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| 1 | Artificial intelligence in drug design显示文摘Thanks to the fast improvement of the computing power and the rapid development of the computational chemistry and biology,the computer-aided drug design techniques have been successfully applied in almost every stage of the drug discovery and development pipeline to speed up the process of research and reduce the cost and risk related to preclinical and clinical trials.Owing to the development of machine learning theory and the accumulation of pharmacological data, the artificial intelligence(AI) technology, as a powerful data mining tool, has cut a figure in various fields of the drug design, such as virtual screening,activity scoring, quantitative structure-activity relationship(QSAR) analysis, de novo drug design, and in silico evaluation of absorption, distribution, metabolism, excretion and toxicity(ADME/T) properties. Although it is still challenging to provide a physical explanation of the AI-based models, it indeed has been acting as a great power to help manipulating the drug discovery through the versatile frameworks. Recently, due to the strong generalization ability and powerful feature extraction capability,deep learning methods have been employed in predicting the molecular properties as well as generating the desired molecules,which will further promote the application of AI technologies in the field of drug design. | Feisheng Zhong Jing Xing Xutong Li Xiaohong Liu Zunyun Fu Zhaoping Xiong Dong Lu Xiaolong Wu Jihui Zhao Xiaoqin Tan Fei Li Xiaomin Luo Zhaojun Li Kaixian Chen Mingyue Zheng Hualiang Jiang | 2018 | Science China(Life Sciences)2018，61，10： | 10 |
| 2 | Long-distance ranging with high precision using a soliton microcomb显示文摘Laser-based light detection and ranging(lidar)plays a significant role in both scientific and industrial areas.However,it is difficult for existing lidars to achieve high speed,high precision,and long distance simultaneously.Here,we demonstrate a high-performance lidar based on a chip-scaled soliton microcomb(SMC)that can realize all three specialties simultaneously.Aided by the excellent properties of ultrahigh repetition rate and the smooth envelope of the SMC,traditional optical frequency comb(OFC)-based dispersive interferometry is heavily improved and the measuring dead zone induced by the mismatch between the repetition rate of the OFC and resolution of the optical spectrum analyzer is totally eliminated.Combined with an auxiliary dual-frequency phase-modulated laser range finder,the none-dead-zone measurable range ambiguity is extended up to 1500 m.The proposed SMC lidar is experimentally implemented in both indoor and outdoor environment.In the outdoor baseline field,real-time,high-speed(up to 35 k Hz)measurement of a long distance of^1179 m is achieved with a minimum Allan deviation of 5.6μm at an average time of 0.2 ms(27 nm at an average time of 1.8 s after high-pass filtering).The present SMC lidar approaches a compact,fast,high-precision,and none-dead zone long-distance ranging system,aimed at emerging applications of frontier basic scientific research and advances in industrial manufacturing. | JINDONG WANG ZHIZHOU LU WEIQIANG WANG FUMIN ZHANG JIAWEI CHEN YANG WANG JIHUI ZHENG SAI T.CHU WEI ZHAO BRENT E.LITTLE XINGHUA QU WENFU ZHANG | 2020 | Photonics Research2020，8，12： | 8 |
| 3 | Important role of a LAL regulator Sta R in the staurosporine biosynthesis and high-production of Streptomyces fradiae CGMCC 4.576显示文摘Staurosporine, belonging to indolocarbazole compounds, is regarded as an excellent lead compound for synthesizing antitumor agents as a potent inhibitor against various protein kinases. In this study, two separate clusters(cluster A and cluster B),corresponding to biosyntheses of K-252 c(staurosporine aglycone) and sugar moiety, were identified in Streptomyces fradiae CGMCC 4.576 and heterologously expressed in Streptomyces coelicolor M1146 separately or together. Sta R, a cluster-situated LAL family regulator, activates staurosporine biosynthesis by binding to the promoter regions of sta O-sta C and sta G-sta N. The conserved sequences GGGGG and GCGCG were found through gradually truncating promoters of sta O and sta G, and further determined by mutational experiments. Overexpression of sta R with the supplementation of 0.01 g L^–1 Fe SO4 increased staurosporine production to 5.2-fold compared with that of the parental strain Streptomyces fradiae CGMCC 4.576 in GYM medium. Our results provided an approach for improvement of staurosporine production mediated by a positive regulator and established the basis for dissecting the regulatory mechanisms of other indolocarbazole compounds with clinical application value. | Hanye Guan Yue Li Jiazhen Zheng Ning Liu Jihui Zhang Huarong Tan | 2019 | Science China(Life Sciences)2019，62，12： | 6 |
