|
|
|
题名
|
作者
|
年代
|
出处
|
被引量
|
| 1 | The PI3K/Akt/GSK-3β/ROS/eIF2B pathway promotes breast cancer growth and metastasis via suppression of NK cell cytotoxicity and tumor cell susceptibility显示文摘Objective: To examine the effect of pSer9-GSK-3β on breast cancer and to determine whether the underlying metabolic and immunological mechanism is associated with ROS/eIF2B and natural killer(NK) cells.Methods: We employed TWS119 to inactivate GSK-3β by phosphorylating Ser9 and explored its effect on breast cancer and NK cells. The expression of GSK-3β, natural killer group 2 member D(NKG2D) ligands, eIF2B was quantified by PCR and Western blot. We measured intracellular reactive oxygen species(ROS) and mitochondrial ROS using DCFH-DA and MitoSOX^(TM) probe,respectively, and conducted quantitative analysis of cellular respiration on 4T1 cells with mitochondrial respiratory chain complex Ⅰ/Ⅲ kits.Results: Our investigation revealed that TWS119 downregulated NKG2D ligands(H60 a and Rae1), suppressed the cytotoxicity of NK cells, and promoted the migration of 4T1 murine breast cancer cells. Nevertheless, LY290042, which attenuates p-GSK-3β formation by inhibiting the PI3K/Akt pathway, reversed these effects. We also found that higher expression of p Ser9-GSK-3β induced higher levels of ROS, and observed that abnormality of mitochondrial respiratory chain complex Ⅰ/Ⅲ function induced the dysfunction of GSK-3β-induced electron transport chain, naturally disturbing the ROS level. In addition, the expression of NOX3 and NOX4 was significantly up-regulated, which affected the generation of ROS and associated with the metastasis of breast cancer. Furthermore, we found that the expression of pSer535-eIF2B promoted the expression of NKG2D ligands(Mult-1 and Rae1) following by expression of pSer9-GSK-3β and generation of ROS.Conclusions: The PI3K/Akt/GSK-3β/ROS/eIF2B pathway could regulate NK cell activity and sensitivity of tumor cells to NK cells,which resulted in breast cancer growth and lung metastasis. Thus, GSK-3β is a promising target of anti-tumor therapy. | Fengjiao Jin Zhaozhen Wu Xiao Hu Jiahui Zhang Zihe Gao Xiao Han Junfang Qin Chen Li Yue Wang | 2019 | Cancer Biology & Medicine2019，16，1： | 20 |
| 2 | Spatial distribution and pollution assessment of mercury in sediments of Lake Taihu,China显示文摘Spatial distribution patterns of total mercury (THg) in 36 surficial sediment samples representing five regions of Lake Taihu were assessed using the ArcGis geostatistical analyst module. The pollution levels of THg were also evaluated from the same five lake regions. Concentrations of THg were in a ranged of 23-168 ng/g (mean 55 ng/g) in surfical sediments, which was significantly higher than those established baseline levels of the lake. Results of THg indicated that the northern region exhibited notably higher values, the bay regions showed elevated values relative to open areas, and the lakeside regions were higher than those observed in the central area. Lake Taihu suffered moderate to high Hg pollution, and expressed clear Hg enrichment status according to monomial pollution index I geo and human activity factors. The concentrations of THg in the surficial sediments of Lake Taihu showed moderate-strong variation (coefficient of variation 52%). Geostatistical analysis indicated a weak spatial self-correlation, suggesting the contamination of Hg in Lake Taihu is primarily the result of anthropogenic activities. | Chunxiao Chen Binghui Zheng Xia Jiang Zheng Zhao Yuzhu Zhan Fengjiao Yi Jiaying Ren | 2013 | Journal of Environmental Sciences2013，25，2： | 16 |
