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| 1 | Discovery of Novel Androgen Receptor Ligands by Structure-based Virtual Screening and Bioassays显示文摘Androgen receptor(AR) is a ligand-activated transcription factor that plays a pivotal role in the development and progression of many severe diseases such as prostate cancer, muscle atrophy, and osteoporosis. Binding of ligands to AR triggers the conformational changes in AR that may affect the recruitment of coactivators and downstream response of AR signaling pathway.Therefore, AR ligands have great potential to treat these diseases. In this study, we searched for novel AR ligands by performing a docking-based virtual screening(VS) on the basis of the crystal structure of the AR ligand binding domain(LBD) in complex with its agonist. A total of 58 structurally diverse compounds were selected and subjected to LBD affinity assay, with five of them(HBP1-3, HBP1-17, HBP1-38, HBP1-51, and HBP1-58) exhibiting strong binding to AR-LBD. The IC50 values of HBP1-51 and HBP1-58 are 3.96 m M and 4.92 m M, respectively, which are even lower than that of enzalutamide(Enz, IC50= 13.87 m M), a marketed second-generation AR antagonist. Further bioactivity assays suggest that HBP1-51 is an AR agonist, whereas HBP1-58 is an AR antagonist. In addition, molecular dynamics(MD) simulations and principal components analysis(PCA) were carried out to reveal the binding principle of the newlyidentified AR ligands toward AR. Our modeling results indicate that the conformational changes of helix 12 induced by the bindings of antagonist and agonist are visibly different. In summary,the current study provides a highly efficient way to discover novel AR ligands, which could serve as the starting point for development of new therapeutics for AR-related diseases. | Wenfang Zhou Mojie Duan Weitao Fu Jinping Pang Qin Tang Huiyong Sun Lei Xu Shan Chang Dan Li Tingjun Hou | 2018 | Genomics, Proteomics & Bioinformatics2018，16，6： | 3 |
| 2 | Hyperlipidemia affects neuronal nitric oxide synthase expression in brains of focal cerebral ischemia rat model显示文摘BACKGROUND: Hyperlipidemia, a risk factor for ischemic cerebrovascular disease, may mediate production of neuronal nitric oxide synthase (nNOS) to induce increased nitric oxide levels, resulting in brain neuronal injury. OBJECTIVE: To investigate effects of hyperlipidemia on brain nNOS expression, and to verify changes in infarct volume and pathology during reperfusion, as well as neuronal injury following ischemia/reperfusion in a rat model of focal cerebral ischemia. DESIGN, TIME AND SETTING: Complete, randomized grouping experiment was performed at the Laboratory of Physiology, Shanxi Medical University from March 2005 to March 2006. MATERIALS: A total of 144 eight-week-old, male, Wistar rats, weighing 160-180 g, were selected. A rat model of middle cerebral artery occlusion was established by suture method after 4 weeks of formulated diet. Nitric oxide kit and rabbit anti-rat nNOS kit were respectively purchased from Nanjing Jiancheng Bioengineering Institute, China and Wuhan Boster Biological Technology, Ltd., China. METHODS: The rats were equally and randomly divided into high-fat diet and a normal diet groups. Rats in the high-fat diet group were fed a high-fat diet, consisting of 10% egg yolk powder, 5% pork fat, and 0.5% pig bile salt combined with standard chow to create hyperlipidemia. Rats in the normal diet group were fed a standard rat chow. A total of 72 rats in both groups were randomly divided into 6 subgroups: sham-operated, 4-hour ischemia, 4-hour ischemia/2-hour reperfusion, 4-hour ischemia/4-hour reperfusion, 4-hour ischemia/6-hour reperfusion, and 4-hour ischemia/12-hour reperfusion, with 12 rats in each subgroup. MAIN OUTCOME MEASURES: nNOS expression was measured by immunohistochemistry, and pathomorphology