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| 1 | Pneumoconiosis: current status and future prospects显示文摘Pneumoconiosis refers to a spectrum of pulmonary diseases caused by inhalation of mineral dust,usually as the result of certain occupations.The main pathological features include chronic pulmonary inflammation and progressive pulmonary fibrosis,which can eventually lead to death caused by respiratory and/or heart failure.Pneumoconiosis is widespread globally,seriously threatening global public health.Its high incidence and mortality lie in improper occupational protection,and in the lack of early diagnostic methods and effective treatments.This article reviews the epidemiology,safeguard procedures,diagnosis,and treatment of pneumoconiosis,and summarizes recent research advances and future research prospects. | Xian-Mei Qi Ya Luo Mei-Yue Song Ying Liu Ting Shu Ying Liu Jun-Ling Pang Jing Wang Chen Wang | 2021 | Chinese Medical Journal2021，，8： | 22 |
| 2 | Celastrol induces ferroptosis in activated HSCs to ameliorate hepatic fibrosis via targeting peroxiredoxins and HO-1显示文摘Ferroptosis is a form of regulated cell death, characterized by excessive membrane lipid peroxidation in an iron-and ROS-dependent manner. Celastrol, a natural bioactive triterpenoid extracted from Tripterygium wilfordii, shows effective anti-fibrotic and anti-inflammatory activities in multiple hepatic diseases. However, the exact molecular mechanisms of action and the direct protein targets of celastrol in the treatment of liver fibrosis remain largely elusive. Here, we discover that celastrol exerts anti-fibrotic effects via promoting the production of reactive oxygen species(ROS) and inducing ferroptosis in activated hepatic stellate cells(HSCs). By using activity-based protein profiling(ABPP) in combination with bio-orthogonal click chemistry reaction and cellular thermal shift assay(CETSA), we show that celastrol directly binds to peroxiredoxins(PRDXs), including PRDX1, PRDX2, PRDX4 and PRDX6,through the active cysteine sites, and inhibits their anti-oxidant activities. Celastrol also targets to heme oxygenase 1(HO-1) and upregulates its expression in activated-HSCs. Knockdown of PRDX1, PRDX2,PRDX4, PRDX6 or HO-1 in HSCs, to varying extent, elevated cellular ROS levels and induced ferroptosis. Taken together, our findings reveal the direct protein targets and molecular mechanisms via which celastrol ameliorates hepatic fibrosis, thus supporting the further development of celastrol as a promising therapeutic agent for liver fibrosis. | Piao Luo Dandan Liu Qian Zhang Fan Yang Yin-Kwan Wong Fei Xia Junzhe Zhang Jiayun Chen Ya Tian Chuanbin Yang Lingyun Dai Han-Ming Shen Jigang Wang | 2022 | Acta Pharmaceutica Sinica B2022，12，5： | 14 |
| 3 | Tetrandrine alleviates silicosis by inhibiting canonical and non-canonical NLRP3 inflammasome activation in lung macrophages显示文摘Silicosis caused by inhalation of silica particles leads to more than ten thousand new occupational exposure-related deaths yearly.Exacerbating this issue,there are currently few drugs reported to effectively treat silicosis.Tetrandrine is the only drug approved for silicosis treatment in China,and despite more than decades of use,its efficacy and mechanisms of action remain largely unknown.Here,in this study,we established silicosis mouse models to investigate the effectiveness of tetrandrine of early and late therapeutic administration.To this end,we used multiple cardiopulmonary function test,as well as markers for inflammation and fibrosis.Moreover,using single cell RNA sequencing and transcriptomics of lung tissue and quantitative