| 3 | An ACC Oxidase Gene Essential for Cucumber Carpel Development显示文摘在植物的性决心产生便于 outcrossing 并且提高基因差异的单性的花。在黄瓜和甜瓜,乙烯支持心皮开发并且逮捕雄蕊开发。五性决心基因被识别了,包括四个编码在乙烯生合成催化限制率的步骤的 1-aminocyclopropane-1-carboxylate (ACC ) synthase,和抄写因素基因在甜瓜对应于孟德尔的地点 gynoecious 并且是女性的一个否定管理者的 CmWIP1。ACC oxidase (ACO ) 把 ACC 变换成乙烯;然而,它留下逃犯在黄瓜染色体的基因为性决心是它 ACO 并且怎么批评的 CmWIP1 镇压女花的开发。在这研究,我们在 ACO 基因发现了那个变化, CsACO2,在忍受仅仅男的花的黄瓜授与 androecy。变化破坏 CsACO2 的酶的活动,导致从射击尖端的 50% 更少的乙烯排放。CsACO2 在心皮 primordia 被表示,它的表示为性决心在关键阶段在女花与 CsACS11 的重叠了,大概提供为合适的 CsACS2 要求的足够的乙烯表示。CmACO3, CsACO2 的 ortholog,在心皮区域显示出一个类似的表示模式,建议 CsACO2/CmACO3 的保存功能。我们表明了那 CsWIP1, CmWIP1 的 ortholog,能直接绑 CsACO2 的倡导者并且镇压它的表示。一起拿,我们建议由 WIP1 抄写因素和 ACO 组成的一个大概保存的规章的模块在黄瓜和甜瓜控制单性的花开发。 | Huiming Chen Jinjing Sun Shuai Li Qingzhi Cui Huimin Zhang Fengjiao Xin Huaisong Wang Tao Lin Dongli Gao Shenhao Wang Xia Li Donghui Wang Zhonghua Zhang Zhihong Xu Sanwen Huang | 2016 | Molecular Plant2016，9，9： | 16 |
| 4 | Generation of B Cell-Deficient Pigs by Highly Efficient CRISPR/Cas9-Mediated Gene Targeting显示文摘Generating B cell-deficient mutant is the first step to produce human antibody repertoires in large animal models. In this study, we applied the clustered regularly interspaced short palindromic repeat(CRISPR)/CRISPR-associated(Cas) system to target the JHregion of the pig Ig M heavy chain gene which is crucial for B cell development and differentiation. Transfection of Ig M-targeting Cas9 plasmid in primary porcine fetal fibroblasts(PFFs) enabled inducing gene knock out(KO) in up to 53.3% of colonies analyzed, a quarter of which harbored biallelic modification, which was much higher than that of the traditional homologous recombination(HR). With the aid of somatic cell nuclear transfer(SCNT) technology, three piglets with the biallelic Ig M heavy chain gene mutation were produced. The piglets showed no antibody-producing B cells which indicated that the biallelic mutation of the Ig M heavy chain gene effectively knocked out the function of the Ig M and resulted in a B cell-deficient phenotype. Our study suggests that the CRISPR/Cas9 system combined with SCNT technology is an efficient genome-editing approach in pigs. | Fengjiao Chen Ying Wang Yilin Yuan Wei Zhang Zijian Ren Yong Jin Xiaorui Liu Qiang Xiong Qin Chen Manling Zhang Xiaokang Li Lihua Zhao Ze Li Zhaoqiang Wu Yanfei Zhang Feifei Hu Juan Huang Rongfeng Li Yifan Dai | 2015 | Journal of Genetics and Genomics2015，42，8： | 15 |
| 5 | Valuation of Lake and Marsh Wetlands Ecosystem Services in China显示文摘Wetlands are highly productive natural ecosystems, providing valuable goods and services. There is growing interest in transferring ecosystem service value from the existing wetlands studied to other wetlands ecosystems at a large geographic scale. The benefit transfer method uses the known values from wetlands to predict the value of other wetland sites. This methodology requires only limited time and resources. The present study calculated the value of the ecological services provided by lake and marsh wetlands in China in terms of biodiversity indices, water quality indices and economic indices. Basic data on wetlands were obtained through remote sensing images. The results show that: 1) The total ecosystem service value of the lake and marsh wetlands in 2008 was calculated to be 8.1841 × 1010 United States Dollars(USD), with the marsh and lake wetlands contributing 5.6329 × 1010 and 2.5512 × 1010 USD, respectively. Values of marsh ecosystem service were concentrated in Heilongjiang Province(2.5516 × 1010 USD), Qinghai Province(1.2014 × 1010 USD), and Inner Mongolia Autonomous Region(1.1884 × 1010 USD). The value of the lakes were concentrated in Tibet Autonomous Region(6.223 × 109 USD), Heilongjiang(5.810 × 109 USD), and Qinghai(5.500 × 109 USD). 