| 4 | Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase显示文摘Human 5-lipoxygenase(5-LOX)is a well-validated drug target and its inhibitors are potential drugs for treating leukotriene-related disorders.Our previous work on structural optimization of the hit compound 2 from our in-house collection identified two lead compounds,3a and 3b,exhibiting a potent inhibitory profile against 5-LOX with IC_(50) values less than 1 mmol/L in cell-based assays.Here,we further optimized these compounds to prepare a class of novel pyrazole derivatives by opening the fusedring system.Several new compounds exhibited more potent inhibitory activity than the lead compounds against 5-LOX.In particular,compound 4e not only suppressed lipopolysaccharide-induced inflammation in brain inflammatory cells and protected neurons from oxidative toxicity,but also significantly decreased infarct damage in a mouse model of cerebral ischemia.Molecular docking analysis further confirmed the consistency of our theoretical results and experimental data.In conclusion,the excellent in vitro andin vivo inhibitory activities of these compounds against 5-LOX suggested that these novel chemical structures have a promising therapeutic potential to treat leukotriene-related disorders. | Yu Zhou Jun Liu Mingyue Zheng Shuli Zheng Chunyi Jiang Xiaomei Zhou Dong Zhang Jihui Zhao Deju Ye Mingfang Zheng Hualiang Jiang Dongxiang Liu Jian Cheng Hong Liu | 2016 | Acta Pharmaceutica Sinica B2016，6，1： | 1 |
| 5 | LOSARTAN PREVENTS SEPSIS-INDUCED ACUTE LUNG INJURY AND DECREASES ACTIVATION OF NUCLEAR FACTORκB AND MITOGEN-ACTIVATED PROTEIN KINASES显示文摘 | Lihan Shen Hongying Mo Lin Cai Tianhan Kong Weihao Zheng Jihui Ye Junhua Qi Zhenglun Xiao | 2009 | Shock2009，，5： | 1 |
| 6 | Guidelines for the diagnosis and treatment of acute pancreatitis in China (2021)显示文摘Acute pancreatitis(AP)is a common acute abdominal condition of the digestive system.In recent years,treatment concepts,methods,and strategies for the diagnosis of AP have advanced,and this has played an important role in promoting the standardization of AP diagnosis and treatment and improving the treatment quality of AP patients.On the basis of previous guidelines and expert consensus,this guideline adopts an evidence-based,problem-based expression;synthesizes important clinical research data at home and abroad in the most recent 5 years;and forms 29 recommendations through multidisciplinary expert discussion,including diagnosis,treatment,and follow-up.It is expected to provide evidence support for the treatment of AP in the clinical setting in China. | Fei Li Shouwang Cai Feng Cao Rufu Chen Deliang Fu Chunlin Ge Chunyi Hao Jihui Hao Heguang Huang Zhixiang Jian Gang Jin Ang Li Haimin Li Shengping Li Weiqin Li Yixiong Li Tingbo Liang Xubao Liu Wenhui Lou Yi Miao Yiping Mou Chenghong Peng Renyi Qin Chenghao Shao Bei Sun Guang Tan Xiaodong Tian Huaizhi Wang Lei Wang Wei Wang Weilin Wang Junmin Wei Heshui Wu Wenming Wu Zheng Wu Changqing Yan Yinmo Yang Xiaoyu Yin Xianjun Yu Chunhui Yuan Taiping Zhang Yupei Zhao on behalf of the Chinese Pancreatic Surgery Association | 2021 | Journal of Pancreatology2021，4，2： | 1 |
| 7 | Effect of humidityand temperature on power electric-field intensity显示文摘 | YU Jihui ZHENG Yali XU Luwen | 2009 | Journal ofChongqing University: Natural Sciences Edition2009，32，2： | 1 |
