCs,ATM knockdown by shRNAs and deactivated via ATM phosphorylation inhibitor KU55933 were *** VM and high pATM expression occurred in 38.5% and 41.8% of tumors,respectively,and were significantly associated with reduced progression-free and overall *** with VM-positive GBMs exhibited higher pATM levels(r_(s)=0.425,P=0.01).The multivariate analysis established VM as an independent negative prognostic factor(P=0.002).Furthermore,GSLCs expressed high levels of pATM and formed vascular-like networks in *** inactivation or knockdown hindered VM-like network formation concomitant with the downregulation of pVEGFR-2,VE-cadherin,and laminin *** VM may predict a poor GBM prognosis and is associated with pATM *** propose that pATM promotes VM through extracellular matrix modulation and VE-Cadherin/pVEGFR-2 activation,thereby highlighting ATM activation as a potential target for enhancing anti-angiogenesis therapies for GBM.

关键词： Glioblastoma Vasculogenic mimicry Ataxia-telangiectasia mutated(ATM) Glioma stem-like cell

Influence of pressure disturbance wave on dynamic response characteristics of liquid film seal for multiphase pump

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Petroleum Science 2024年第3期21卷 2048-2065页

作者： qing-Ping Li Jin-Ya Zhang Jia-Xiang Zhang Yong-xue Zhang CNOOC Research Institute Company Limited Beijing100028China State Key Laboratory of Natural Gas Hydrate Beijing100028China College of Mechanical and Transportation Engineering China University of PetroleumBeijing2249China

Slug flow or high GVF(Gas Volume Fraction)conditions can cause pressure disturbance waves and alternating loads at the boundary of mechanical seals for multiphase pumps,endangering the safety of multiphase pump *** mechanical seal model is simplified by using periodic boundary conditions and numerical calculations are carried out based on the Zwart-Gerber-Belamri cavitation ***(User Define Function)programs such as structural dynamics equations,alternating load equations,and pressure disturbance equations are embedded in numerical calculations,and the dynamic response characteristics of mechanical seal are studied using layered dynamic mesh *** results show that when the pressure disturbance occurs at the inlet,as the amplitude and period of the disturbance increase,the film thickness gradually *** the fundamental reason for the hysteresis of the film thickness change is that the pressure in the high-pressure area cannot be restored in a timely *** maximum value of leakage and the minimum value of axial velocity are independent of the disturbance period and determined by the disturbance *** mutual interference between enhanced waves does not have a significant impact on the film thickness,while the front wave in the attenuated wave has a promoting effect on the subsequent film thickness changes,and the fluctuation of the liquid film cavitation rate and axial velocity under the attenuated wave condition deviates from the initial *** with pressure disturbance conditions,alternating load conditions have a more significant impact on film thickness and *** actual operation,it is necessary to avoid alternating load conditions in multiphase pump mechanical seals.

关键词： Multiphase pump Liquid film seal Pressure disturbance wave Dynamic response characteristics