2) Waste treatment and climate regulation services contributed to 26.29% and 24.74% respectively, of the total ecosystem service value of the marsh wetlands. Hydrological regulation and waste treatment contributed to 41.39% and 32.75%, respectively, of the total ecosystem service value of the lake wetlands. 3) The total ecological service value of the lake and marsh wetlands was 54.64% of the total service value of natural grassland ecosystems and 30.34% of the total service value of forests ecosystems in China. | ZHANG Yiran ZHOU Demin NIU Zhenguo XU Fengjiao | 2014 | Chinese Geographical Science2014，24，3： | 13 |
| 6 | Stabilizing nickel sulfide nanoparticles with an ultrathin carbon layer for improved cycling performance in sodium ion batteries显示文摘Nanostructured 金属硫化物是为钠离子电池的潜在的电极材料;然而,他们典型地由于大体积变化和分泌物产品的溶解受不了很差的骑车的稳定性。此处,我们建议合理材料设计策略让基于硫化物的材料处理这些问题。拿镍硫化物(是的 NiS x ) 一个例子,我们证明它的电气化学的性能能被限制 NiS 在滤的 x nanoparticles 传导性的碳 nanotube 网络,并且与 ultrathin 碳涂层层稳定他们。碳层用作一个物理障碍减轻体积变化和活跃材料的溶解的效果。混合材料展出了一个大可逆特定的能力 > 超过 200 的 500 mAh/g 和优秀骑车稳定性骑车。作为电池阳极材料给 NiS x 的传统地有问题的性质,我们相信这里报导的观察高效反映我们的材料设计策略的有效性。 | Feipeng Zhao Qiufang Gong Brian Traynor Duo Zhang Jiaojiao Li Hualin Ye Fengjiao Chen Na Han Yeyun Wang Xuhui Sun Yanguang Li | 2016 | Nano Research2016，9，10： | 6 |
| 7 | Climatological Characteristics of Summer Precipitation over East Asia Measured by TRMM PR:A Review显示文摘Precipitation is an important indicator of climate change and a critical process in the hydrological cycle, on both the global and regional scales. Methods of precipitation observation and associated analyses are of strategic importance in global climate change research. As the first space-based radar, the Tropical Rainfall Measuring Mission(TRMM)Precipitation Radar(PR) has been in operation for almost 17 years and has acquired a huge amount of cloud and precipitation data that provide a distinctive view to help expose the nature of cloud and precipitation in the tropics and subtropics. In this paper we review recent advances in summer East Asian precipitation climatology studies based on long-term TRMM PR measurements in the following three aspects:(1) the three-dimensional structure of precipitation,(2) the diurnal variation of precipitation, and(3) the recent precipitation trend. Additionally, some important prospects regarding satellite remote sensing of precipitation and its application in the near future are discussed. | Yunfei FU Xiao PAN Yuanjian YANG Fengjiao CHEN Peng LIU | 2017 | Journal of Meteorological Research2017，31，1： | 6 |
| 8 | A Study on Spatial Interpolation of Temperature in Anhui Province Based on ANUSPLIN显示文摘To achieve refined temperature grid data with high accuracy and high spatial resolution,hourly temperature grid dataset with spatial resolution of 1 km in Anhui Province from January to December in 2016 was established using the ANUSPLIN thin plate spline algorithm,which meets the needs of climate change research and meteorological disaster risk assessment. And the interpolation error was analyzed. The results show that the interpolated values of hourly temperature by ANUSPLIN are close to the observed values in 2016. The error is generally below 1. 5 ℃,and the root mean square error is 0. 937 6 ℃. On monthly scale,the interpolated values of hourly temperature by ANUSPLIN are also close to the observed values.In October,November,June and May,the interpolation accuracy is the highest,and the proportion of absolute error of hourly temperature lower than 2 ℃ is up to 99%,97. 4%,98. 1% and 97. 4% respectively. In February,March,August and December,the interpolation accuracy is the lowest,and the proportion of absolute error higher than 2 ℃ is 8. 1%,5. 3%,4. 1% and 4. 2% respectively. Due to the effect of complex topography in Anhui,the interpolation accuracy is the lowest in the mountainous areas of southern and western Anhui,and the interpolation error in these regions even exceeds 1. 5 ℃ annually and 1. 8 ℃ monthly. | Wen Huayang Chen Fengjiao Li Jun Qiu Kangjun Wang Gen | 2019 | Meteorological and Environmental Research2019，10，2： | 5 |