changes were detected by hematoxylin-eosin staining. Infarct volume and nitric oxide levels were respectively measured using 2, 3, 5-triphenyltetrazolium chloride (TTC) and immunohistochemistry. RESULTS: In the ischemic region, pathology changes were significant in the 4-hour ischemia/4-hour, 4-hour ischemia/6-hour reperfusion, and 4-hour ischemia/12-hour reperfusion subgroups fed on a high-fat diet compared to the same groups fed on a normal diet. In each ischemia subgroup, nNOS expression in brain tissues was higher than in the sham-operated subgroups fed on either the high-fat diet or normal diet (P < 0.01). At each ischemia/reperfusion time point, rats fed on a high-fat diet expressed higher levels of nNOS compared to rats fed on the normal diet (P < 0.05). When tissue was stained with TTC, a white infarction area was detected in the ischemic hemisphere, demonstrating that the infarct volume gradually increased with prolonged reperfusion time in each ischemia subgroup. At each ischemia/reperfusion time point, the infarct volume was larger in rats fed on a high-fat diet compared to those fed on a normal diet. CONCLUSION: nNOS expression was greater in hyperlipidemia rats following ischemia/reperfusion. Cerebral ischemia/reperfusion injury is aggravated with prolonged reperfusion time. | Jianji Pei Liqiang Liu Jinping Pang Xiaohong Tian | 2008 | Neural Regeneration Research2008，3，6： | 1 |
| 3 | Automatically varying the composition of a mixed refrigerant solution for single mixed refrigerant LNG (liquefied natural gas) process at changing working conditions显示文摘 | Xiongwen Xu Jinping Liu Le Cao Weiqiang Pang | 2014 | Energy2014，，： | 1 |
| 4 | ZmMYC7 directly regulates ZmERF147 to increase maize resistance to Fusarium graminearum显示文摘The jasmonic acid(JA)signaling pathway is involved in plant growth,development,and response to abiotic or biotic stresses.MYC2,a bHLH transcription factor,is a regulatory hub in the pathway.The function of ZmMYC7,a putative MYC2 ortholog,in jasmonate-signaled defense responses of maize has not been reported.In this study,we found that ZmMYC7 possesses JID,TAD,bHLH and Zip domains and essential characteristics of transcription factors:a nuclear location and transactivation activity.The ZmMYC7mutants showed markedly increased sensitivity to Fusarium graminearum and Setosphaeria turcica.The expression levels of the defense-associated genes ZmPR1,ZmPR2,ZmPR3,ZmPR5,ZmPR6,and ZmPR7 in response to F.graminearum infection were downregulated in ZmMYC7 mutants,while ZmPR4 and ZmPR10 were up-regulated.ZmMYC7 interacted with members of the ZmJAZ family,including ZmJAZ8,ZmJAZ11,and ZmJAZ12.ZmMYC7 physically interacted with G-box cis-elements in the ZmERF147 promoter in vitro and transcriptional activation of ZmERF147 by ZmMYC7 was inhibited by ZmJAZ11 and ZmJAZ12.ZmERF147 mutants were more susceptible to F.graminearum infection than inbred line B73with concomitant down-regulation of all defense-associated ZmPRs except ZmPR4.These findings indicate that ZmMYC7 functions in maize resistance to F.graminearum and sheds light on maize defense responses to pathogenic fungi via the JA signaling pathway. | Hongzhe Cao Kang Zhang Wei Li Xi Pang Pengfei Liu Helong Si Jinping Zang Jihong Xing Jingao Dong | 2023 | The Crop Journal2023，11，1： | 0 |
