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| 1 | Structural basis of anti-PD-L1 monoclonal antibody avelumab for tumor therapy显示文摘 | Kefang Liu ShuguangTan Yan Chai Danqing Chen Hao Song Catherine Wei-Hong Zhang yi Shi Jun Liu Wenjie Tan Jianxin Lyu Shah Gao Jinghua Yan Jianxun Qi George F Gao | 2017 | Cell Research2017，27，1： | 11 |
| 2 | Crystal clear: visualizing the intervention mechanism of the PD-1/PD-L1 interaction by two cancer therapeutic monoclonal antibodies显示文摘基于抗体的 PD-1/PD-L1 封锁治疗为癌症在免疫疗法拿了中心舞台,与多重临床的成功。发信号的 PD-1 在肿瘤驱动的 T 房间机能障碍起枢轴的作用。与优先的途径相对照产生或增加肿瘤特定的 T 房间回答,基于抗体的 PD-1/PD-L1 封锁指向导致肿瘤的 T 房间缺点并且恢复先存在调制 antitumor 免疫的 T 房间功能。在这评论,表达式规定和 PD-1 的禁止的函数和基于抗体的 PD-1/PD-L1 封锁治疗的现在的理解上的基本知识简短被总结。我们然后有关 PD-1/PD-Ls 相互作用的结构的基础集中于最近的突破工作并且怎么指向 PD-L1 的治疗学的抗体, pembrolizumab 指向 PD-1 和 avelumab,与 PD-1/PD-L1 的绑定竞争打断 PD-1/PD-L1 相互作用。我们相信这个结构的信息将有益于指向 PD-1 发信号的治疗学的抗体的设计和改进。 | ShuguangTan Danqing Chen Kefang Liu Mengnan He Hao Song Yi Shi Jun Liu Catherine W.-H. Zhang Jianxun Qi Jinghua Yan Shan Gao George F. Gao | 2016 | Protein & Cell2016，7，12： | 8 |
| 3 | A new strategy to iteratively update scalable universal quantitative models for the testing of azithromycin by near infrared spectroscopy显示文摘The training set of a universal near infrared (NIR) model for quantitative analysis of a drug should cover as many samples of this drug in the market as possible. Inevitably the model may fail for new products that have different excipients and production processes. In such circumstances the model should be updated. We here propose a new strategy to iteratively update a universal NIR quantitative model for azithromycin. We prove that universal quantitative models generated from this new strategy are comparably effective for azithromycin injection powders and azithromycin tablets, compared to the strategy using hierarchical clustering method which we reported previously. Furthermore, we establish the correlation coefficient r between a new sample and the training set samples can be used to decide whether or not the model should be updated. | ZOU WenBo FENG YanChun DONG JiXiong SONG DanQing HU ChangQin | 2013 | Science China Chemistry2013，56，4： | 5 |
| 4 | Synthesis and biological evaluation of 12-N-p-chlorobenzyl sophoridinol derivatives as a novel family of anticancer agents显示文摘Taking 12-N-p-chlorobenzyl sophoridinol 2 as a lead, a series of novel sophoridinic derivatives with various 30-substituents at the 11–side chain were synthesized and evaluated for their anticancer activity from sophoridine(1), a natural antitumor medicine. Among them, the sophoridinic ketones 5a–b, alkenes 7a–b and sophoridinic amines 14a–b displayed reasonable antiproliferative activity with IC50 values ranging from 3.8 to 5.4 μmol/L. Especially, compounds 5a and 7b exhibited an equipotency in both adriamycin(AMD)-susceptible and resistant MCF-7 breast carcinoma cells,indicating a different mechanism from AMD. The primary mechanism of action of 5a was to arrest the cell cycle at the G0/G1 phase, consistent with that of parent compound 1. Thus, we consider 12-chlorobenzyl sophoridinic derivatives with a tricyclic scaffold to be a new class of promising antitumor agents with an advantage of inhibiting drug-resistant cancer cells. | Chongwen Bi Cheng Ye Yinghong Li Wuli Zhao Rongguang Shao Danqing Song | 2016 | Acta Pharmaceutica Sinica B2016，6，3： | 4 |
| 5 | Synthesis and biological evaluation of 8-substituted berberine derivatives as novel anti-mycobacterial agents显示文摘Tuberculosis(TB)is a disease which kills two million people every year and infects over one-third of the world's population.Eighteen new 8-substituted berberine derivatives were synthesized and evaluated for their anti-mycobacterial activities against M ycobacterium tuberculosis(M.tuberculosis)strain H_(37)Rv.Among these compounds,compound 6i was the most effective antitubercular agent with an MIC of 1.0μg/mL.Most importantly,compound 6i also exhibited a potent effect against clinically isolated rifampicin-and isoniazid-resistant M.tuberculosis strains,suggesting a different mode of action from the current drugs.Therefore,it shows potential for the development of new anti-TB agents. | Yanxiang Wang Haigen Fu Yinghong Li Jiandong Jiang Danqing Song | 2012 | Acta Pharmaceutica Sinica B2012，2，6： | 4 |