| 8 | Gender differences in challenging behaviors,management and outcomes in elderly patients with delirium显示文摘BACKGROUND:Gender differences have been reported in some common mental disorders.However,few studies have monitored gender differences in individuals with delirium.OBJECTIVE:To explore gender differences in challenging behaviors,management and outcomes in age-matched elderly patients with delirium.DESIGN,TIME AND SETTING:A retrospective cohort study was performed in the Bankstown-Lidcombe Hospital,Sydney,Australia,from October 2008 to April 2009.METHODS:Patients,aged 65-90 years,diagnosed with delirium according to the International Classification of Diseases(ICD)-10 in the Psychogeriatric Unit of Bankstown Lidcombe Hospital from January 2002 to October 2008 were reviewed.All the patients were measured according to the Confusion Assessment Method upon admission.Those who developed delirium during hospitalization were excluded.MAIN OUTCOME MEASURES:Cause of delirium,wandering,aggression,duration of delirium,physical restraint,use of antipsychotic medicine,recovery from delirium,discharge back home,length of stay,one-to-one nursing care,falls and absconding rate.RESULTS:The 131 age-matched delirious patients comprised 54 males and 77 females.The behavioral disorders of wandering [odds ration(OR) = 2.612,95% confidence interval(CI) = 1.26-5.413,P = 0.009] and aggression(OR = 2.243,95% CI = 1.028-4.891,P = 0.04) were more frequent in males than in females.More males received one-to-one nursing care(OR = 4.114,95% CI = 1.355-12.491,P = 0.008),were more likely to receive antipsychotic medications(OR = 2.24,95% CI = 1.095-4.583,P = 0.021) and more likely to be physically restrained(OR = 2.07,95% CI = 1.02-1.02,P = 0.043) compared with female patients.All absconding patients(3/131,2.3%) were male.In addition,male patients displayed a greater falling rate compared with females(OR = 4.57,95% CI = 1.519-13.722,P = 0.004).CONCLUSION:There are gender differences in challenging behaviors,management and outcomes in elderly delirious patients.Males with delirium display more challenging behaviors that require physical restraint and pharmacological management including wandering and aggression;males also abscond and have a higher rate of falls compared with female patients. | Jihui Lv Qing Shen Daniel Kan Yin Chan Anne Hoolahan Xi Zheng Bin Ong Sharon Reutens Zheng Chen | 2010 | Neural Regeneration Research2010，5，10： | 0 |
| 9 | High frequency of alternative splicing variants of the oncogene Focal Adhesion Kinase in neuroendocrine tumors of the pancreas and breast显示文摘The characteristic genetic abnormality of neuroendocrine neoplasms(NENs),a heterogeneous group of tumors found in various organs,remains to be identified.Here,based on the analysis of the splicing variants of an oncogene Focal Adhesion Kinase(FAK)in The Cancer Genome Atlas datasets that contain 9193 patients of 33 cancer subtypes,we found that Box 6/Box 7-containing FAK variants(FAK^(6/7))were observed in 7(87.5%)of 8 pancreatic neuroendocrine carcinomas and 20(11.76%)of 170 pancreatic ductal adenocarcinomas(PDACs).We tested FAK variants in 157 tumor samples collected from Chinese patients with pancreatic tumors,and found that FAK^(6/7)was positive in 34(75.6%)of 45 pancreatic NENs,19(47.5%)of 40 pancreatic solid pseudopapillary neoplasms,and 2(2.9%)of 69 PDACs.We further tested FAK splicing variants in breast neuroendocrine carcinoma(BrNECs),and found that FAK^(6/7)was positive in 14(93.3%)of 15 BrNECs but 0 in 23 non-NEC breast cancers.We explored the underlying mechanisms and found that a splicing factor serine/arginine repetitive matrix protein 4(SRRM4)was overexpressed in FAK^(6/7)-positive pancreatic tumors and breast tumors,which promoted the formation of FAK^(6/7)in cells.These results suggested that FAK^(6/7)could be a biomarker of NENs and represent a potential therapeutic target for these orphan diseases. | Dawei Xie Zheng Wang Beibei Sun Liwei Qu Musheng Zeng Lin Feng Mingzhou Guo Guizhen Wang Jihui Hao Guangbiao Zhou | 2023 | Frontiers of Medicine2023，17，5： | 0 |
