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An Update on the Clinical Pipelines of New Antibacterial Drugs Developed in China

Engineering 2024年第7期38卷 52-68页

作者： Xinyi Yang Congran Li Xiukun Wang Zhonghui Zheng Peiyi sun Chunjie Xu Luni Chen Jiandong Jiang Staffan Normark Birgitta Henriques-Normark Xuefu you Beijing Key Laboratory of Antimicrobial Agents/Laboratory of Pharmacology Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Division for Medicinal Microorganism-Related Strains CAMS Collection Center of Pathogenic MicroorganismsChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Shandong Xinhua Pharmaceutical Co. Ltd.Zibo 255005China Department of Microbiology Tumor and Cell BiologyKarolinska InstitutetStockholm SE-17177Sweden State Key Laboratory of Bioactive Substances and Function of Natural Medicines Institute of Materia MedicaChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China Clinical Microbiology Karolinska University HospitalBioclinicumStockholm SE-17176Sweden

Antibacterial resistance is a global health threat that requires further concrete action on the part of all *** this context,one of the biggest concerns is whether enough new antibacterial drugs are being discovered and *** several high-quality reviews on clinical antibacterial drug pipelines from a global perspective were published recently,none provides comprehensive information on original antibacterial drugs at clinical stages in *** this review,we summarize the latest progress of novel antibacterial drugs approved for marketing and under clinical evaluation in China since *** was obtained by consulting official websites,searching commercial databases,retrieving literature,asking personnel from institutions or companies,and other means,and a considerable part of the data covered here has not been included in other *** of June 30,2023,a total of 20 antibacterial projects from 17 Chinese pharmaceutical companies or developers were identified and *** them,two new antibacterial drugs that belong to traditional antibiotic classes were approved by the National Medical Products Administration(NMPA)in China in 2019 and 2021,respectively,and 18 antibacterial agents are in clinical development,with one under regulatory evaluation,five in phase-3,six in phase-2,and six in *** of the clinical candidates are new analogs or monocomponents of traditional antibacterial pharmacophore types,including two dual-acting hybrid antibiotics and a recombinant antibacterial ***,despite there being 17 antibacterial clinical candidates,our analysis indicates that there are still relatively few clinically differentiated antibacterial agents in stages of clinical development in ***,Chinese pharmaceutical companies and institutions will develop more innovative and clinically differentiated candidates with good market potential in the future research and development(R&D)of original antibacterial drugs.

关键词： Antimicrobial resistance New antibiotics Clinical pipelines WHO priority pathogens National Mega-Project for Innovative Drugs

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Super-resolution Imaging of Telescopic Systems based on Optical-neural Network Joint Optimization

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Research in Astronomy and Astrophysics 2024年第9期24卷 167-177页

作者： you-Hong sun Tao Zhang Hao-Dong Shi Qiang Fu Jia-Nan Liu Kai-Kai Wang Chao Wang Research Institute of Chongqing Changchun University of Science and TechnologyChangchun 130022China National and Local Joint Engineering Research Center for Space Photoelectric Technology Changchun University of Science and TechnologyChangchun 130022China The Institute of Remote Sensing Satellites China Academy of Space Technology(CAST)Beijing 100094China

Optical telescopes are an important tool for acquiring optical information about distant objects,and resolution is an important indicator that measures the ability to observe object ***,due to the effects of system aberration,atmospheric seeing,and other factors,the observed image of ground-based telescopes is often degraded,resulting in reduced *** paper proposes an optical-neural network joint optimization method to improve the resolution of the observed image by co-optimizing the point-spread function(PSF)of the telescopic system and the image super-resolution(SR)*** improve the speed of image reconstruction,we designed a generative adversarial net(LCR-GAN)with light parameters,which is much faster than the latest unsupervised *** reconstruct the PSF trained by the network in the optical path,a phase mask is *** improves the image reconstruction effect of LCR-GAN by reconstructing the PSF that best matches the *** results of simulation and verification experiments show that compared with the pure deep learning method,the SR image reconstructed by this method is rich in detail and it is easier to distinguish stars or stripes.

