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Discovery of ARF1-targeting inhibitor demethylzeylasteral as a potential agent against breast cancer

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Acta Pharmaceutica Sinica B 2022年第5期12卷 2619-2622页

作者： Jie Chang Ruirui Yang Lifan Chen Zisheng Fan Jingyi Zhou Hao Guo Yinghui Zhang Yadan Liu Guizhen Zhou Keke Zhang Kaixian Chen hualiang Jiang Mingyue Zheng Sulin Zhang School of Chinese Materia Medica Nanjing University of Chinese MedicineNanjing 210023China Drug Discovery and Design Center State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences Beijing 100049China Shanghai Institute for Advanced Immunochemical Studies and School of Life Science and TechnologyShanghaiTech UniversityShanghai 200031China

To the Editor:ADP-ribosylation factor 1 (ARF1) plays a critical role in regulating vesicle formation and transport1. The dysregulation of ARF1 expression and/or activity is involved in many human cancers, such as brea... 详细信息

关键词： ADP-ribosylation factor 1 Breast cancer Demethylzeylasteral Virtual screening

Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors

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Acta Pharmaceutica Sinica B 2021年第3期11卷 781-794页

作者： 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 State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China Division of Anti-Tumor Pharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences Beijing 100049China School of Chinese Materia Medica Nanjing University of Chinese MedicineNanjing 210023China

Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer *** this study,we synthesized and evaluated the biological activity of 66 pyrazolo[3,4-d]pyridazinone *** 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 *** 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 ***,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.

关键词： Tyrosine kinase Covalent FGFR inhibitors Virtual screening Pyrazolo[3,4-d]pyridazinone Structure-activity relationships Antitumor efficacy

“Qingfei Paidu Decoction”—A Possible Choice of Phytotherapy for Severe Acute Respiratory Infection Caused by Coronavirus Disease-19

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American Journal of Plant Sciences 2020年第7期11卷 1111-1136页

作者： hualiang Chen Dandan Song Tianlai Gao Jingjing Yang Yutao Ma Qian Deng Department of Pharmacy Shaoxing Seventh People’s Hospital Shaoxing China

This work is aimed to study the therapeutics and pharmacology of the treatment of severe acute respiratory infection caused by coronavirus disease-19 (COVID-19) with traditional Chinese medicine (TCM) “Qingfei Paidu Decoction”. We analyze the “Diagnosis and Treatment Protocol for Novel Coronavirus Pneumonia” (Version I to Version VII) made by China, “Clinical management of severe acute respiratory infection when novel coronavirus (2019-nCoV) infection is suspected—Interim guidance” made by World Health Organization (WHO), “Therapeutic Guidelines: Respiratory” published by Australia, and the origin of classical prescription of Qingfei Paidu Decoction: “Shanghan Lun (Treatise on Febrile Diseases)” and “Jinkui Yaolue (Synopsis of Golden Chamber)”. We search the dictionary of traditional Chinese medicine (Version II) manually. We search literatures from 2001 to 2020 on Wiley online library. We conduct a comparative study on the therapeutic options and indications among Qingfei Paidu Decoction, COVID-19 and chronic obstructive pulmonary disease (COPD). And we carry out pharmacological inquiry of Qingfei Paidu Decoction. The therapeutic options and indications of Qingfei Paidu Decoction in China, COVID-19 and COPD are considered to be basically consistent. Qingfei Paidu Decoction has a definite therapeutic effect on the symptoms, basic diseases and complications for COVID-19 and COPD. Qingfei Paidu Decoction is a possible choice of phytotherapy for severe acute respiratory infection caused by COVID-19.

关键词： Qingfei Paidu Decoction COVID-19 COPD Pharmacology Therapeutics

Molecular representation for drug discovery with graph attention mechanism

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Molecular representation for drug discovery with graph atten...