| 5 | Tailoring Anti-Impact Properties of Ultra-High Performance Concrete by Incorporating Functionalized Carbon Nanotubes显示文摘Replacing micro-reinforcing fibers with carbon nanotubes(CNTs)is beneficial for improving the impact properties of ultra-high performance concrete(UHPC);however,the weak wettability and dispersibility of CNTs and the weakly bonded interface between CNTs and UHPC limit their effectiveness as composites.Therefore,this study aims to enhance the reinforcement effect of CNTs on the impact properties of UHPC via functionalization.Unlike ordinary CNTs,functionalized CNTs with carboxyl or hydroxyl groups can break the Si-O-Ca-O-Si coordination bond in the C-S-H gel and form a new network in the UHPC matrix,effectively inhibiting the dislocation slip inside UHPC matrix.Furthermore,functionalized CNTs,particularly carboxyl-fu nctionalized CNTs,co ntrol the crystallization process and microscopic morphology of the hydration products,significantly decreasing and even eliminating the width of the aggregate-matrix interface transition zone of the UHPC.Moreover,the functionalized CNTs further decrease the attraction of the negatively charged silicate tetrahedron to Ca2+in the C-S-H gel,while modifying the pore structure(particularly the nanoscale pore structure)of UHPC,leading to the expansion of the intermediate CS-H layer.The changes in the microstructures of UHPC brought about by the functionalized CNTs significantly enhance its dynamic compressive strength,peak strain,impact toughness,and impact dissipation energy at strain rates of 200-800 s^(-1).Impact performance of UHPC containing a small amount of carboxyl-functionalized CNTs(especially the short ones)is generally better than that of UHPC containing hydroxyl-functionalized and ordinary CNTs;it is even superior to that of UHPC with a high steel fiber content. | Jialiang Wang Sufen Dong Sze Dai Pang Xun Yu Baoguo Han Jinping Ou | 2022 | Engineering2022，，11： | 0 |
| 6 | Nanomaterials disrupting cell-cell junctions towards various diseases显示文摘As the continuous development of the industrial revolution,nanomaterials with excellent characteristics have been widely applied in various fields,greatly increasing the probability of human exposure to nanomaterials and the concerns about the potential nanotoxicity.Existing studies have shown that the toxicity of nanomaterials may be closely related to oxidative stress,inflammatory response,phagocytosis dysfunction,DNA damage,etc.Based on our focus,nanomaterials may cross the human barrier through various channels and disrupt various cell-cell junctions,while the integrity of cellular barrier is a necessary for the normal physiological function of various organs.However,until now,there is still a lack of systematic discussion in this field.This review illustrates the importance of cell-cell junctions in maintaining various organ functions and highlights the mechanism of various nanomaterials disrupt cell-cell junctions,as well as the possible damage to various organs,such as brain,eye,lung,breast,intestine,placenta,testis,heart,liver,kidney,skin,etc.Awareness of the potential negative effects of nanomaterials will help scientists deeply understand the limitations of nanotechnology,inspiring them to develop safer and more efficient nanomaterials for future personalized nanomedicine. | Shanbin Xu Xinlong Pang Xinyu Zhang Qian Lv Meng Zhang Jinping Wang Nengyi Ni Xiao Sun | 2023 | Nano Research2023，16，5： | 0 |
| 7 | Facile synthesis of polypyrrole nanowires for high-performance supercapacitor electrode materials显示文摘Polypyrrole nanowires are facile synthesized under a mild condition with FeCl_3 as an oxidant. Polypyrrole nanowires with the width of 120 nm form many nanogaps or pores due to the intertwined nanostructures. More importantly, PPy nanowires were further applied for supercapacitor electrode materials.After electrochemical testing, it was observed that the PPy nanowire based electrode showed a large specific capacitance(420 Fg^(-1), 1.5 Ag^(-1)) and good rate capability(272 Fg^(-1), 18.0 Ag^(-1)), which is larger than that of most of published results. The as-prepared electrode can work well even after 8000 cycles at 1.5 Ag^(-1). | Junhong Zhao Jinping Wu Bing Li Weimin Du Qingli Huang Mingbo Zheng Huaiguo Xue Huan Pang | 2016 | Progress in Natural Science:Materials International2016，26，3： | 0 |
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