关键词： Techniques:image processing Telescopes Stars:imaging

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Ingredients-based Methodology and Fuzzy Logic Combined Short-Duration Heavy Rainfall Short-Range Forecasting:An Improved Scheme

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Journal of Tropical Meteorology 2024年第3期30卷 241-256页

作者： TIAN Fu-you XIA Kun sun Jian-hua ZHENG Yong-guang HUA Shan National Meteorological Center Beijing100081 China State Key Laboratory of Numerical Modeling for Atmospheric Sciences and Geophysical Fluid Dynamics(LASG) Institute of Atmospheric PhysicsChinese Academy of Sciences(IAP/CAS)Beijing 100029 China Key Laboratory of Cloud-Precipitation Physics and Severe Storms(LACS) Institute of Atmospheric PhysicsChinese Academy of Sciences(IAP/CAS)Beijing 100029 China

Short-duration heavy rainfall(SHR),as delineated by the National Meteorological Center of the China Me-teorological Administration,is characterized by hourly rainfall amounts no less than 20.0 *** is one of the most common convective weather phenomena that can cause severe ***-range forecasting of SHR is an important part of operational severe weather *** the present study,an improved objective SHR forecasting scheme was developed by adopting the ingredients-based methodology and using the fuzzy logic *** 1.0°×1.0°National Centers for Environmental Prediction(NCEP)final analysis data and the ordinary rainfall(0.1-19.9 mm h-1)and SHR observational data from 411 stations were used in the improved *** best lifted index,the total precipitable water,the 925 hPa specific humidity(Q 925),and the 925 hPa divergence(DIV 925)were selected as predictors based on objective *** distributed membership functions of predictors were obtained based on relative frequency *** weights of predictors were also objectively *** with a typhoon SHR case and a spring SHR case show that the main possible areas could be captured by the improved *** of SHR forecasts within 96 hours with NCEP global forecasts 1.0°×1.0°data initiated at 08:00 Beijing Time during the warm seasons in 2015 show the results were improved from both deterministic and probabilistic *** study provides an objectively feasible choice for short-range guidance forecasts of *** scheme can be applied to other convective phenomena.

关键词： ingredients-based methodology fuzzy logic approach probability of short-duration heavy rainfall(SHR) improved forecasting scheme objectively obtained membership functions

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Chemical and mechanical properties of stainless, environment-friendly, and nonflammable Mg alloys (SEN alloys): A review

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Journal of Magnesium and Alloys 2024年第3期12卷 841-872页

作者： Jong Un Lee Hyun Ji Kim Sang-Cheol Jin Ye Jin Kim young Min Kim Bong sun you Jun Ho Bae sung Hyuk Park Advanced Metals Division Korea Institute of Materials ScienceChangwon 51508Republic of Korea Department of Materials Science and Metallurgical Engineering Kyungpook National UniversityDaegu 41566Republic of Korea Missile Research Institute Agency for Defense DevelopmentDaejeon 34060Republic of Korea

This review article provides overall understanding of stainless,environment-friendly,and nonflammable Mg alloys(SEN alloys)recently developed at the Korea Institute of Materials *** alloys are produced by adding small amounts of Ca and Y(each<1 wt%)into commercial Mg–Al based alloys,resulting in exceptional ignition and corrosion resistances and impressive mechanical *** main advantages of SEN alloys are as follows.(1)A dense multi-oxide layer of SEN alloys comprising MgO,CaO,and Y_(2)O_(3) impedes the outward dispersion of Mg vapor and the inward penetration of O_(2) during oxidation,thereby enhancing the oxidation and ignition resistances.(2)The presence of Ca-and Y-based second-phase particles in SEN alloys can enhance their corrosion resistance because Ca-containing particles prevent the spread of corrosion,and the replacement of Al-containing particles with less noble ones containing Y(e.g.,Al–Mn–Y or Al–Y particles)retards corrosion.(3)The addition of minor amounts of Ca and Y renders excellent mechanical properties due to improved strengthening *** enhanced properties are attributed to more pronounced dynamic recrystallization and grain refining behaviors caused by the second-phase particles during extrusion.(4)Despite the presence of various types of second-phase particles,the fatigue properties of SEN9 alloys are similar to those of commercial AZ91 alloys.(5)Simultaneous introduction of Ca and Y suppresses the formation of Mg17Al12 discontinuous precipitates during aging,leading to the enhanced elongation of aged SEN alloys.(6)Adding mischmetal into the SEN9 alloy leads to a six-fold enhancement in ***,the studies conducted on SEN alloys demonstrate their excellent ignition and corrosion resistances and mechanical properties,which broaden the industrial applications of Mg alloys by addressing their inherent weaknesses.