microarray analysis of serum from silicosis and control mice,our results provide a novel description of the target pathways for tetrandrine.Specifically,we found that tetrandrine attenuated silicosis by inhibiting both the canonical and non-canonical NLRP3 inflammasome pathways in lung macrophages.Taken together,our work showed that tetrandrine yielded promising results against silicosis-associated inflammation and fibrosis and further lied the groundwork for understanding its molecular targets.Our results also facilitated the wider adoption and development of tetrandirne,potentially accelerating a globally accepted therapeutic strategy for silicosis. | Mei-yue Song Jia-xin Wang You-liang Sun Zhi-fa Han Yi-tian Zhou Ying Liu Tian-hui Fan Zhao-guo Li Xian-mei Qi Ya Luo Pei-ran Yang Bai-cun Li Xin-ri Zhang Jing Wang Chen Wang | 2022 | Acta Pharmacologica Sinica2022，43，5： | 12 |
| 4 | Evaluating the suitability of TRMM satellite rainfall data for hydrological simulation using a distributed hydrological model in the Weihe River catchment in China显示文摘这研究的目的到份量上评估热带降雨测量有雨计量器数据并且进一步的使命(TRMM ) 数据到使用驱使一个分布式的时间变体获得模型(DTVGM ) 在中国在半潮湿的 Weihe 河集水执行水文学模拟的这个 TRMM 数据。在模拟前,比较与一 10 年(20012010 ) 设置的每日的雨计量器数据表明在每日的时间步, TRMM 降雨数据擅长比降雨极端捕获雨出现和吝啬的值。在每月的时间规模上,在 TRMM 和雨计量器降雨数据之间的好线性关系被发现,与决心系数 R < 啜 class= “ a-plus-plus ” > 为个人在 0.78 和 0.89 之间变化的 2 驻扎。每日的水文学过程上的数据的七年( 20012007 )的随后的模拟结果证实 DTVGM 什么时候由雨计量器数据校准了,比什么时候由 TRMM 数据校准更好表现,但是 TRMM 数据驾驶的模拟的性能比在每月的时间规模上由计量器数据开车的好。结果因此建议 TRMM 降雨数据对在学习的每月的流速及流水量模拟更合适区域,和那当为水平衡部件的刻度和结果的效果也被考虑时, TRMM 3B42-V7 产品有潜力表现很好在类似的盆。 | ZHAO Haigen | 2015 | Journal of Geographical Sciences2015，25，2： | 12 |
| 5 | Response of sediment yield to vegetation restoration at a large spatial scale in the Loess Plateau显示文摘The impact of vegetation coverage on erosion and sediment yield in the Loess Plateau has been extensively studied,but the research has been primarily based on observations from slope runoff plots or secondary forest regions;the scaling method remains unresolved when it is applied at a large spatial scale,and it is difficult to apply to regions with severe soil and water loss given the predominance of herbs and shrubs.To date,there is little data on the quantitative impact of changes to vegetation on sediment concentration at a large spatial scale.This paper is based on vegetation information from remote sensing images,measured rainfall and sediment data over nearly 60 years,and results from previous runoff and sediment variation research on the Yellow River.We introduce the concepts of a sediment yield coefficient and the percentage of effective vegetation and erodible area,analyze the impact of different vegetation conditions on the flood sediment concentration and sediment yield,and evaluate the effect of rainfall intensity on sediment yield under different vegetation conditions at the watershed scale.We propose models to evaluate the impact of vegetation on sediment yield in the loess gully hilly region,which are based on remote sensing data and support an application at a large spatial scale.The models can be used to assess sediment reduction that results from the current significant improvement of vegetation in the Loess Plateau. | LIU XiaoYan YANG ShengTian DANG SuZhen LUO Ya LI XiaoYu ZHOU Xu | 2014 | Science China(Technological Sciences)2014，57，8： | 11 |
