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Palladium-catalyzed vinylation of indoles with vinyl ethers via deoxygenative coupling

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Science China Chemistry 2024年第11期67卷 3785-3790页

作者： Bowen Wang Jianxiao Li Wanqing Wu Liangbin Huang Huanfeng Jiang key laboratory of Functional Molecular Engineering of guangdong province School of Chemistry and Chemical EngineeringSouth China University of Technology

Indole is a promising heteroarene in many natural products and pharmaceuticals; therefore, various synthetic methods for indole functionalizations have arisen in recent years. Herein, we report a Pd-catalyzed deoxygenative coupling for the N-vinylation of indoles by employing vinyl ethers. The vinylated indoles could be readily prepared in good to excellent yields with N1-regioselectivity regardless of the electronic characteristics and substitution patterns of indole substrates. Some indole-based pharmaceutical molecules, such as gramine, evodiamine, rutaecarpine, and melatonine, are also successfully vinylated. Moreover, carbazoles and indazoles are shown to participate. Additionally, vinylated indole can readily transform into structurally interesting indole derivatives.

关键词： indole vinylation regioselectivity N-vinyl indole palladium catalyst

Palladium-Catalyzed anti-Markovnikov Halosulfonamidation of Unactivated Alkene

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Chinese Journal of Chemistry 2024年第5期42卷 464-470页

作者： Bowen Wang Jianxiao Li Wanqing Wu Huanfeng Jiang State key laboratory of Pulp and Paper Engineering Key Laboratory of Functional Molecular Engineering of Guangdong ProvinceSchool of Chemistry and Chemical EngineeringSouth China University of TechnologyGuangzhouGuangdong510641 China

Palladium-catalyzed regioselective amination of unactivated alkene remains a challenge and is of great ***,a three-component coupling of unactivated alkene,sulfonamide,and N-halo compounds accessing vicinal haloamine has been *** aminohalogenation represents a modular and regioselective *** electrophilic halogenating agent enables regioselective anti-Markovnikov aminopalladation and facilitates subsequent halogenation *** this protocol is characterized by gram-scale syntheses and late-stage *** note,the recovered byproduct phthalimide allows for reusing by conversion to the starting material.

关键词： Unactivated alkene anti-Markovnikov aminopalladation Vicinal haloamine Palladium catalysis Halosulfonamidation Selectivity N-Halo compounds

Ultrafast pulse-dilation framing camera and its application for time-resolved X-ray diagnostic

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Nuclear Science and Techniques 2024年第7期35卷 101-114页

作者： Hou-Zhi Cai Qiu-Yan Luo Kai-Xuan Lin Xuan Deng Jun-Kai Liu Kai-Zhi Yang Dong Wang Jia-Jie Chen Jia-Heng Wang Jing-Hua Long Li-Hong Niu Yun-Fei Lei Jin-Yuan Liu key laboratory of Optoelectronic Devices and Systems of Ministry of Education and guangdong province Shenzhen Key Laboratory of Photonics and BiophotonicsCollege of Physics and Optoelectronic EngineeringShenzhen UniversityShenzhen518060China

An ultrafast framing camera with a pulse-dilation device,a microchannel plate(MCP)imager,and an electronic imaging system were *** camera achieved a temporal resolution of 10 ps by using a pulse-dilation device and gated MCP imager,and a spatial resolution of 100μm by using an electronic imaging system comprising combined magnetic *** spatial resolution characteristics of the camera were studied both theoretically and *** results showed that the camera with combined magnetic lenses reduced the field curvature and acquired a larger working area.A working area with a diameter of 53 mm was created by applying four magnetic lenses to the ***,the camera was used to detect the X-rays produced by the laser-targeting *** diagnostic results indicated that the width of the X-ray pulse was approximately 18 ps.

关键词： Inertial confinement fusion Plasma diagnostics Framing camera Combined lenses Pulse-dilation

Multimodal Nature of the Single-cell Primate Brain Atlas:Morphology,Transcriptome,Electrophysiology,and Connectivity

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Neuroscience Bulletin 2024年第4期40卷 517-532页

作者： Yuhui Shen Mingting Shao Zhao-Zhe Hao Mengyao Huang Nana Xu Sheng Liu State key laboratory of Ophthalmology Zhongshan Ophthalmic CenterSun Yat-sen UniversityGuangdong Provincial Key Laboratory of Ophthalmology and Visual ScienceGuangzhou510060China guangdong province key laboratory of Brain Function and Disease Guangzhou510080China