关键词： SEN magnesium alloy Corrosion resistance Ignition resistance Mechanical properties Extrudability.

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How to manage the malposition of deep vein catheterization into the artery?

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Journal of Geriatric Cardiology 2024年第6期21卷 682-685页

作者： Jun-Na sun Hai DONG Peng CHEN Zi-Qi LI Li-you SUI Bin QI Quan-Min JING Department of Cardiovascular Diseases the First Affiliated Hospital of Henan University of Chinese MedicineZhengzhouChina Department of Cardiology General Hospital of Northern Theater CommandShenyangChina

Central venous catheterization establishes temporary,efficient,and rapid use of deep venous access in patients,which provides high flow rate fluid perfusion,enables measurement of central venous pressure,and acts as an important reference for clinical ***,various complications such as pneumothorax,hemothorax,hematoma,and puncture failure can easily occur during the puncture and catheterization process.

关键词： process enable catheter

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Resilience and response:Unveiling the impacts of extreme droughts on forests through integrated dendrochronological and remote sensing analyses

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Forest Ecosystems 2024年第4期11卷 491-501页

作者： Han Shi Xi Peng Yong-Jiao Zhou Ai-Ying Wang Xue-Kai sun Na Li Quan-Sheng Bao Gude Buri Guang-you Hao CAS Key Laboratory of Forest Ecology and Silviculture Institute of Applied EcologyChinese Academy of SciencesShenyang110016China Daqinggou Ecological Research Station Institute of Applied EcologyChinese Academy of SciencesShenyang110016China University of Chinese Academy of Sciences Beijing100049China School of Life Science and Engineering Shenyang UniversityShenyang110044China Wudantala Forestry Forestry and Grassland Administration of Horqin Northeast CountyTongliao028100China

Extreme droughts are anticipated to have detrimental impacts on forest ecosystems,especially in water-limited regions,due to the influence of climate ***,considerable uncertainty remains regarding the patterns in species-specific responses to extreme ***,we conducted a study integrating dendrochronology and remote sensing methods to investigate the mosaic-distributed maple-oak(native)natural forests and poplar plantations(introduced)in the Horqin Sandy Land,Northeast *** assessed the impacts of extreme droughts on tree performances by measuring interannual variations in radial growth and vegetation *** results showed that precipitation and self-calibrated palmer drought severity index(scPDSI)are the major factors influencing tree-ring width index(RWI)and normalized difference vegetation index(NDVI).The severe droughts between 2000 and 2004 resulted in reduced RWI in the three studied tree species as well as led to NDVI reductions in both the maple-oak natural forests and the poplar *** RWI reached the nadir during the2000-2004 severe droughts and remained at low levels two years after the severe drought,creating a legacy *** contrast to the lack of significant correlation between RWI and scPDSI,NDVI exhibited a significant positive correlation with scPDSI indicating the greater sensitivity of canopy performance to droughts than radial ***,interspecific differences in RWI and NDVI responses were observed,with the fast-growing poplar species experiencing a more significant RWI decrease and more negative NDVI anomaly during severe droughts than native species,highlighting the species-specific trade-offs between drought resilience and growth *** study emphasizes the importance of combining tree-level radial growth with landscape-scale canopy remote sensing to understand forest resilience and *** study improves our understanding of forest responses to extreme drought and highlights species di

关键词： Introduced tree species Native tree species NDVI Severe drought Tree-ring width