| 6 | Synthesis and biological evaluation of sophocarpinic acid derivatives as anti-HCV agents显示文摘Chronic hepatitis C virus(HCV)infection has become a major public health burden worldwide.Twenty-two sophocarpinic acid or matrine derivatives were synthesized and their anti-HCV activities were evaluated in vitro.The structure-activity analysis revealed that(i)sophocarpinic acids with a D-seco 3-ring structure scaffold were more favorable than matrines with a 4-ring scaffold;(ii)the introduction of an electron-withdrawing group on the phenyl ring in 12-N-benzenesulfonylΔβγsophocarpinic acids was beneficial for the antiviral activity against HCV.Among them,compounds 9h and 9j exhibited the most potent inhibitory activities on HCV replication with selectivity indies of 70.3 and 30.9,respectively.Therefore,both were selected as antiviral candidates for further investigation. | Yinghong Li Zonggen Peng Limei Gao Danqing Song | 2014 | Acta Pharmaceutica Sinica B2014，4，4： | 4 |
| 7 | Synthesis and biological evaluation of new 13-n-nonylprotoberberine derivatives as antitubercular agents显示文摘Tuberculosis is a serious threat to public health throughout the world.A series of new l3-n-nonylprotoberberine derivatives was designed,synthesized and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis strain H_(37)Rv.Several compounds(2,11a-c,11g,13d,15c)exhibited excellent anti-tubercular activity with an MIC below 1.0μg/mL.Notably,compound 13d showed potential antibacterial effect against both drug-susceptible and multidrug-resistant(MDR)M.tuberculosis with MIC ranges of 0.0625-1.0μg/mL.These results suggest a mode of action different from that of the current anti-mycobacterial drugs rifampicin and isoniazid.Hence,compound 13d is an attractive lead compound for the development of new antitubercular agents. | Yinghong Li Yanxin Liu Yanxiang Wang Sheng Tang Danqing Song | 2013 | Acta Pharmaceutica Sinica B2013，3，1： | 3 |
| 8 | Synthesis and biological evaluation of novel tricyclic matrinic derivatives as potential anti-filovirus agents显示文摘Twenty-six novel tricyclic sophoridinic and matrinic derivatives containing a common chlorinated benzene fragment were designed, synthesized and evaluated for their anti-ebolavirus(EBOV)activities. Structure–activity relationship analysis indicated:(i) 12 N-dichlorobenzyl motif was beneficial for the activity;(ii) the chiral configuration at C5 atom might not affect the activity much. Among the target compounds, compound 7d exhibited the most potent potency against EBOV with an IC_(50) value of 5.29 μmol/L and an SI value of over 37.8. Further in vivo anti-EBOV assay of 7d identified its high effectiveness, and in vivo anti-MARV assay of 7d suggested its inspiring broad-spectrum anti-filovirus activity. The results provided powerful information on further strategic optimization and development of this kind of compounds against filoviruses. | Xin Zhang Qiang Liu Qianqian Li Yinghong Li Zhandong Liu Hongbin Deng Sheng Tang Yanxiang Wang Youchun Wang Danqing Song | 2018 | Acta Pharmaceutica Sinica B2018，8，4： | 2 |
| 9 | Discovery and identification of EIF2AK2 as a direct key target of berberine for anti-inflammatory effects显示文摘Using chemoproteomic techniques,we first identified EIF2AK2,eEF1A1,PRDX3 and VPS4B as direct targets of berberine(BBR)for its synergistically anti-inflammatory effects.Of them,BBR has the strongest affinity with EIF2AK2 via two ionic bonds,and regulates several key inflammatory pathways through EIF2AK2,indicating the dominant role of EIF2AK2.Also,BBR could subtly inhibit the dimerization of EIF2AK2,rather than its enzyme activity,to selectively modulate its downstream pathways including JNK,NF-κB,AKT and NLRP3,with an advantage of good safety profile.In EIF2AK2 gene knockdown mice,the inhibitory IL-1β,IL-6,IL-18 and TNF-a secretion of BBR was obviously attenuated,confirming an EIF2AK2-dependent anti-inflammatory efficacy.The results highlight the BBR's network mechanism on anti-inflammatory effects in which EIF2AK2 is a key target,and inhibition of EIF2AK2 dimerization has a potential to be a therapeutic strategy against inflammationrelated disorders. | Wei Wei Qingxuan Zeng Yan Wang Xixi Guo Tianyun Fan Yinghong Li Hongbin Deng Liping Zhao Xintong Zhang Yonghua Liu Yulong Shi Jingyang Zhu Xican Ma Yanxiang Wang Jiandong Jiang Danqing Song | 2023 | Acta Pharmaceutica Sinica B2023，13，5： | 2 |