2019中国化学会第十五届全国计算（机）化学学术会议

作者：郑明月 Zhaoping Xiong hualiang Jiang 中科院上海药物所 Drug Discovery and Design Center State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences School of Life Science and Technology ShanghaiTech University

Hunting for chemicals with favorable pharmacological and toxicological properties remains a formidable challenge for AI drug design, and the "black box" nature of deep learning models may induce distrust and restrict deep learning applications in practice. Here, we aim to approach these challenges by developing an AI molecular representation that is interpretable, and may help medicinal chemists gain chemical insights from discovery data directly. Called Attentive FP, this new molecular representation uses a graph attention mechanism to learn from relevant drug discovery related data. It achieves state-of-the-art predictive performances on a variety of data sets, and what it learns is interpretable via feature visualization for. The results suggested that Attentive FP automatically learns nonlocal intramolecular interactions from specified tasks, such as chemical environment and aromaticity.

关键词： Drug design Artificial intelligence Molecular representation

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出版的价值诉求“一元性”与“多元性”

出版科学 2023年第3期31卷 50-57页

作者：徐华亮湖南省社会科学院(湖南省人民政府发展研究中心) 长沙410003

出版是有意识的社会活动,出版的政治价值根植于意识、思想、信念层面,文化价值根植于国家、社会和国民层面,涉及到公共性、真实性和异质性的“多元”出版文化与权威性、倾向性和话语性“一元”意识形态的复杂关系。出版需要把握好一元... 详细信息

出版是有意识的社会活动,出版的政治价值根植于意识、思想、信念层面,文化价值根植于国家、社会和国民层面,涉及到公共性、真实性和异质性的“多元”出版文化与权威性、倾向性和话语性“一元”意识形态的复杂关系。出版需要把握好一元导向与非主流意识形态、反主流多元导向意识形态之间的“张力”。出版“产业”利益追求和“事业”文化使命之间的博弈日益激烈,在意识形态、经济利益和文化使命环境中,社会性、媒介性、公共性价值决定了出版的内在价值。出版价值诉求是具有多重文化属性实践活动的“多元”,又是社会属性意识理念的“一元”。出版价值诉求遵从“阶级性—人民性”统一价值、“群体符号—个体自觉”递进价值、“监督权—自由权”融合价值的行动逻辑,其中,统一价值是根本价值,递进价值是核心价值,融合价值是负荷价值。

关键词：出版价值诉求一元性二元性

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Rational Design of Organelle-Targeted Fluorescent Probes:Insights from Artificial Intelligence

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Research 2023年第3期2023卷 769-779页

作者： Jie Dong Jie Qian Kunqian Yu Shuai Huang Xiang Cheng Fei Chen hualiang Jiang Wenbin Zeng Xiangya School of Pharmaceutical Sciences Central South UniversityChangsha 410083P.R.China National Engineering Research Center of Rice and Byproduct Deep Processing School of Food Science and EngineeringCentral South University of Forestry and TechnologyChangsha 410004P.R.China State Key Laboratory of Drug Research Drug Discovery and Design CenterShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203P.R.China

Monitoring the physiological changes of organelles is essential for understanding the local biological information of cells and for improving the diagnosis and therapy of ***,fluorescent probes are considered as the most powerful tools for imaging and have been widely applied in biomedical ***,the expected targeting effects of these probes are often inconsistent with the real *** design of fluorescent probes mainly depends on the empirical knowledge of researchers,which was inhibited by limited chemical space and low ***,we proposed a novel multilevel framework for the prediction of organelle-targeted fluorescent probes by employing advanced artificial intelligence *** this way,not only the targeting mechanism could be interpreted beyond intuitions but also a quick evaluation method could be established for the rational ***,the targeting and imaging powers of the optimized and synthesized probes based on this methodology were verified by quantitative calculation and experiments.