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Sequence-controlled dynamic covalent units enable decoupling of mechanical and self-healing performance of polymers

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Science China Chemistry 2024年

作者： Luzhi Zhang Hongfei Huang Lijie sun Xiaopeng Ma Hui Tan Zhengwei you Respiratory Department Shenzhen Children's Hospital Affiliated to Shantou University Medical College State Key Laboratory for Modification of Chemical Fibers and Polymer Materials College of Materials Science and EngineeringInstitute of Functional MaterialsShanghai Key Laboratory of Lightweight CompositeShanghai Engineering Research Center of Nano-Biomaterials and Regenerative MedicineDonghua University Yangtze Delta Region Institute (Huzhou) University of Electronic Science and Technology of China

Sequence regulation provides an effective approach to controlling the properties of polymer ***,this approach remains an open question in the field of dynamic polymers,which emerge as more and more important new generation ***,we systematically investigate the effect of sequence control of dynamic covalent units in tuning the properties of *** sequence-controlled poly(oxime-urethanes) are *** dynamic oxime-urethane groups are relatively dispersed (SCP-1) or concentrated (SCP-2) distributed in their molecular *** sequence control strategy provides an efficient way to decouple the mechanical and self-healing performance of polymers,which is one of the most pressing challenges in the *** relatively dispersed oxime-urethane groups in SCP-1 not only facilitate the reorganization of the dynamic covalent bonds but also increase the probability of the reformation of hydrogen *** reversible dissociation/reassociation of dynamic bonds is conducive to dissipating energy to enhance mechanical performance and promote self-healing *** a result,SCP-1 exhibits much faster self-healing than SCP-2,and its tensile strength is nearly twice that of *** addition,energy dissipation capacity and degradation behavior also show significant sequence ***,this work reveals a new molecular structure-property relationship and provides a powerful strategy to construct high-performance polymers.

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Automatic detection of breast lesions in automated 3D breast ultrasound with cross-organ transfer learning

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虚拟现实与智能硬件（中英文） 2024年第3期6卷 239-251页

作者： Lingyun BAO Zhengrui HUANG Zehui LIN Yue sun Hui CHEN you LI Zhang LI Xiaochen YUAN Lin XU Tao TAN Affiliated Hangzhou First People's Hospital School of MedicineWestlake UniversityHangzhou 330100China Faculty of Applied Sciences Macao Polytechnic UniversityMacao 999078China Pathology Department Changsha First HospitalChangsha 410073China Radiology Department Changsha First HospitalChangsha 410073China College of Aerospace Science and Engineering National University of Defense TechnologyChangsha 410073China Hunan Provincial Key Laboratory of Image Measurement and Vision Navigation Changsha 410073China School of Information Science and Technology Shanghaitech UniversityShanghai 201210China

Background Deep convolutional neural networks have garnered considerable attention in numerous machine learning applications,particularly in visual recognition tasks such as image and video *** is a growing interest in applying this technology to diverse applications in medical image *** three dimensional Breast Ultrasound is a vital tool for detecting breast cancer,and computer-assisted diagnosis software,developed based on deep learning,can effectively assist radiologists in ***,the network model is prone to overfitting during training,owing to challenges such as insufficient training *** study attempts to solve the problem caused by small datasets and improve model detection *** We propose a breast cancer detection framework based on deep learning(a transfer learning method based on cross-organ cancer detection)and a contrastive learning method based on breast imaging reporting and data systems(BI-RADS).Results When using cross organ transfer learning and BIRADS based contrastive learning,the average sensitivity of the model increased by a maximum of 16.05%.Conclusion Our experiments have demonstrated that the parameters and experiences of cross-organ cancer detection can be mutually referenced,and contrastive learning method based on BI-RADS can improve the detection performance of the model.