| 9 | Contribution of tropical cyclone rainfall at categories to total precipitation over the Western North Pacific from 1998 to 2007显示文摘从中国气象学的管理( CMA )从热带降雨测量使命( TRMM )多卫星 降水分析( TMPA ) 3B42 和最好的轨道数据基于 10 年 降水数据,季节,热带气旋( TC )的每月、年度的贡献到全部的降雨的 降水从5月在 1998~2007 期间在西方的诺思太平洋( WNP )上被分析到12月。结果显示出那:(1 ) TC 季节的降雨贡献在内陆区域从 4%到上面 40% 在 15 的海洋区域 ???? 蹂 ? ? 吗?? | CHEN FengJiao FU YunFei | 2015 | Science China Earth Sciences2015，58，11： | 4 |
| 10 | Long-term variability of the carbon balance in a large irrigated area along the lower Yellow River from 1984 to 2006显示文摘The irrigated areas in the northern region of China are important food production areas. Therefore, studies on the variability of the carbon balance in these agro-ecosystems are fundamental for the management of carbon sequestration. This paper simulated the long-term variability of the carbon balance in a typical irrigated area along the lower Yellow River from 1984 to 2006, using a process-based ecosystem model called the Simple Biosphere Model, version 2. The mean annual gross primary production (GPP), mean annual net assimilation rate (NAR), mean annual soil respiration (Rs ), and mean annual net ecosystem exchange (NEE) were 1733, 1642, 1304, and 338g C m-2 a-1 , respectively. A significant increasing trend in the seasonal total NAR during the wheat growing season, and a significant decreasing trend in the seasonal total NAR during the maize growing season were detected. However, no significant trend was found in the annual NAR, R s , and NEE. The average carbon sequestration was 1.93 Tg C a-1 when the grain harvest was not taken into account, and the carbon sequestration amount during the maize season was higher than that during the wheat season. However, the agro-ecosystem was a weak carbon source with a value of 0.23 Tg C a-1 , when the carbon in the grain was assumed emitted into the atmosphere. | LEI HuiMin YANG DaWen CAI JianFeng WANG FengJiao | 2013 | Science China Earth Sciences2013，56，4： | 4 |
| 11 | Impacts of Park Landscape Structure on Thermal Environment Using QuickBird and Landsat Images显示文摘Urban parks composed mostly of vegetation and water bodies can effectively mitigate the urban heat island effect. Many studies have investigated the cooling effects of urban parks; however, little attention has been given to park landscape structure. Based on landscape metrics, this study has explored the influences of the park landscape structure on its inner thermal environment, taking heavily urbanized Beijing Municipality in China as the study area. Three indices, including the percentage of landscape(PLAND), landscape shape index(LSI) and aggregation index(AI), were used to measure the composition and configuration characteristics of the landscape components inside the parks. The indices were calculated for five landscape types being interpreted from Quickbird images. Urban thermal conditions were measured using the land surface temperature(LST) derived from Landsat TM images. The results showed that the park LST had a negative relationship with the park size, but no significant relationship was found with park shape. For the park's interior landscape, however, the configuration and