Primates exhibit complex brain structures that augment cognitive *** neocortex fulfills high-cognitive functions through billions of connected *** neurons have distinct transcriptomic,morphological,and electrophysiological properties,and their connectivity principles *** features endow the primate brain atlas with a multimodal *** recent integration of next-generation sequencing with modified patch-clamp techniques is revolutionizing the way to census the primate neocortex,enabling a multimodal neuronal atlas to be established in great detail:(1)single-cell/single-nucleus RNA-seq technology establishes high-throughput transcriptomic references,covering all major transcriptomic cell types;(2)patch-seq links the morphological and electrophysiological features to the transcriptomic reference;(3)multicell patch-clamp delineates the principles of local ***,we review the applications of these technologies in the primate neocortex and discuss the current advances and tentative gaps for a comprehensive understanding of the primate neocortex.

关键词： Neuron Brain atlas Patch-seq Connectivity Primate

Synergistic induction of mitotic pyroptosis and tumor remission by inhibiting proteasome and WEE family kinases

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Signal Transduction and Targeted Therapy 2024年第8期9卷 3467-3482页

作者： Zhan-Li Chen Chen Xie Wei Zeng Rui-Qi Huang Jin-E Yang Jin-Yu Liu Ya-Jing Chen Shi-Mei Zhuang MOE key laboratory of Gene Function and Regulation Guangdong Province Key Laboratory of Pharmaceutical Functional GenesSchool of Life SciencesState Key Laboratory of Oncology in Southern ChinaSun Yat-sen UniversityGuangzhouPR China key laboratory of Liver Disease of guangdong province The Third Affiliated HospitalSun Yat-sen UniversityGuangzhou 510630PR China

Mitotic catastrophe(MC),which occurs under dysregulated mitosis,represents a fascinating tactic to specifically eradicate tumor *** pyroptosis can be a death form of MC remains ***-mediated protein degradation is crucial for ***(BTZ),which inhibits the 20S catalytic particle of proteasome,is approved to treat multiple myeloma and mantle cell lymphoma,but not solid tumors due to primary *** date,whether and how proteasome inhibitor affected the fates of cells in M-phase remains ***,we show that BTZ treatment,or silencing of PSMC5,a subunit of 19S regulatory particle of proteasome,causes G2-and M-phase arrest,multi-polar spindle formation,and consequent caspase-3/GSDME-mediated pyroptosis in M-phase(designated as mitotic pyroptosis).Further investigations reveal that inhibitor of WEE1/PKMYT1(PD0166285),but not inhibitor of ATR,CHK1 or CHK2,abrogates the BTZ-induced G2-phase arrest,thus exacerbates the BTZ-induced mitotic arrest and *** BTZ and PD0166285 treatment(named BP-Combo)selectively kills various types of solid tumor cells,and significantly lessens the IC50 of both BTZ and PD0166285 compared to BTZ or PD0166285 *** using various mouse models show that BP-Combo has much stronger inhibition on tumor growth and metastasis than BTZ or PD0166285 monotreatment,and no obvious toxicity is observed in BP-Combo-treated *** findings disclose the effect of proteasome inhibitors in inducing pyroptosis in M-phase,characterize pyroptosis as a new death form of mitotic catastrophe,and identify dual inhibition of proteasome and WEE family kinases as a promising anti-cancer strategy to selectively kill solid tumor cells.

关键词： proteasome inhibiting catastrophe

Improved observation of colonized roots reveals the regulation of arbuscule development and senescence by drought stress in the arbuscular mycorrhizae of citrus

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Horticultural Plant Journal 2024年第2期10卷 425-436页

作者： Xilong Yin Wei Zhang Zengwei Feng Guangda Feng Honghui Zhu Qing Yao College of Horticulture South China Agricultural UniversityKey Laboratory of Biology and Genetic Improvement of Horticultural Crops(South China)Ministry of Agriculture and Rural AffairsGuangdong Province Key Laboratory of Microbial Signals and Disease ControlGuangzhouGuangdong 510642China key laboratory of Agricultural Microbiomics and Precision Application Ministry of Agriculture and Rural AffairsGuangdong Provincial Key Laboratory of Microbial Culture Collection and ApplicationKey Laboratory of Agricultural MicrobiomicsState Key Laboratory of Applied Microbiology Southern ChinaGuangdong Microbial Culture Collection Center(GDMCC)Institute of MicrobiologyGuangdong Academy of SciencesGuangzhouGuangdong 510070China