关键词： Breast ultrasound Automated 3D breast ultrasound Breast cancers Deep learning Transfer learning Convolutional neural networks Computer-aided diagnosis Cross organ learning

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Divergent responses of runoff to climate change in the upper basins of the Third Pole dominated by westerlies and monsoon

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Science China Earth Sciences 2024年第8期67卷 2592-2614页

作者： Qikai sun Fengge SU He sun State Key Laboratory of Tibetan Plateau Earth System Environment and Resources(TPESER)Institute of Tibetan Plateau ResearchChinese Academy of SciencesBeijing 100101China University of Chinese Academy of Sciences Beijing 100101China

The diverse climates,distribution of snow and glaciers,and geographic locations directly affect the runoff response to climate change in the upper basins of the Third *** present,a comprehensive analysis of runoff variations and their distinct responses to climate change in the westerlies-and monsoon-dominated upper basins is still *** study comprehensively analyzed annual runoff variations in westerlies-dominated basins(the upper basins of the Aksu(UAKS),Syr Darya(USRD),Yarkant(UYK),Hotan(UHT),Amu Darya(UAMD),and Indus(UI))and monsoon-dominated basins(the upper basins of the Yangtze(UYA),Yellow(UYE),Lancang(ULC),Nujiang(UNJ),and Yarlung Zangbo(UYZ))of the Third Pole from 1961 *** multi-source meteorological data and large-scale circulation factors,this study investigated the divergent responses of runoff in the upper basins to climate change,and explored the large-scale circulation mechanisms underlying runoff variations in these upper *** results showed that:(1)The annual runoff in the majority of upper basins(except for the UYE and UYZ)exhibited an increasing trend,and the annual runoff in the UAKS,UYK,and UI showed a significant increasing trend from1961 to *** annual runoff in the upper basins of the Third Pole changed abruptly from decreasing to increasing between the 1980s and 2000s,with the exception of the UYE.(2)The runoff in the monsoon-dominated upper basins has been controlled primarily by changes in precipitation over the past 55 *** contrast,the runoff in the westerlies-dominated upper basins exhibited three distinct long-term responses to climate change:temperature-dominated(UYK and UHT),precipitation-dominated(USRD and UAMD),and the combined influence of precipitation and temperature(UAKS and UI).Since the 1960s,the sensitivity of runoff to warm season temperature changes in the most westerlies-dominated upper basins has decreased,while the response of runoff to precipitation changes has intensified.(3)The stud

关键词： Upper basins of the Third Pole Climate change Westerlies and monsoon Runoff variations Large-scale circulation factors

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Hyperlanins A and B, Two Highly Rearranged Meroterpenoids from Hypericum lancasteri

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Chinese Journal of Chemistry 2024年第18期42卷 2180-2186页

作者： Jin-Qiu you Yun-Qi Jin Meng-Yu Li Bo-Chao Zhang Xin-Yu sun Chun-Yong Ding Jing-Ya Li Ai-Jun Hou Shanghai Frontiers Science Center of Drug Target Identification and Delivery School of Pharmaceutical SciencesShanghai Jiao Tong UniversityShanghai200240China National Key Laboratory of Innovative Immunotherapy Shanghai Jiao Tong UniversityShanghai 200240China Shanghai Jiao Tong University School of Medicine Shanghai 200025China Shanghai Institute of Materia Medica Chinese Academy of SciencesShanghai 201203China

Hyperlanins A(1)and B(2),two highly rearranged polycyclic polyprenylated acylphloroglucinol(PPAP)-related meroterpenoids based on different new carbon skeletons,were isolated from Hypericum *** 1 incorporates an unprecedented 5/6/7/5 ring system featuring a 3,13-dioxatetracyclo[9.***.1.12.5.01.8]pentadecane *** 2 possesses a unique compact 6/6/5/6/6/5/6 ring system with a caged tetracyclo[6.***.1.13.8.05,11]dodecane *** structures were established by spectroscopic data,X-ray diffraction,and computational *** compounds showed anti-inflammatory activity in *** 1 and 2 could decrease the lipopolysaccharide(LPS)-/nigericin-induced IL-1βrelease in THP-1 *** compounds also showed inhibition in hypoxia-inducible factor-1α(HIF-1αa)pathway luciferase reporter assay.

关键词： Natural products Hypericum lancasteri Meroterpenoids Structureelucidation Inflammation

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