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| 1 | Small molecule compound induces chromatin de-condensation and facilitates induced pluripotent stern cell generation显示文摘 | Xiaoyuan Wei Yueting Chen Yongyu Xu YangZhan Ru Zhang Min Wang Qiuhong Hua Haifeng Gu Fajun Nan Xin Xie | 2014 | Journal of Molecular Cell Biology2014，8，5： | 13 |
| 2 | Dynamic Perception of Jasmonates by the F-Box Protein C0l1显示文摘 | Jianbin Yan Ruifeng Yao Li Chen Suhua Lit Min Gut Fajun Nan Daoxin Xie | 2018 | Molecular Plant2018，11，10： | 7 |
| 3 | The HDAC inhibitor GCJ-490A suppresses c-Met expression through IKKα and overcomes gefitinib resistance in non-small cell lung cancer显示文摘Objective:The novel compound GCJ-490A has been discovered as a pan-histone deacetylase(HDAC)inhibitor that exerts potent inhibitory activity against HDAC1,HDAC3,and HDAC6.Because of the important roles of HDACs in lung cancer development and the high distribution of GCJ-490A in lung tissue,we explored the anti-tumor potency of GCJ-490A against non-small cell lung cancer(NSCLC)in vitro and in vivo in this study.Methods:The in vitro effects of GCJ-490A alone or combined with the EGFR inhibitor gefitinib against NSCLC were measured with proliferation,apoptosis,and colony formation assays.NSCLC xenograft models were used to investigate the efficacy of GCJ-490A combined with gefitinib for the treatment of NSCLC in vivo.Western blot assays,luciferase reporter assays,chromatin immunoprecipitation assays,quantitative real time-PCR,immunohistochemistry,and transcription factor activity assays were used to elucidate possible mechanisms.Results:GCJ-490A effectively inhibited NSCLC cell proliferation and induced apoptosis in vitro and in vivo.Interestingly,inhibition of HDAC1 and HDAC6 by GCJ-490A increased histone acetylation at the IKKαpromoter and enhanced IKKαtranscription,thus decreasing c-Met.Moreover,this c-Met downregulation was found to be essential for the synergistic anti-tumor activity of GCJ-490A and gefitinib.Conclusions:These findings highlight the promising potential of HDAC inhibitors in NSCLC treatment and provide a rational basis for the application of HDAC inhibitors in combination with EGFR inhibitors in clinical trials. | Ting He Yinglei Gao Yanfen Fang Yangming Zhang Shuwei Zhang Fajun Nan Jian Ding Yi Chen | 2022 | Cancer Biology & Medicine2022，19，8： | 3 |
| 4 | Troglitazone inhibits cell proliferation by attenuation of epidermal growth factor receptor signaling independent of peroxisome proliferator-activated receptor γ显示文摘Peroxisome 激活 proliferator 的受体(PPAR ) 属于 ligand 依赖的抄写因素的原子荷尔蒙受体总科。最近的结果证明了 PPAR 纬的收缩筋例如 troglitazone (TGZ ) ,能禁止房间增长并且支持独立于 PPAR 纬的房间区别。在现在的学习,我们提供 TGZ 可以直接绑在 EGFR 并且触发它发信号和 PPAR 纬的成为主观独立人士的证据。详细研究表明有 TGZ 的延长孵化有效地稀释了由指向受体到 endo-lysosomal 降级机械发信号的 EGFR。尽管细胞外的调整信号的发信号 kinase 小径被 TGZ 短暂地在 EGFR overexpressing 癌症细胞激活,导致 EGF 的 Akt phosphorylation 的抑制很可能说明了 TGZ 在 pharmacologically 可完成的集中引起的肿瘤细胞的生长拘捕。因此,我们提供了显示 TGZ 由支持 EGFR 降级和 attenuating Akt phosphorylation 禁止房间增长的证据的一根新线。 | Xiaoqi Li Xuanming Yang Youli Xu Xuejun Jiang Xin Li Fajun Nan Hong Tang | 2009 | Cell Research2009，19，6： | 2 |
| 5 | Development of the novel ACLY inhibitor 326E as a promising treatment for hypercholesterolemia显示文摘Hepatic cholesterol accumulation is an important contributor to hypercholesterolemia,which results in atherosclerosis and cardiovascular disease(CVD).ATP-citrate lyase(ACLY)is a key lipogenic enzyme that converts cytosolic citrate derived from tricarboxylic acid cycle(TCA cycle)to acetyl-CoA in the cytoplasm.Therefore,ACLY represents a link between mitochondria oxidative phosphorylation and cytosolic de novo lipogenesis.In this study,we developed the small molecule 326E with an enedioic acid structural moiety as a novel ACLY inhibitor,and its CoA-conjugated form 326E-CoA inhibited ACLY activity with an IC_(50)=5.31±1.2μmol/L in vitro.326E treatment reduced de novo lipogenesis,and increased cholesterol efflux in vitro and in vivo.326E was rapidly absorbed after oral