| 10 | Berberine reduces insulin resistance through protein kinase C-dependent up-regulation of insulin receptor expression 显示文摘 | KONG Weijia ZHANG Hao SONG Danqing | 2009 | Metabolism Clinical and Experimental2009，58，： | 1 |
| 11 | The Mycoplasma gallisepticum α-enolase is cell surface-exposed and mediates adherence by binding to chicken plasminogen显示文摘 | Hongjun Chen Shengqing Yu Xinyue Shen Danqing Chen Xvsheng Qiu Cuiping Song Chan Ding | 2011 | Microbial Pathogenesis2011，，： | 1 |
| 12 | Construction of a universal quantitative model for the determination of azithro- mycin in granules using near-infrared diffuse reflectance spectros- copy 显示文摘 | Zou Wenbo Feng Yanchun Song Danqing | 2012 | Joumal of Chinese Pharmaceutical Sciences2012，21，005： | 1 |
| 13 | BrΦnsted acid-promoted ‘on-water’ C(sp^3)-H functionalization fot the synthesis of isoindolinone/[1,2,4]triazolo[1,5-a]pyrimidine derivatives targeting the SKP2-CKS1 interaction显示文摘The isoindolinone and biaryl scaffolds are prevalent in natural products and drug molecules,which have showed broad and interesting biological activities.The efficient construction of such hybridized molecules and biological evaluation are of great interest to medicinal chemistry community.In this communication,we report an efficient BrΦnsted acid-promoted C(sp^3)-H functionalization approach that enables the rapid construction of biologically important isoindolinone/[1,2,4]triazolo[1,5-a]pyrimidine hybrids from 5-methyl-7-(2,4,6-trimethoxyphenyl)-[1,2,4]triazolo[1,5-a]pyrimidine,2-formylbenzoic acid and various anilines.The title compounds were generated in high to excellent yields(up to 96%)regardless of the electronic nature and steric effects of the substituents.In this reaction,an isoindolinone scaffold,one C-C single bond,and two C-N bonds were formed simultaneously with high atom economy.In this work,we have envisioned that the methyl group linked to the electron-deficient Nheterocycles could be used as a new synthetic handle for late-state diversification and may have broad applications in the field of organic and medicinal chemistry.Besides,the title compounds have exhibited promising activity against the SKP2-CKS1 interaction. | Shuo Yuan Sixi Wang Min Zhao Danqing Zhang Jinjie Chen Jian-Xin Li Jingya Zhang Yihui Song Jinyi Wang Bin Yu Hongmin Liu | 2020 | Chinese Chemical Letters2020，31，2： | 1 |
| 14 | Laboratory-scale investigation of response characteristics of liquid-filled rock joints with different joint inclinations under dynamic loading显示文摘In underground rock engineering,water-bearing faults may be subjected to dynamic loading,resulting in the coupling of hydraulic and dynamic hazards.Understanding the interaction mechanism between the stress waves induced by dynamic loadings and liquid-filled rock joints is therefore crucial.In this study,an auxiliary device for simulating the liquid-filled layer was developed to analyze the dynamic response characteristics of liquid-filled rock joints in laboratory.Granite and polymethyl methacrylate(PMMA)specimens were chosen for testing,and high-amplitude shock waves induced by a split Hopkinson pressure bar(SHPB)were used to produce dynamic loadings.Impact loading tests were conducted on liquid-filled rock joints with different joint inclinations.The energy propagation coefficient and peak liquid pressure were proposed to investigate the energy propagation and attenuation of waves propagating across the joints,as well as the dynamic response characteristics of the liquid in the liquid-filled rock joints.For the inclination angle range considered herein,the experimental results showed that the energy propagation coefficient gently diminished with increasing joint inclination,and smaller coefficient values were obtained for granite specimens compared with PMMA specimens.The peak liquid pressure exhibited a gradually decreasing trend with increasing joint inclination,and the peak pressure for granite specimens was slightly higher than that for PMMA specimens.Overall,this paper may provide a considerably better method for studying liquid-filled rock joints at the laboratory scale,and serves as a guide for interpreting the underlying mechanisms for interactions between stress waves and liquid-filled rock joints. | Jin Huang Xiaoli Liu Danqing Song Jian Zhao Enzhi Wang Jianmin Zhang | 2022 | Journal of Rock Mechanics and Geotechnical Engineering2022，14，2： | 1 |