composition characteristics of the landscape components inside the park explained 70% of the park LST variance. The area percentage of water bodies and the aggregation index of woodland were identified as the key influencing characteristics. In addition, when the composition and configuration characteristics of the park landscape components were separately considered, the configuration characteristics(LSI and AI) explained approximately 54% of the variance in park LST, which was comparable with that explained by the composition characteristics(PLAND). Thus, this study suggested that an effective and practical way for urban cooling park design is the optimization of spatial configuration of landscape components inside the park. | XU Xinliang CAI Hongyan QIAO Zhi WANG Liang JIN Cui GE Yaning WANG Luyao XU Fengjiao | 2017 | Chinese Geographical Science2017，27，5： | 4 |
| 12 | Bone morphogenetic proteins:Relationship between molecular structure and their osteogenic activity显示文摘Bone morphogenetic proteins(BMPs)are a family of potent,multifunctional growth factors belonging to transforming growth factor-(TGF-).They are highly conservative in structures.Over 20 members of BMPs with varying functions such as embryogenesis,skeletal formation,hematopoiesis and neurogenesis have been identified in human body.BMPs are unique growth factors that can induce the formation of bone tissue individually.BMPs can induce the differentiation of bone marrow mesenchymal stem cells into osteoblastic lineage and promote the proliferation of osteoblasts and chondrocytes.BMPs stimulate the target cells by specific membrane-bound receptors and signal transduced through mothers against decapentaplegic(Smads)and mitogen activated protein kinase(MAPK)pathways.It has been demonstrated that BMP-2,BMP-4,BMP-6,BMP-7,and BMP-9 play an important role in bone formation.This article focuses on the molecular characterization of BMPs family members,mechanism of osteogenesis promotion,related signal pathways of osteogenic function,relationships between structure and osteogenetic activity,and the interactions among family members at bone formation. | Jian Yang Pujie Shi Maolin Tu Yun Wang Meng Liu Fengjiao Fan Ming Du | 2014 | Food Science and Human Wellness2014，3，3： | 4 |
| 13 | Material design at nano and atomic scale for electrocatalytic CO2 reduction显示文摘Electrocatalytic CO2 reduction (ECR) into value-added chemicals offers potential solution for renewable energy as well as global carbon footprint concerns. In this review we introduce the general methods and metrics that are commonly applied in ECR, followed by a discussion of current reaction mechanisms and different pathways. We highlight how size and structure of electrocatalysts affect ECR performance and review recent advances in metalfree and single-atom catalysts. The challenges of ECR are also discussed and optimistic perspectives are made for future work. | Fengjiao Yu Penghui Wei Yang Yang Yuhui Chen Limin Guo Zhangquan Peng | 2019 | Nano Materials Science2019，1，1： | 3 |
| 14 | Augmented renal clearance in Chinese intensive care unit patients after traumatic brain injury: a cross-sectional study显示文摘To the Editor:Augmented renal clearance(ARC)refers to an enhanced elimination of circulating solutes,including drugs,by the kidneys at a rate statistically higher than normal.On the first day of intensive care unit(ICU)admission,ARC occurrence may predict continued creatinine clearance(CrCl)elevation for 1 day to several weeks.[1]ARC has a substantial adverse effect on renally cleared antibiotics'pharmacokinetics/pharmacodynamics.Treatment failure or worse outcomes are more frequent in ARC patients.Thus,a'one size fits all'approach to drug dosing in ARC patients is inappropriate;dosing requires adjustment for some variables. | Zilong Dang Hong Guo Bin Li Maohua Zhen Jian Liu Yuhui Wei Hongyan Qin Zhimin Dou Lei Zhang Lei Zhu Yongqiang Cao Fengjiao Li Xinan Wu | 2022 | Chinese Medical Journal2022，，6： | 3 |