Citrus is the typical mycorrhizal fruit tree species establishing symbiosis with arbuscular mycorrhizal (AM) fungi. However, arbuscule development and senescence in colonized citrus roots, especially in response to drought stress, remain unclear, which is mainly due to the difficulty in clearing and staining lignified roots with the conventional method. Here, we improved the observation of colonized roots of citrus plants with the sectioning method, which enabled the clear observation of AM fungal structures. Furthermore, we investigated the effects of one week of drought stress on arbuscule development and senescence with the sectioning method. Microscopy observations indicated that drought stress significantly decreased mycorrhizal colonization (F%and M%) although it did not affect plant growth performance. Fluorescence probes (WGA 488 and/or Nile red) revealed that drought stress inhibited arbuscule development by increasing the percentage of arbuscules at the early stage and decreasing the percentages of arbuscules at the midterm and mature stages. Meanwhile, drought stress accelerated arbuscule senescence, which was characterized by the increased accumulation of neutral lipids. Overall, the sectioning method developed in this study enables the in-depth investigation of arbuscule status, and drought stress can inhibit arbuscule development but accelerate arbuscule senescence in the colonized roots of citrus plants. This study paves the way to elaborately dissecting the arbuscule dynamics in the roots of fruit tree species in response to diverse abiotic stresses.

关键词： Arbuscular mycorrhizae Citrus Drought stress Arbuscule development Arbuscule senescence Fruit tree species

Double contrast-enhanced ultrasonography improves diagnostic accuracy of T staging compared with multi-detector computed tomography in gastric cancer patients

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World Journal of Gastroenterology 2024年第23期30卷 3005-3015页

作者： Yan-Fen Xu Hui-Yun Ma Gui-Ling Huang Yu-Ting Zhang Xue-Yan Wang Ming-Jie Wei Xiao-Qing Pei Department of Ultrasound State Key Laboratory of Oncology in South ChinaGuangdong Key Laboratory of Nasopharyngeal Carcinoma Diagnosis and TherapyGuangdong Provincial Clinical Research Center for CancerSun Yat-sen University Cancer CenterGuangzhou 510060Guangdong ProvinceChina Department of Radiology State Key Laboratory of Oncology in South ChinaGuangdong Key Laboratory of Nasopharyngeal Carcinoma Diagnosis and TherapyGuangdong Provincial Clinical Research Center for CancerSun Yat-sen University Cancer CenterGuangzhou 510060Guangdong ProvinceChina Department of Medical Ultrasound State Key Laboratory of Oncology in South ChinaGuangdong Key Laboratory of Nasopharyngeal Carcinoma Diagnosis and TherapyGuangdong Provincial Clinical Research Center for CancerSun Yat-sen University Cancer CenterGuangzhou 510060Guangdong ProvinceChina

BACKGROUND Gastric cancer(GC)is the most common malignant tumor and ranks third for cancer-related deaths among the *** disease poses a serious public health problem in China,ranking fifth for incidence and third for *** of the invasive depth of the tumor is vital to treatment *** To evaluate the diagnostic performance of double contrast-enhanced ultrasonography(DCEUS)for preoperative T staging in patients with GC by comparing with multi-detector computed tomography(MDCT).METHODS This single prospective study enrolled patients with GC confirmed by preoperative gastroscopy from July 2021 to March *** underwent DCEUS,including ultrasonography(US)and intravenous contrast-enhanced ultrasonography(CEUS),and MDCT examinations for the assessment of preoperative T *** of GC were identified on DCEUS and criteria developed to evaluate T staging according to the 8th edition of AJCC cancer staging *** diagnostic performance of DCEUS was evaluated by comparing it with that of MDCT and surgical-pathological findings were considered as the gold *** A total of 229 patients with GC(80 T1,33 T2,59 T3 and 57 T4)were *** accuracies were 86.9%for DCEUS and 61.1%for MDCT(P<0.001).DCEUS was superior to MDCT for T1(92.5%vs 70.0%,P<0.001),T2(72.7%vs 51.5%,P=0.041),T3(86.4%vs 45.8%,P<0.001)and T4(87.7%vs 70.2%,P=0.022)staging of *** DCEUS improved the diagnostic accuracy of preoperative T staging in patients with GC compared with MDCT,and constitutes a promising imaging modality for preoperative evaluation of GC to aid individualized treatment decision-making.