| 6 | Antidepressant-Like Action of Single Facial Injection of Botulinum Neurotoxin A is Associated with Augmented 5-HT Levels and BDNF/ERK/CREB Pathways in Mouse Brain显示文摘The present study was designed to examine the therapeutic effects of Botulinum neurotoxin A(BoNT/A)on depression-like behaviors in mice and to explore the potential mechanisms.These results revealed that a single facial injection of BoNT/A induced a rapid and prolonged improvement of depression-like behaviors in naive and space-restriction-stressed(SRS)mice,reflected by a decreased duration of immobility in behavioral despair tests.BoNT/A significantly increased the 5-hydroxytryptamine(5-HT)levels in several brain regions,including the hippocampus and hypothalamus,in SRS mice.BoNT/A increased the expression of the N-methyl-Daspartate receptor subunits NR1 and NR2 B in the hippocampus,which were significantly decreased in SRS mice.Furthermore,BoNT/A significantly increased the expression of brain-derived neurotrophic factor(BDNF)in the hippocampus,hypothalamus,prefrontal cortex,and amygdala,which were decreased in SRS mice.Finally,BoNT/A transiently increased the levels of phosphorylated extracellular signal-regulated kinase(p-ERK)and cAMPresponse element binding protein(p-CREB),which were suppressed in the hippocampus of SRS mice.Collectively,these results demonstrated that BoNT/A treatment has antidepressant-like activity in mice,and this is associated with increased 5-HT levels and the activation of BDNF/ERK/CREB pathways in the hippocampus,supporting further investigation of BoNT/A therapy in depression. | Yang Li Jing Liu Xu Liu Cun-Jin Su Qi-Lin Zhang Zhi-Hong Wang Lei-Fang Cao Xue-Yan Guo Ya Huang Weifeng Luo Tong Liu | 2019 | Neuroscience Bulletin2019，35，4： | 10 |
| 7 | A critical review on the application of biochar in environmental pollution remediation:Role of persistent free radicals(PFRs)显示文摘Biochar as an emerging carbonaceous material has exhibited a great potential in environmental application for its perfect adsorption ability.However,there are abundant persistent free radicals(PFRs)in biochar,so the direct and indirect PFRs-mediated removal of organic and inorganic contaminants by biochar was widely reported.In order to comprehend deeply the formation of PFRs in biochar and their interactions with contaminants,this paper reviews the formation mechanisms of PFRs in biochar and the PFRs-mediated environmental applications of biochar in recent years.Finally,future challenges in this field are also proposed.This review provides a more comprehensive understanding on the emerging applications of biochar from the viewpoint of the catalytic role of PFRs. | Kun Luo Ya Pang Dongbo Wang Xue Li Liping Wang Min Lei Qi Huang Qi Yang | 2021 | Journal of Environmental Sciences2021，33，10： | 8 |
| 8 | Human vascular smooth muscle cells and endothelial cells cocultured on polyglycolic acid (70/30) scaffold in tissue engineered vascular graft显示文摘背景当前的修复术的、小直径显示出差的长期的明显率的脉管的接枝导致了另外的生物材料的追求。Biomaterials 成功地集成到包围织物应该匹配纸巾,而且地形学的不仅机械性质。Polyglycolic 酸(70/30 ) 被用作合成接枝决定人的脉管的光滑的肌肉房间和 endothelial 房间是否依附,幸存并且藏匿 endothelin 和 6-keto-prostaglandin F1 (6-keto-PGF1 ).Methods Endothelial 房间,光滑的肌肉房间从成年人的伟人被孤立 saphenous 静脉。他们独立在 vitro 在 polyglycolic 酸支架上被播种种脉管的补丁(分别地组织 A 和 B ) 并且在 vitro 到的 cocultured 长成脉管的补丁(组 C ) 。光滑的肌肉房间和 endothelial 房间被 immunohistochemical 分析识别, polyglycolic 酸上的房间的生长用扫描电子显微镜学被调查。在 culturing 溶液的 endothelin 和 6-keto-PGF1 的层次被 radioimmunology 检验测量光滑的肌肉房间遵守了的 endothelial function.Results 种子 polyglycolic 酸支架和超过 28 天在空隙成长了在整个支架形成一致房间分布。然后,种子 endothelial 房间在光滑的肌肉房间上形成了完全的 endothelial 层。在 culturing 答案的 endothelin 和 6-keto-prostaglandin F1 alpha 的层次是( 234 ??僚?????????????????????僚?????愠慮浥慩?湯汣獵潩獮????????????吗???吠?? | WEN Shao-jun ZHAO Li-min WANG Shen-guo LI Jing-xing CHEN Hua-ying LIU Jie-lin LIU Ya LUO Yi Roo Changizi | 2007 | Chinese Medical Journal2007，，15： | 8 |