| 15 | Photocatalytic decompositions of gaseous HCHO and methylene blue with highly ordered TiO_2 nanotube arrays显示文摘The highly ordered Ti O_2nanotubes(NTs) were fabricated by the anodic oxidation method.Their morphology,structure and crystalline phase were characterized by scanning electron microscopy(SEM) and X-ray diffractometer(XRD).The effects of morphology,specific surface area,pore structures and photocatalytic activity of the Ti O_2 NTs were investigated.UV–vis spectra analysis showed that its light absorption had been extended to the visible light range.The photocatalytic activity of the as-prepared samples was evaluated by photocatalytic oxidation of gaseous HCHO and MB aqueous solution.The samples had better adhesion strength in the dark and showed a higher photocatalytic activity than nanoparticles.Especially,with ultraviolet light pretreatment,the nanotubes exhibited more stable active for photocatalytic decomposition and the photodecomposition rate remained at high level after 3 cycles of the photocatalysis experiment.Thus,how the number of surface active group ·OH increased and the mechanism for the great improvement for the photocatalytic activity are discussed. | Lixia Li Jing Ya Fengjiao Hu Zhifeng Liu Lei E | 2016 | Journal of Energy Chemistry2016，25，4： | 2 |
| 16 | Controllable Biosynthesis and Properties of Gold Nanoplates Using Yeast Extract显示文摘Biosynthesis of gold nanostructures has drawn increasing concerns because of its green and sustainable synthetic process. However, biosynthesis of gold nanoplates is still a challenge because of the expensive source and difficulties of controllable formation of morphology and size. Herein, one-pot biosynthesis of gold nanoplates is proposed, in which cheap yeast was extracted as a green precursor. The morphologies and sizes of the gold nanostructures can be controlled via varying the pH value of the biomedium. In acid condition, gold nanoplates with side length from 1300 ± 200 to 300 ± 100 nm and height from 18 to 15 nm were obtained by increasing the pH value. Whereas, in neutral or basic condition, only gold nanoflowers and nanoparticles were obtained. It was determined that organic molecules, such as succinic acid, lactic acid, malic acid, and glutathione, which are generated in metabolism process, played important role in the reduction of gold ions. Besides, it was found that the gold nanoplates exhibited plasmonic property with prominent dipole infrared resonance in near-infrared region, indicating their potential in surface plasmon-enhanced applications, such as bioimaging and photothermal therapy. | Zhi Yang Zhaohui Li Xuxing Lu Fengjiao He Xingzhong Zhu Yujie Ma Rong He Feng Gao Weihai Ni Yasha Yi | 2017 | Nano-Micro Letters2017，9，1： | 2 |
| 17 | Heat Exchanger Network Retrofit of Diesel Hydrotreating Unit Using Pinch Analysis显示文摘Diesel hydrotreating unit(DHT)is an integral part of the refinery,and its energy-saving optimization is of great significance to the enterprise.In this paper,process simulation software and energy management software are used to simulate the flowsheet and analyze the energy consumption,respectively.Stream data obtained from an existing DHT are applied in the pinch analysis for retrofitting the heat exchanger network(HEN)to achieve maximum energy utilization by using pinch analysis.Since DHT