administration,exhibited a higher blood exposure than that of the approved ACLY inhibitor bempedoic acid(BA)used for hypercholesterolemia.Chronic 326E treatment in hamsters and rhesus monkeys resulted in remarkable improvement of hyperlipidemia.Once daily oral administration of 326E for 24 weeks prevented the occurrence of atherosclerosis in ApoE^(-/-)mice to a greater extent than that of BA treatment.Taken together,our data suggest that inhibition of ACLY by 326E represents a promising strategy for the treatment of hypercholesterolemia. | Zhifu Xie Mei Zhang Qian Song Long Cheng Xinwen Zhang Gaolei Song Xinyu Sun Min Gu Chendong Zhou Yangming Zhang Kexin Zhu Jianpeng Yin Xiaoyan Chen Jingya Li Fajun Nan | 2023 | Acta Pharmaceutica Sinica B2023，13，2： | 1 |
| 6 | Effect of GR24 Stereoisomers on Plant Development in Arabidopsis显示文摘 | Suhua Li Linhai Chen Yuwen Li Ruifeng Yao Fei Wang Mai Yang Min Gu Fajun Nan Daoxin Xie Jianbin Yan | 2016 | Molecular Plant2016，9，10： | 1 |
| 7 | A Versatile Approach to PI(3,4)P2, PI(4,5)P2, and PI(3,4,5)P3 from (L)-quebrachitol显示文摘 | LIXIN QIQA YOUHONG HU FAJUN NAN | 2000 | Organic Letters2000，2，2： | 1 |
| 8 | Synthetic Analogues of Betulinic Acid as Potent Inhibitors of PS1/BACE1 Interaction to Reduce Aβ Generation显示文摘lupane 类型 triterpenoids 被赋予以大量生物活动例如抗病毒,反煽动性并且 anticancer 活动。我们这里在 Alzheimers 描述它的潜在的申请疾病(广告) 治疗作为 PS1/BACE1 的一个禁止者相互作用。3-α-Akebonoic 酸,从高产量发出了屏蔽,被发现防碍 PS1/BACE1 相互作用和还原剂淀粉的 β-protein (Aβ) 生产。鉴于有限来源,当为铅优化和它的衍生物的一个集中的图书馆的开始的材料被构造获得 PS1/BACE1 相互作用的 triterpenoid 类型禁止者的结构活动关系(SAR ) 的更好的理解,我们相反使用了自然地富有的 betulinic 酸(化合物 2 ) 。化合物 22 最后被选择为大多数有势力 PS1/BACE1 相互作用禁止者,它有效地减少了 Aβ 产生。 | Chenlu Zhang Xiaoyin Wang Jin Cui Xiaohang Li Yangming Zhang Xin Wang Haifeng Gu Wei Li Xin Xie Jian Zhao Gang Pei Fajun Nan | 2017 | Chinese Journal of Chemistry2017，35，1： | 0 |
| 9 | Protecting-Group-Free One-Step Palladium-Catalyzed Coupling on C25 of Cucurbitacin B Expands Chemical Diversity with Improved Cytotoxicity against A549 Cells显示文摘The natural product cucurbitacin B has been widely studied because of its multiple biological activities,especially its potent antitumor effects.However,modifications of cucurbitacin B are mainly focused on the C2 and C16 site,studies on the C25 acetoxy group are still limited.We successfully developed a palladium-catalyzed allylic coupling of cucurbitacin B with boronic acids,providing a one-step approach to expand the chemical diversity of the C25 position.Our method was protecting-group-free,showing a good functional group tolerance and a wide substrate scope under mild reaction conditions.A library of 29 derivatives was prepared,compounds 2q and 2u showed higher cytotoxicity against A549 cells than cucurbitacin B,compounds 2n and 2o maintained potency,and the introduced hydroxyl and amino groups could be further derived. | Ning Zhuo Jie Ma Lei Cao Linhai Chen Fajun Nan | 2022 | Chinese Journal of Chemistry2022，40，14： | 0 |
| 10 | Synthesis toward the Lindenane-type Sesquiterpenoid Monomer of Chlorahololide A显示文摘向用一个 Yamamoto 重新整理, intramolecular cyclopropanation 反应, 1,3-dipolar 环合,和 intramolecular 的 Chlorahololide A 的 lindenane 类型 sesquiterpenoid 单体的合成的调查哎呀反应给了枢轴的中介 20。这给能产生 Chloranthaceae 家庭的进一步自然的产品的一条实际合成线路。 | Haizhen Zhang Fajun Nan | 2013 | Chinese Journal of Chemistry2013，31，1： | 0 |
| 11 | Construction of the Hexacyclic Core of Dispirocochlearoids A-C via a Diels-Alder Reaction显示文摘The natural products of dispirocochlearoids are complex Ganoderma meroterpenoids featuring a 6/6/5/6/6/6 ring system and are selective cox-2 inhibitors.Herein,we describe our progress regarding the total synthesis of dispirocochlearoids A-C,in which a hexacyclic skeleton was constructed firstly.The key steps of this work involve an intermolecular[4+2]cycloaddition reaction,a ring cleavage approach via Ticla,and the installation of a profoundly sterically hindering lactone. | Qiang Fu Yonghui Wang Fajun Nan | 2022 | Chinese Journal of Chemistry2022，40，13： | 0 |
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