| 9 | Distributed reinforcement learning to coordinate current sharing and voltage restoration for islanded DC microgrid显示文摘A novel distributed reinforcement learning(DRL)strategy is proposed in this study to coordinate current sharing and voltage restoration in an islanded DC microgrid.Firstly, a reward function considering both equal proportional current sharing and cooperative voltage restoration is defined for each local agent. The global reward of the whole DC microgrid which is the sum of the local rewards is regarged as the optimization objective for DRL. Secondly,by using the distributed consensus method, the predefined pinning consensus value that will maximize the global reward is obtained. An adaptive updating method is proposed to ensure stability of the above pinning consensus method under uncertain communication. Finally, the proposed DRL is implemented along with the synchronization seeking process of the pinning reward, to maximize the global reward and achieve an optimal solution for a DC microgrid. Simulation studies with a typical DC microgrid demonstrate that the proposed DRL is computationally efficient and able toprovide an optimal solution even when the communication topology changes. | Zifa LIU Ya LUO Ranqun ZHUO Xianlin JIN | 2018 | Journal of Modern Power Systems and Clean Energy2018，6，2： | 7 |
| 10 | Two new lignans from Dipteronia dyeriana显示文摘新 sesquilignan, 7 鈥 ? 8 鈥 ? didehydroherpetotriol (1 ) ,和新 lignan glycoside,(+)-isolariciresinol-9 鈥 ?O- 伪 -l-rhamnopyranosyl-(1 鈫 ? 6 )- 尾 -d-glucopyranoside (2 ) ,从 Dipteronia dyeriana 的分支被孤立。他们的结构被分光镜的方法和化学证据阐明。与 39 渭 m ol/L 的 IC50 价值对人的白血球过多症 K562 房间加重 1 项拥有的禁止的活动。 | Rong Guo Min Luo Chun Lin Long Ma Lin Li Zhi Qin Ouyang Yi Ping Zhou Yue Hu Wang Xing Yu Li Ya Na Shi | 2008 | Chinese Chemical Letters2008，19，10： | 7 |
| 11 | Association of Dietary Carotenoids Intake with Skeletal Fluorosis in the Coal-burning Fluorosis Area of Guizhou Province显示文摘Objective To explore whether the intake of dietary carotenoids could protect against skeletal fluorosis in Guizhou province in which coal-burning fluorosis is endemic. Methods A case-control study of 196 patients with skeletal fluorosis and 196 age and gender-matched controls was conducted in Zhijin, Guizhou Province. Face-to-face interviews were conducted to assess habitual dietary intake using a 75-item food frequency questionnaire and various covariates with structured questionnaires. Urinary fluoride was measured using an ion-selective electrode method. The genotype of superoxide dismutase 2(SOD2) rs11968525 was detected by Taq Man method. Results We observed significant dose-dependent inverse associations of skeletal fluorosis with intake of β-carotene, lutein/zeaxanthin, lycopene, and total carotenoids(P-trend = 0.002 to 0.018), whereas α-carotene and β-cryptoxanthin intakes were not found to be related to skeletal fluorosis, after adjustment for potential confounders. The adjusted ORs and 95% CI of skeletal fluorosis for the highest versus lowest quartile were 0.30(0.10, 0.86) for β-carotene, 0.23(0.08, 0.66) for lycopene, 0.26(0.10, 0.75) for lutein/zeaxanthin and 0.34(0.14, 0.74) for total carotenoids(all P-trend < 0.05). Stratified analyses showed that the protective effects of lutein/zeaxanthin and total carotenoids on skeletal fluorosis were more evident for individuals with the AG+AA genotypes of SOD2(rs11968525). Conclusion Increased intakes of β-carotene, lutein/zeaxanthin, lycopene, and total carotenoids are independently associated with a lower risk of coal-burning skeletal fluorosis. SOD2(rs11968525) polymorphisms might modify the inverse associations between dietary carotenoids and skeletal fluorosis. | LIU Jun YANG Sheng LUO Ming Jiang ZHAO Xun ZHANG Yuan Mei LUO Ya | 2018 | Biomedical and Environmental Sciences2018，31，6： | 7 |