关键词： Double contrast-enhanced ultrasonography Multi-detector computed tomography Gastric cancer T staging

Acute primary angle closure during the Omicron outbreak

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International Journal of Ophthalmology(English edition) 2024年第7期17卷 1337-1343页

作者： Dong Fang Wang-Ting Li Jia Liang Lu Chen Ning-Xin Dou Hui-Yan Zheng Can-Feng Huang Ting Xie Yi-Jing Zhuang Peng-Feng Li Xing-Xing Mao Shao-Chong Zhang Shenzhen Eye Hospital Jinan UniversityShenzhen Key Laboratory of OphthalmologyShenzhen 518040Guangdong ProvinceChina

AIM:To investigate Omicron’s impact on clinical presentation of acute primary angle closure(APAC)in ***:A consecutive case series with historical controls was conducted at Shenzhen Eye Hospital,the largest specialized hospital in Shenzhen,*** records from a two-month period during the Omicron pandemic(December 1,2022,to January 31,2023)were compared with records from two control groups(12/2018–1/2019 and 12/2021–1/2022)before *** with APAC were included,and the prevalence of APAC and demographic characteristics in Omicron-infected and noninfected patients were ***:Seventy-one(23.43%)out of 303 patients were diagnosed with APAC in the pandemic cohort,which was 2.98 and 2.61 times higher than that in control cohorts(7.87%in 2019,8.96%in 2022,P<0.001).The pandemic cohort has significantly higher Omicron-infected rate(78.87%vs 0 vs 0;P<0.001),lower proportion of glaucoma history(16.90%vs 42.86%vs 41.67%,P=0.005),higher surgical rate(95.77%vs 83.33%vs 78.57%,P=0.024),higher total medical costs and larger pupil diameter(5.63±0.15 vs 4.68±0.15 vs 4.69±0.22 mm,P<0.01).In 83%Omicron-infected patients,ocular symptoms appeared within 3d after systemic symptoms *** multivariate analysis,Omicron infection(P<0.001)was the only independent predictor of pupil ***:In the Omicron epidemic in China,there is an increase of prevalence and severity of APAC,particularly focusing on the first 3d following infection.

关键词： Omicron acute primary angle closure ocular symptoms

Multi-omics Approach Reveals Influenza-A Virus Target Genes Associated Genomic,Clinical and Immunological Characteristics in Cancers

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Biomedical and Environmental Sciences 2024年第7期37卷 698-715页

作者： Jiaojiao Wang Yong Liao Pinglian Yang Weile Ye Yong Liu Chunxia Xiao Weixiong Liao Chunbo Chen Zhiping Liu Zunnan Huang Center of Scientific Research Department of CardiologyMaoming People’s HospitalMaoming 525000GuangdongChina Department of Pharmacy Maoming People’s HospitalMaoming 525000GuangdongChina State key laboratory of Bioactive Molecules and Druggability Assessment Jinan UniversityGuangzhou 510632GuangdongChina guangdong province key laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research College of PharmacyJinan UniversityGuangzhou 510632GuangdongChina key laboratory of Big Data Mining and Precision Drug Design of guangdong Medical University Key Laboratory of Computer-Aided Drug Design of Dongguan CityKey Laboratory for Research and Development of Natural Drugs of Guangdong ProvinceSchool of PharmacyGuangdong Medical UniversityDongguan 523808GuangdongChina Department of Critical Care Medicine Maoming People’s HospitalMaoming 525000GuangdongChina

Objective To examine the precise function of influenza A virus target genes(IATGs)in *** Using multi-omics data from the TCGA and TCPA datasets,33 tumor types were evaluated for *** expression in cancer cells was analyzed using transcriptome *** number variation(CNV)was assessed using GISTICS ***’s analysis was used to correlate mRNA expression with methylation *** was used for the enrichment ***’s correlation analysis was used to examine the association between IATG mRNA expression and *** ImmuCellAI algorithm was used to calculate the infiltration scores of 24 immune cell *** In 13 solid tumors,IATG mRNA levels were atypically *** for UCS,UVM,KICH,PCPG,THCA,CHOL,LAMI,and MESO,most cancers contained somatic IATG *** main types of CNVs in IATGs are heterozygous amplifications and *** most tumors,IATG mRNA expression is adversely associated with ***-PCR demonstrated that EGFR,ANXA5,CACNA1C,CD209,UVRAG were upregulated and CLEC4M was downregulated in KIRC cell lines,consistent with the TCGA and GTEx *** Genomic changes and clinical characteristics of IATGs were identified,which may offer fresh perspectives linking the influenza A virus to cancer.

关键词： Genomic changes Immune microenvironment Prognosis Drug resistance Experimental validation