| 15 | Ultrasound-responsive matters for biomedical applications显示文摘Ultrasound(US)is a biofavorable mechanical wave that has shown practical significance in biomedical fields.Due to the cavitation effect,sonoluminescence,sonoporation,pyrolysis,and other biophysical and chemical effects,a wide range of matters have been elucidated to be responsive to the stimulus of US.This review addresses and discusses current developments in US-responsive matters,including US-breakable intermolecular conjugations,US-catalytic sonosensitizers,fluorocarbon compounds,microbubbles,and US-propelled micro-and nanorobots.Meanwhile,the interactions between US and advanced matters create various biochemical products and enhanced mechanical effects,leading to the exploration of potential biomedical applications,from US-facilitated biosensing and diagnostic imaging to US-induced therapeutic applications and clinical translations.Finally,the current challenges are summarized and future perspectives on US-responsive matters in biomedical applications and clinical translations are proposed. | Danqing Huang Jinglin Wang Chuanhui Song Yuanjin Zhao | 2023 | The Innovation2023，4，3： | 0 |
| 16 | Author correction to‘Discovery and identification of EIF2AK2 as a direct key target of berberine for anti-inflammatory effects’[Acta Pharmaceutica Sinica B 13(2023)2138-2151]显示文摘The authors regret that there are some misplaced figure numbers in the body of this article due to negligence in the layout and proofreading of the figures.Although it does not affect the conclusion,it is an obvious error.The authors have now modified as below.The authors apologize for any inconvenience caused to the journal and readers. | Wei Wei Qingxuan Zeng Yan Wang Xixi Guo Tianyun Fan Yinghong Li Hongbin Deng Liping Zhao Xintong Zhang Yonghua Liu Yulong Shi Jingyang Zhu Xican Ma Yanxiang Wang Jiandong Jiang Danqing Song | 2024 | Acta Pharmaceutica Sinica B2024，14，3： | 0 |
| 17 | An extended analysis of cardiovascular benefits of indoor air filtration intervention among elderly:a randomized crossover trial(Beijing indoor air purifier study,BIAPSY)显示文摘Objective Evidence on potential cardiovascular benefits of personal-level intervention among the elderly exposed to high levels of particulate matter(PM)remains limited.We aimed to assess improvements in surrogate markers of cardiovascular injury in vulnerable populations at risks by using indoor air filtration units.Methods We conducted a randomized crossover trial for 2 separate 2-week air filtration interventions in 20 households of patients with stable chronic obstructive pulmonary disease and their partners in the winter of 2013,with concurrent measurements of indoor PM.The changes in biomarkers indicative of cardiac injury,atherosclerosis progression and systemic inflammation following intervention were evaluated using linear mixed-effect models.Results In the analysis,average levels of indoor PM with aerodynamic diameters<2.5µm(PM2.5)decreased significantly by 59.2%(from 59.6 to 24.3µg/m3,P<0.001)during the active air filtration.The reduction was accompanied by improvements in levels of high-sensitivity cardiac troponin I by−84.6%(95%confidence interval[CI]:−90.7 to−78.6),growth differentiation factor-15 by−48.1%(95%CI:−31.2 to−25.6),osteoprotegerin by−65.4%(95%CI:−56.5 to−18.7),interleukin-4 by−46.6%(95%CI:−62.3 to−31.0)and myeloperoxidase by−60.3%(95%CI:−83.7 to−3.0),respectively.Conclusion Indoor air filtration intervention may provide potential cardiovascular benefits in vulnerable populations at risks. | Jie Chen Tong Wang Hongbing Xu Yutong Zhu Yipeng Du Beibei Liu Qian Zhao Yi Zhang Lingyan Liu Ningman Yuan Jiakun Fang Yunfei Xie Shuo Liu Rongshan Wu Danqing Shao Xiaoming Song Bei He Bert Brunekreef Wei Huang | 2022 | Global Health Journal2022，6，1： | 0 |