| 12 | Demographic Characteristics and Environmental Risk Factors Exposure of Birth Defects in Pregnant Women: A Population-based Study显示文摘Worldwide, the incidence of birth defects in low-income countries is 6.42%, while in middle-income and high-income countries it is 5.57% and 4.72%, respectively;approximately 303, 000 newborns die from birth defects each year. In China, the incidence of birth defects is about 5.6%, and around 8.14 million people have congenital disabilities, accounting for 9.6% of total disabled people[1]. Birth defect remains a major clinical and public health challenge because of its high fatality rate and protracted and severe sequela. | LIN Hong LUO Mi Yang LUO Jia You ZENG Rong LI Ya Mei DU Qi Yun FANG Jun Qun | 2019 | Biomedical and Environmental Sciences2019，32，1： | 5 |
| 13 | Omics Approaches for Exploring Pneumoconiosis:A Review显示文摘Pneumoconiosis,a fatal lung disease caused by dust inhalation and deposition,is one of the leading occupational diseases worldwide[1].The dust is primarily inorganic particles,such as silica particles,coal dust,and asbestos fibers.If the diameter of dust is less than 5μm,it is defined as‘respirable dust’that can easily reach the distal airways and alveoli[2]. | LUO Ya QI Xian Mei PANG Jun Ling WANG Jing WANG Chen | 2021 | Biomedical and Environmental Sciences2021，34，1： | 5 |
| 14 | Research on Telescope TTL Coupling Noise in Intersatellite Laser Interferometry显示文摘The detection mission of gravitational waves in space is that the accuracy of the long-baseline intersatellite laser interferometry on the million-kilometer order needs to reach the order of 8 pm/Hz.Among all noise sources that affect the interferometry accuracy,tilt-to-length(TTL)coupling noise is the second largest source of noise after shot noise.This paper focuses on studying the contribution of TTL coupling noise of the telescope system in the intersatellite scientific interferometer.By referring to the laser interferometer space antenna(LISA)’s noise budget,TTL coupling noise is required to be within±25μm/rad(±300μrad).Therefore,this paper focuses on studying both the mechanism of TTL coupling noise due to the noise sources of the telescope and the method of suppressing the TTL noise,which can lay a foundation for noise distribution and the development of engineering prototypes in subsequent tasks. | Zhi WANG Tao YU Ya ZHAO Ziren LUO Wei SHA Chao FANG Yukun WANG Shaoxin WANG Keqi QI Yongxian WANG Xuanwen XU | 2020 | Photonic Sensors2020，10，3： | 5 |
| 15 | Preparation of hydrophilic molecularly imprinted polymers for tetracycline antibiotics recognition显示文摘吸水的分子地印的聚合物(MIP ) 作为模板用四圜素被准备,象支持 hydrophilic 合作单体象单体和 glycidilmethacrylate 酸的甲基丙烯。与普通 MIP 相比,为四圜素(TC ) 的吸水的 MIP 的印的效果和吸附数量极大地在水媒介被改进。而且,在玻璃质的碳电极上修改吸水的 MIP 制作的电气化学的传感器在食品样品为 TC 的决心被开发。 | Peng Wang Xiao Fang Fu Jing Li, Jing Luo Xiao Ya Zhao Ming Jun Sun Yin Zhu Shang Cheng Ye | 2011 | Chinese Chemical Letters2011，22，5： | 5 |
| 16 | Can transthoracic Doppler echocardiography be used to detect coronary slow flow phenomenon?显示文摘背景冠的慢流动现象(CSFP ) 是一重要, angiographic 临床的实体但是正在缺乏非侵略的检测技术。这研究试图阐明在诊断的 transthoracic Doppler echocardiography (TTDE ) 的价值并且在左前面的下降冠的慢流动监视(男孩) 我们连续地注册了的冠的 artery.Methods 有在男孩的 CSFP 的 27 个病人从 2009 年 8 月由冠的动脉 X 线摄影法检测了到 2010 年 4 月。有 angiographically 正常的冠的流动的 38 个病人用作控制。在心肌的梗塞(TIMI ) 的改正的 thrombolysis 框架计数(CTFC ) 被用来记录冠的流动速度。所有题目在冠的 angiography 以后在 24 个小时以内经历了 TTDE。男孩流动被检测,冠的心脏舒张的山峰速度(DPV ) 和心脏舒张的吝啬的速度(DMV ) 是 calculated.Results (92.3%) 65 中的六十个成功地使遭到经历了 TTDE。基线临床的特征在二个组之间是类似的。男孩的冠的 DPV 和 DMV 比在控制组在 CSFP 组是显著地更低的((0.228 ? ??????????? 劳 ?? ㄠ ?????????? ┶ ????? | NIE Shao-ping GENG Li-li WANG Xiao ZHANG Xiao-shan YANG Ya LIU Bai-qiu LI Jun QIAO Yan LIU Xin-min LUO Tai-yang DONG Jian-zeng LIU Xiao-hui MA Chang-sheng | 2010 | Chinese Medical Journal2010，，24： | 5 |