| 10 | Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors显示文摘Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer therapy.In this study,we synthesized and evaluated the biological activity of 66 pyrazolo[3,4-d]pyridazinone derivatives.Kinase inhibition,cell proliferation,and whole blood stability assays were used to evaluate their activity on FGFR,allowing us to explore structureàactivity relationships and thus to gain understanding of the structural requirements to modulate covalent inhibitors’selectivity and reactivity.Among them,compound 10h exhibited potent enzymatic activity against FGFR and remarkably inhibited proliferation of various cancer cells associated with FGFR dysregulation,and suppressed FGFR signaling pathway in cancer cells by the immunoblot analysis.Moreover,10h displayed highly potent antitumor efficacy (TGI Z 91.6%,at a dose of 50 mg/kg) in the FGFR1-amplified NCI-H1581 xenograft model. | Xiaowei Wu Mengdi Dai Rongrong Cui Yulan Wang Chunpu Li Xia Peng Jihui Zhao Bao Wang Yang Dai Dan Feng Tianbiao Yang Hualiang Jiang Meiyu Geng Jing Ai Mingyue Zheng Hong Liu | 2021 | Acta Pharmaceutica Sinica B2021，11，3： | 0 |
| 11 | Consensus of clinical diagnosis and treatment for non-functional pancreatic neuroendocrine neoplasms with diameter<2 cm显示文摘In clinical practice,pancreatic neuroendocrine neoplasms(pNENs)with a diameter smaller than 2 cm are commonly referred to as small pNENs.Due to their generally favorable biological characteristics,the diagnosis and treatment of small pNENs differ from other pNENs and are somewhat controversial.In response to this,the Chinese Pancreatic Surgery Association,Chinese Society of Surgery,Chinese Medical Association have developed a consensus on the diagnosis and treatment of small pNENs,which is based on evidence-based medicine and expert opinions.This consensus covers various topics,including concepts,disease assessment,treatment selection,follow-up,and other relevant aspects. | Wu Wenming Cai Shouwang Chen Rufu Fu Deliang Ge Chunlin Hao Chunyi Hao Jihui Huang Heguang Jian Zhixiang Jin Gang Li Fei Li Haimin Li Shengping Li Weiqin LiYixiong Liang Tingbo Liu Xubao Lou Wenhui Miao Yi Mou Yiping Peng Chenghong Qin Renyi Shao Chenghao Sun Bei Tan Guang Wang Huaizhi Wang Lei Wang Wei Wang Weilin Wei Junmin Wu Heshui Wu Zheng Yan Changqing Yang Yinmo Yin Xiaoyu Yu Xianjun Yuan Chunhui Zhao Yupei | 2023 | Journal of Pancreatology2023，6，3： | 0 |
| 12 | Guidelines for the diagnosis and treatment of pancreatic cancer in China (2021)显示文摘The incidence of pancreatic cancer has been rising worldwide,and its clinical diagnosis and treatment remain a great challenge.To present the update and improvements in the clinical diagnosis and treatment of pancreatic cancer in recent years,Chinese Pancreatic Association,the Chinese Society of Surgery,Chinese Medical Association revised the Guidelines for the Diagnosis and Treatment of Pancreatic Cancer in China(2014)after reviewing evidence-based and problem-oriented literature published during 2015-2021,mainly focusing on highlight issues regarding diagnosis and surgical treatment of pancreatic cancer,conversion strategies for locally advanced pancreatic cancer,treatment of pancreatic cancer with oligo metastasis,adjuvant and neoadjuvant therapy,standardized processing of surgical specimens and evaluation of surgical margin status,systemic treatment for unresectable pancreatic cancer,genetic testing,as well as postoperative follow up of patients with pancreatic cancer.Forty recommendation items were finally proposed based on the above issues,and the quality of evidence and strength of recommendations were graded using the Grades of Recommendation,Assessment,Development,and Evaluation system.This guideline aims to standardize the clinical diagnosis and therapy,especially surgical treatment of pancreatic cancer in China,and further improve the prognosis of patients with pancreatic cancer. | Yinmo Yang Xueli Bai Dapeng Bian Shouwang Cai Rufu Chen Feng Cao Menghua Dai Chihua Fang Deliang Fu Chunlin Ge Xiaochao Guo Chunyi Hao Jihui Hao Heguang Huang Zhixiang Jian Gang Jin Fei Li Haimin Li Shengping Li Weiqin Li Yixiong Li Hongzhen Li Tingbo Liang Xubao Liu Wenhui Lou Yi Miao Yiping Mou Chenghong Peng Renyi Qin Chenghao Shao Bei Sun Guang Tan Xiaodong Tian Huaizhi Wang Lei Wang Wei Wang Weilin Wang Junmin Wei Heshui Wu Wenming Wu Zheng Wu Jingyong Xu Changqing Yan Xiaoyu Yin Xianjun Yu Chunhui Yuan Taiping Zhang Jixin Zhang Jun Zhou Yupei Zhao on behalf of the Chinese Pancreatic Surgery Association | 2021 | Journal of Pancreatology2021，4，2： | 0 |
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