is constrained by pressure,the pressure factor is considered in the process of retrofitting.The results show that the amount of cross-pinch heat transfer is reduced,the inlet temperature of the furnace is increased by 55℃,and the amount of hot and cold utilities can be reduced by 70.25%and 50.16%,respectively.The economic evaluation indicates that the operating cost is saved by 4.39×10^(6)$/a,and the payback period is about 2 months. | Sun Mengying Zhang Fengjiao Liu Xinglong Sun Lanyi | 2021 | China Petroleum Processing & Petrochemical Technology2021，23，2： | 2 |
| 18 | Chromosome G-banding in SituHybridization of RFLP Marker umc58 Linked with the Gene hm1 Dictating Helminthosporium carbonum Susceptibility1 in Maize显示文摘ChromosomeG┐bandinginSituHybridizationofRFLPMarkerumc58LinkedwiththeGenehm1DictatingHelminthosporiumcarbonumSusceptibility1in... | Deng Fengjiao Feng Xiaorong Zheng Junying Liu Ting Yi Qingming Zhang Xiyuan Xiao Hanbing Xue Zhigang | 1997 | Wuhan University Journal of Natural Sciences1997，2，2： | 2 |
| 19 | A New Indicator for Global Food Security Assessment: Harvested Area Rather Than Cropland Area显示文摘Cropland area has long been used as a key indicator of food security.However,grain yield is not solely controlled by the area of the cropland.Therefore,we proposed a new indicator to assess food security.Results show that from 1992 to 2004,the global cropland area increased by 840200 km^(2)(99.4%),but the grain yield increased only by 310 million t(29.1%);and from 2004 to 2015,the cropland area decreased by 39000 km^(2)(4.64%),but the grain yield increased by 370 million t(70.84%).This result showed that grain yield was not linearly correlated with cropland area,and delimiting the threshold of cropland protection may not guarantee food security.Combined with further correlation analysis,we found that the increase in the global grain yield was more closely related to the harvested area(R^(2)=0.94),which indicated that the harvested area is a more scientific and accurate indicator than cropland area in terms of guaranteeing food security.Therefore,if governments want to ensure the food security,they should choose a new and more accurate indicator:harvested area rather than cropland area. | SONG Fengjiao WANG Shijie BAI Xiaoyong WU Luhua WANG Jinfeng LI Chaojun CHEN Huan LUO Xuling XI Huipeng ZHANG Sirui LUO Guofeng YAN Mengqi ZHEN Qingqing | 2022 | Chinese Geographical Science2022，32，2： | 2 |
| 20 | Synthesis of selective PAK4 inhibitors for lung metastasis of lung cancer and melanoma cells显示文摘The p21 activated kinase 4(PAK4) is serine/threonine protein kinase that is critical for cancer progression.Guided by X-ray crystallography and structure-based optimization,we report a novel subseries of C-3-substituted 6-ethynyl-1 H-indole derivatives that display high potential and specificity towards group Ⅱ PAKs.Among these inhibitors,compound 55 exhibited excellent inhibitory activity and kinase selectivity,displayed superior anti-migratory and anti-invasive properties against the lung cancer cell line A549 and the melanoma cell line B16.Compound 55 exhibited potent in vivo antitumor metastatic efficacy,with over 80% and 90% inhibition of lung metastasis in A549 or B16-BL6 lung metastasis models,respectively.Further mechanistic studies demonstrated that compound 55 mitigated TGF-β1-induced epithelial-mesenchymal transition(EMT). | Peilu Song Fan Zhao Dahong Li Jiqiang Qu Miao Yao Yuan Su Hanxun Wang Miaomiao Zhou Yujie Wang Yinli Gao Feng Li Dongmei Zhao Fengjiao Zhang Yu Rao Mingyu Xia Haitao Li Jian Wang Maosheng Cheng | 2022 | Acta Pharmaceutica Sinica B2022，12，6： | 2 |
您所在的机构暂未开通此部分的功能，请联系管理员