| 17 | The effect of environmental factors on spatial variability in land use change in the high-sediment region of China's Loess Plateau显示文摘In areas with topographic heterogeneity, land use change is spatially variable and influenced by climate, soil properties, and topography. To better understand this variability in the high-sediment region of the Loess Plateau in which soil loss is most severe and sediment diameter is larger than in other regions of the plateau, this study builds some indicators to identify the characteristics of land use change and then analyze the spatial variability as it is affected by climate, soil property, and topography. We build two indicators, a land use change intensity index and a vegetation change index, to characterize the intensity of land use change, and the degree of vegetation restoration, respectively. Based on a subsection mean method, the two indicators are then used to assess the spatial variability of land use change affected by climatic, edaphic, and topographic elements. The results indicate that: 1) Land use changed significantly in the period 1998–2010. The total area experiencing land use change was 42,302 km2, accounting for 22.57%of the study area. High-coverage grassland, other woodland, and forest increased significantly, while low-coverage grassland and farmland decreased in 2010 compared with 1998. 2) Land use change occurred primarily west of the Yellow River, between 35 and 38 degrees north latitude. The four transformation types, including(a) low-coverage grassland to medium-coverage grassland,(b) medium-coverage grassland to high-coverage grassland,(c) farmland to other woodland, and(d) farmland to medium-coverage grassland, were the primary types of land use change, together constituting 60% of the area experiencing land use change. 3) The spatial variability of land use change was significantly affected by properties of dryness/wetness, soil conditions and slope gradient. In general, land use changed dramatically in semi-arid regions, remained relativelystable in arid regions, changed significantly in clay-rich soil, remained relatively stable in clay-poor soil, changed dramatically in steeper slopes, and remained relatively stable in tablelands and low-lying regions. The increase in vegetation coincided with increasing changes in land use for each physical element. These findings allow for an evaluation of the effect of the Grain to Green Program, and are applicable to the design of soil and water conservation projects on the Loess Plateau of China. | LUO Ya YANG Shengtian ZHAO Changsen LIU Xiaoyan LIU Changming WU Linna ZHAQ Haigen ZHANG Yichi | 2014 | Journal of Geographical Sciences2014，24，5： | 5 |
| 18 | Genome-wide detection of additional fetal chromosomal abnormalities by cell-free DNA testing of 15,626 consecutive pregnant women显示文摘Cell-free DNA(cfDNA) testing for common fetal trisomies(T21, T18, T13) is highly effective. However, the usefulness of cfDNA testing in detecting other chromosomal abnormalities is unclear. We evaluated the performance of cfDNA testing for genome-wide abnormalities, and analyzed the incremental yield by reporting extra abnormalities. We performed genome-wide cfDNA testing in 15,626 consecutive pregnancies prospectively enrolled in this study. cfDNA testing results were reported and counseling was given depending