关键词： inhibited diagnosis Probe

PanGu Drug Model: learn a molecule like a human

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Science China(Life Sciences) 2023年第4期66卷 879-882页

作者： Xinyuan Lin Chi Xu Zhaoping Xiong Xinfeng Zhang Ningxi Ni Bolin Ni Jianlong Chang Ruiqing Pan Zidong Wang Fan Yu Qi Tian hualiang Jiang Mingyue Zheng Nan Qiao Laboratory of Health Intelligence Huawei Cloud Computing Technologies Co.LtdGuizhou 550025China Shanghai Institute for Advanced Immunochemical Studies and School of Life Science and TechnologyShanghaiTech UniversityShanghai 200031China Drug Discovery and Design Center State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China

Dear Editor,Recent achievements in large-scale pre-trained models like GPT-3 and PanGu-α have demonstrated astounding performances in many downstream tasks of natural language processing (NLP),confirming AI to be user-oriented for even industrial *** learning has been recognized as the most promising technology for pharmaceuticals,a powerful molecule pre-trained model that could economize researchers’tons of *** the strategic application of AI capabilities to the drug discovery field,we pre-trained a model called PanGu Drug Model with 1.7 billion small molecules from ZINC20 (Irwin et al.,2020),DrugSpaceX(Yang et al.,2021),and UniChem (Chambers et al.,2013).

关键词： fir trained strategic

交易费用与出租汽车政府规制模式选择--基于Q市个案的分析

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甘肃行政学院学报 2020年第1期 114-124,M0006页

作者：郑华良赖诗攀中山大学政治与公共事务管理学院广州510275 华侨大学政治与公共管理学院福建泉州362000

作为共享经济在出租汽车领域的代表,网约车给人们带来了极大的便利,也给传统的政府规制模式带来了挑战。本文以Q市出租汽车规制为个案,剖析出租汽车政府规制不同模式的差异及其内在机制。基于规制的标准制定、控制机制及执法方式等要素... 详细信息

作为共享经济在出租汽车领域的代表,网约车给人们带来了极大的便利,也给传统的政府规制模式带来了挑战。本文以Q市出租汽车规制为个案,剖析出租汽车政府规制不同模式的差异及其内在机制。基于规制的标准制定、控制机制及执法方式等要素上的差异,本文将Q市巡游车与网约车规制分别概括为科层规制与合作规制模式。通过对规制空间中不同行动者的交易费用分析,研究发现Q市传统巡游车规制存在高昂的市场型与管理型交易费用,所以采用科层规制模式;而面对新业态的网约车规制,政府对共享经济的倡导降低了政治型交易费用,信息技术的充分应用减少了市场型与管理型交易费用,因此选择了合作规制模式。但随之产生的政府与平台公司之间高昂的管理型交易费用,是出租汽车政府规制实践中需要重点关注的内容。

关键词：政府规制规制要素科层规制合作规制交易费用出租汽车

Wide field-of-view metalens: a tutorial

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Advanced Photonics 2023年第3期5卷 1-21页

作者： Fan Yang Mikhail YShalaginov Hung-I Lin Sensong An Anu Agarwal hualiang Zhang Clara Rivero-Baleine Tian Gu Juejun Hu Massachusetts Institute of Technology Department of Materials Science and EngineeringCambridgeMassachusettsUnited States University of Massachusetts Lowell Department of Electrical and Computer EngineeringLowellMassachusettsUnited States Lockheed Martin Corporation OrlandoFloridaUnited States Massachusetts Institute of Technology Materials Research LaboratoryCambridgeMassachusettsUnited States

Wide field-of-view(FOV)optics are essential components in many optical systems,with applications spanning imaging,display,sensing,and beam *** refractive wide FOV optics often involve multiple stacked lenses,resulting in large size and weight as well as high *** lenses or metalenses promise a viable solution to realizing wide FOV optics without complex lens *** review the various architectures of wide FOV metalenses,elucidate their fundamental operating principles and design trade-offs,and quantitatively evaluate and contrast their imaging *** applications enabled by wide FOV metasurface optics are also discussed.

关键词： metasurface lens imaging field of view aberration