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| 1 | A novel inhibitor of N^(6)-methyladenosine demethylase FTO induces m RNA methylation and shows anti-cancer activities显示文摘N^(6)-methyladenosine(m^(6)A)modification is critical for m RNA splicing,nuclear export,stability and translation.Fat mass and obesity-associated protein(FTO),the first identified m^(6)A demethylase,is critical for cancer progression.Herein,we developed small-molecule inhibitors of FTO by virtual screening,structural optimization,and bioassay.As a result,two FTO inhibitors namely 18077 and 18097 were identified,which can selectively inhibit demethylase activity of FTO.Specifically,18097 bound to the active site of FTO and then inhibited cell cycle process and migration of cancer cells.In addition,18097 reprogrammed the epi-transcriptome of breast cancer cells,particularly for genes related to P53 pathway.18097 increased the abundance of m^(6)A modification of suppressor of cytokine signaling1(SOCS1)m RNA,which recruited IGF2 BP1 to increase m RNA stability of SOCS1 and subsequently activated the P53 signaling pathway.Further,18097 suppressed cellular lipogenesis via downregulation of peroxisome proliferator-activated receptor gamma(PPARγ),CCAAT/enhancer-binding protein alpha(C/EBPa),and C/EBPβ.Animal studies confirmed that 18097 can significantly suppress in vivo growth and lung colonization of breast cancer cells.Collectively,we identified that FTO can work as a potential drug target and the small-molecule inhibitor 18097 can serve as a potential agent against breast cancer. | Guoyou Xie Xu-Nian Wu Yuyi Ling Yalan Rui Deyan Wu Jiawang Zhou Jiexin Li Shuibin Lin Qin Peng Zigang Li Hongsheng Wang Hai-Bin Luo | 2022 | Acta Pharmaceutica Sinica B2022，12，2： | 4 |
| 2 | Flexible,video-rate,and aberration-compensated axial dual-line scanning imaging with field-of-view jointing and stepped remote focusing显示文摘Parallel dual-plane imaging with a large axial interval enables the simultaneous observation of biological structures and activities in different views of interest.However,the inflexibility in adjusting the field-of-view(FOV)positions in three dimensions and optical sectioning effects,as well as the relatively small effective axial range limited by spherical aberration,have hindered the application of parallel dual-plane imaging.Herein,we propose a flexible,video-rate,and defocus-aberration-compensated axial dual-line scanning imaging method.We used a stepped mirror to remotely generate and detect dual axial lines with compensation for spherical aberration and FOV-jointing to rearrange into a head-to-head line for high-speed optical sectioning acquisition.The lateral and axial positions of the two FOVs could be flexibly adjusted before and during imaging,respectively.The method also allows the adjustment of optical sectioning effects according to specific experimental requirements.We experimentally verified the consistent imaging performance over an axial range of 300μm.We demonstrated high throughput by simultaneously imaging Brownian motions in two 250μm×250μm FOVs with axial and lateral intervals of 150μm and 240μm,respectively,at 24.5 Hz.We also showed potential application in functional imaging by simultaneously acquiring neural activities in the optic tectum and hindbrain of a zebrafish brain.The proposed method is,thus,advantageous compared to existing parallel dual-plane imaging and potentially facilitates intravital biological study in large axial range. | RUI JIN YALAN YU DAN SHEN QINGMING LUO HUI GONG JING YUAN | 2021 | Photonics Research2021，9，8： | 2 |
| 3 | Monodisperse mierospheres with poly(N-isopropylacrylamide) core and poly(2- hydroxyethyl methaerylate) shell 显示文摘 | Yu Yalan Xie Rui Zhang Maojie | 2010 | Journal of Colloid and Interface Science2010，346，2： | 1 |
| 4 | Dual drug delivery system with flexible and controllable drug ratios for synergistic chemotherapy显示文摘Determination of whether multidrug nanocarriers can deliver and release loaded drugs at a predefined synergistic ratio to target cancer cells is crucial.Although there are many successful applications for delivery of multiple drugs,most current carriers are unable to achieve coordinated loading and release,leading to a drug release ratio that disagrees with the predefined loading ratio.In this work,a simple dual-drug delivery system with a flexible and controllable drug release ratio was constructed to deliver two anticancer drugs,doxorubicin(DOX)and curcumin(CUR).The drug ratio of DOX and CUR can be easily tuned for an enhanced synergistic effect,and the drugs can be released at predesigned ratios due to synchronous drug activation and nanoparticle collapse.Drug release at predefined ratios for synergistic anticancer therapy was demonstrated via in vitro and in vivo experiments. | Yalan Tu Rui Zheng Fangzhou Yu Xuan Xiao Maoling Jiang Youyong Yuan | 2021 | Science China Chemistry2021，64，6： | 1 |
| 5 | Moxibustion modulates working memory in patients with amnestic mild cognitive impairment:a functional magnetic resonance imaging study显示文摘OBJECTIVE:To investigate the correlation between changes in brain activity associated with working memory and assessment scales of memory scores in amnestic mild cognitive impairment(aMCI)before and after moxibustion therapy.METHODS:aMCI patients were randomized into the moxibustion treatment(MT)group and the placebo moxibustion(PM)group.Each group received either moxibustion therapy or a placebo moxibustion for eight weeks.Neuropsychological performance and functional brain responses to a working memory task were assessed at baseline and at the end of treatment.Memory function was evaluated individually by the Rivermead behavioral memory test(RBMT),and working memory was assessed by the N-back task.RESULTS:Compared with the PM group,RBMT score changes were significant(P<0.05).In the MT group,the accuracy of the N-back texts increased compared with those before the intervention.After moxibustion intervention,the right insula,postcentral gyrus,precentral gyrus,superior temporal gyrus,thalamus,lingual gyrus,calcarine sulcus,posterior cingulate gyrus,middle frontal gyrus and anterior frontal gyrus were significantly activated(P=0.01,Cluster-level Family-Wise Error=0.05).Pearson correlation analysis showed that the insula,lingual gyrus and posterior cingulate gyrus were associated with changes in N-back score.Spearman correlation analysis showed that the postcentral gyrus,superior temporal gyrus,thalamus,lingual gyrus,and posterior cingulate gyrus were correlated with RBMT score changes.CONCLUSION:Moxibustion treatment improved memory in aMCI patients and was associated with the activation of the brain region of the insula,lingual gyrus,posterior cingulate gyrus,postcentral gyrus,superior temporal gyrus,and thalamus,which may be an important mechanism by which moxibustion improves the memory function. | LI Xingjie LIU Qiqi XIA Rui LIU Jun WANG Dan SHI Jiao KUANG Yuxing DAI Yalan HUANG Haoyu TANG Wei CHEN Shangjie | 2023 | Journal of Traditional Chinese Medicine2023，43，4： | 1 |
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