on the presence of extra chromosomal abnormalities. cfDNA testing identified 190 cases(1.2%)of chromosomal abnormalities including 100 common trisomies and 90 additional abnormalities. By expanding the cfDNA reporting range to genome-wide abnormalities, the false positive rate increased to 0.39%(P<0.001) and positive predictive value(PPV) was reduced to 65.58%(P=0.42). However, the detection yield increased from 0.44% to 0.65%(P=0.014), and cfDNA testing detected 38.61%(39/101) additional abnormalities with no ultrasound and biochemical screening findings. cfDNA testing outperformed biochemical screening by showing 60 times higher true positive rate and fewer false negative results.Genome-wide cfDNA testing significantly increased the diagnostic yield by detecting extra abnormalities, especially those without diagnostic indications. Genome-wide cfDNA testing has fewer false positive and false negative results compared with biochemical screening. | Hong Yao Ya Gao Jia Zhao Rong Zhang Huixin Xu Huamei Hu Yanmei Luo Yuying Yuan Meili Fu Hongyun Zhang Hui Jiang Wei Wang Huanming Yang Jian Wang Zhiqing Liang Fang Chen | 2019 | Science China(Life Sciences)2019，62，2： | 4 |
| 19 | Synthesis of tanshinoneⅡA analogues and their inhibitory activities against Cdc25 phosphatases显示文摘Two series of tanshinone IIA derivatives were synthesized and evaluated for their antitumor activities as Cdc25 phosphatase inhibitors.Most of them demonstrated potent Cdc25 inhibitory activity and powerful cytotoxicity against A549 tumor cell line, producing IC_(50) values in very low micromolar range.At last,the preliminary SAR was discussed. | Wei Gang Huang Jing Ya Li Yu Luo Jia Li Wei Lu | 2009 | Chinese Chemical Letters2009，20，12： | 4 |
| 20 | Inhibiting Hv1 channel in peripheral sensory neurons attenuates chronic inflammatory pain and opioid side effects显示文摘Both opioids and nonsteroidal anti-inflammatory drugs(NSAIDS)produce deleterious side effects and fail to provide sustained relief in patients with chronic inflammatory pain.Peripheral neuroinflammation(PN)is critical for initiation and development of inflammatory pain.A better understanding of molecular mechanisms underlying PN would facilitate the discovery of new analgesic targets and the development of new therapeutics.Emerging evidence suggests that peripheral sensory neurons are not only responders to painful stimuli,but are also actively engaged in inflammation and immunity,whereas the intrinsic regulatory mechanism is poorly understood.Here we report the expression of proton-selective ion channel Hv1 in peripheral sensory neurons in rodents and humans,which was previously shown as selectively expressed in microglia in mammalian central nervous system.Neuronal Hv1 was up-regulated by PN or depolarizing stimulation,which in turn aggravates inflammation and nociception.Inhibiting neuronal Hv1 genetically or by a newly discovered selective inhibitor YHV98-4 reduced intracellular alkalization and ROS production in inflammatory pain,mitigated the imbalance in downstream SHP-1-pAKT signaling,and also diminished pro-inflammatory chemokine release to alleviate nociception and morphine-induced hyperalgesia and tolerance.Thus,our data reveal neuronal Hv1 as a novel target in analgesia strategy and managing opioids-related side effects. | Qiansen Zhang Yimin Ren Yiqing Mo Peipei Guo Ping Liao Yuncheng Luo Jie Mu Zhuo Chen Yang Zhang Ya Li Linghui Yang Daqing Liao Jie Fu Juwen Shen Wei Huang Xuewen Xu Yanyan Guo Lianghe Mei Yunxia Zuo Jin Liu Huaiyu Yang Ruotian Jiang | 2022 | Cell Research2022，32，5： | 3 |
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