| 18 | Evolution and development of potent monobactam sulfonate candidate IMBZ18g as a dual inhibitor against MDR Gram-negative bacteria producing ESBLs显示文摘A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria.Compound 33a(IMBZ18G)is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant(MDR)Gram-negative strains,with a highly druglike nature.The checkerboard assay reveals its significant synergistic effect withβ-lactamase inhibitor avibactam,and the MIC values against MDR enterobacteria were reduced up to 4—512folds.X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and Cβ-lactamases.Accordingly,preclinical studies of 33a alone and 33a-avibactam combination as potential innovative candidates are actively going on,in the treatment ofβ-lactamase-producing MDR Gram-negative bacterial infections. | Zhiwen Li Zhihao Guo Xi Lu Xican Ma Xiukun Wang Rui Zhang Xinxin Hu Yanxiang Wang Jing Pang Tianyun Fan Yonghua Liu Sheng Tang Haigen Fu Jingpu Zhang Yinghong Li Xuefu You Danqing Song | 2023 | Acta Pharmaceutica Sinica B2023，13，7： | 0 |
| 19 | Discovery and development of tricyclic matrinic derivatives as anti-diabetic candidates by AMPKαactivation显示文摘We found compound 12N-p-trifluoromethylbenzenesulfonyl matrinane(1)was a potent anti-diabetic agent.Thirty-five tricyclic matrinic derivatives were synthesized and determined for their stimulatory effects on glucose consumption in L6 myotubes,taking 1 as the lead.In high-fat diet(HFD)and STZ induced diabetic mice,9a significantly lowers blood glucose,improves glucose tolerance,and especially alleviates diabetic nephropathy and islet damage.Mechanism study indicates that 9a simultaneously targets mitochondrial complex I to increase AMP/ATP ratio,as well as liver kinase B1(LKB1)and calcium/calmodulindependent protein kinase(Ca MKK),which synergistically activates AMPKαand then stimulates glucose transporter 4(GLUT4)membrane translocation and 2-deoxyglucose(2-DG)uptake to exert anti-diabetic efficacy.Therefore,compound 9a with a novel structure is a promising anti-diabetic candidate with the advantage of multiple-target mechanism,worthy of further investigation. | Yinghong Li Yuanhui Zhang Tianyu Niu Yudong Pang Yulong Shi Qingxuan Zeng Jingpu Zhang Jingyang Zhu Xiuli Zhong Yanxiang Wang Yan Wang Sheng Tang Weijia Kong Danqing Song Jiandong Jiang | 2023 | Chinese Chemical Letters2023，34，1： | 0 |
| 20 | Modeling landslide susceptibility based on convolutional neural network coupling with metaheuristic optimization algorithms显示文摘Landslides are one of the most common geological hazards worldwide,especially in Sichuan Province(Southwest China).The current study's main,purposes are to explore the potential applications of convolutional neural networks(CNN)hybrid ensemble metaheuristic optimization algorithms,namely beluga whale optimization(BWO)and coati optimization algorithm(COA),for landslide susceptibility mapping in Sichuan Province(China).For this aim,fourteen landslide conditioning factors were compiled in a spatial database.The effectiveness of the conditioning factors in the development of the landslide predictive model was quantified using the linear support vector machine model.The receiver operating characteristic(ROC)curve(AUC),the root mean square error,and six statistical indices were used to test and compare the three resultant models.For the training dataset,the AUC values of the CNN-COA,CNN-BWO and CNN models were 0.946,0.937 and 0.855,respectively.In terms of the validation dataset,the CNN-COA model exhibited a higher AUC value of 0.919,while the AUC values of the CNN-BWO and CNN models were 0.906 and 0.805,respectively.The results indicate that the CNN-COA model,followed by the CNN-BWO model,and the CNN model,offers the best overall performance for landslide susceptibility analysis. | Zhuo Chen Danqing Song | 2023 | International Journal of Digital Earth2023，16，1： | 0 |
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