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新型Bcl-2小分子抑制剂的设计、合成与初步活性评价

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沈阳药科大学学报 2024年第7期41卷 889-899,913页

作者：王宇璇杨灿苏明波池岛乔白海云沈阳药科大学无涯创新学院辽宁沈阳110016 长三角高等研究院江苏南通226133 百极弘烨(南通)医药科技有限公司江苏南通226000

目的设计并合成一系列新型Bcl-2小分子抑制剂,测试其对Bcl-2和Bcl-2 G101V(Bcl-2突变体)与BH3-only蛋白相互作用的抑制活性,初步探究其构效关系,为后续相关研究提供参考。方法以临床化合物BGB-11417为先导化合物,通过骨架跃迁等方法,设... 详细信息

目的设计并合成一系列新型Bcl-2小分子抑制剂,测试其对Bcl-2和Bcl-2 G101V(Bcl-2突变体)与BH3-only蛋白相互作用的抑制活性,初步探究其构效关系,为后续相关研究提供参考。方法以临床化合物BGB-11417为先导化合物,通过骨架跃迁等方法,设计新型含螺环结构的Bcl-2小分子抑制剂。以苯甲醛为原料,通过取代、环化和偶联等反应合成目标化合物,并通过1H NMR和LC-MS进行结构确定。采用时间分辨荧光共振能量转移(TR-FRET)评价目标化合物对Bcl-2和Bcl-2 G101V(Bcl-2突变体)与BH3-only蛋白相互作用的抑制能力。结果共合成8个新型螺环Bcl-2小分子抑制剂,其中29a[IC_(50)(Bcl-2):0.8 nmol·L^(-1),IC_(50)(Bcl-2 G101V):55.41 nmol·L^(-1)],29d[IC_(50)(Bcl-2):0.27 nmol·L^(-1),IC_(50)(Bcl-2 G101V):18.65 nmol·L^(-1)]对Bcl-2和Bcl-2 G101V与BH3-only蛋白的相互作用有较好的抑制活性。结论建立了一种新型螺环Bcl-2小分子抑制剂合成方法,发现了对Bcl-2和Bcl-2 G101V(Bcl-2突变体)与BH3-only蛋白相互作用有较好抑制活性的新化合物,其中29d具有进一步研究的价值。

关键词：细胞凋亡 Bcl-2 家族 Bcl-2 突变蛋白小分子抑制剂分子对接

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Real-Time 3D Ultrasound Imaging System Based on a Hybrid Reconstruction Algorithm

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Chinese Journal of Electronics 2024年第1期33卷 245-255页

作者： Yifei LYU Yu SHEN mingbo ZHANG Junchen WANG School of Mechanical Engineering and Automation Beihang University The First Medical Center General Hospital of Chinese PLA

As a safe and convenient imaging technology in clinical routine diagnosis, ultrasound imaging can provide real-time 2D images of internal tissues and organs. To realize real-time 3D image reconstruction, pixel nearest neighbor interpolation(PNN) reconstruction algorithm and Bezier interpolation algorithm are combined into a hybrid reconstruction algorithm. On this basis, a real-time interactive 3D ultrasound imaging system is *** temporal calibration and spatial calibration, the six degrees of freedom poses of 2D ultrasound images can be accurately collected. The 3D volume reconstructed by the proposed 3D reconstruction algorithm is visualized by volume rendering. A multi-thread software system allows parallel operation of data acquisition, 3D reconstruction,volume visualization and other functions. 3D imaging experiments on a 3D printing femur model, a neck phantom and the neck of human volunteers were performed for systematic evaluation. When the reconstruction voxel size was set to be(0.53 mm3, 1.03 mm3, 1.53 mm3), the reconstruction errors of the femur and trachea model were respectively(0.23 mm, 0.31 mm, 0.56 mm) and(0.62 mm, 0.88 mm, 1.41 mm). Clinical feasibility was demonstrated by application of the 3D ultrasound imaging on the neck of human volunteers.

关键词： Interpolation Three-dimensional displays Ultrasonic imaging Imaging Data visualization Reconstruction algorithms Real-time systems

An Elite-Class Teaching-Learning-Based Optimization for Reentrant Hybrid Flow Shop Scheduling with Bottleneck Stage

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Computers, Materials & Continua 2024年第4期79卷 47-63页

作者： Deming Lei surui Duan mingbo Li Jing Wang College of Automation Wuhan University of TechnologyWuhan430070China

Bottleneck stage and reentrance often exist in real-life manufacturing processes;however,the previous research rarely addresses these two processing conditions in a scheduling *** this study,a reentrant hybrid flow shop scheduling problem(RHFSP)with a bottleneck stage is considered,and an elite-class teaching-learning-based optimization(ETLBO)algorithm is proposed to minimize maximum completion *** produce high-quality solutions,teachers are divided into formal ones and substitute ones,and multiple classes are *** teacher phase is composed of teacher competition and teacher *** learner phase is replaced with a reinforcement search of the elite *** adjustment on teachers and classes is established based on class quality,which is determined by the number of elite solutions in *** experimental results demonstrate the effectiveness of new strategies,and ETLBO has a significant advantage in solving the considered RHFSP.

关键词： Hybrid flow shop scheduling reentrant bottleneck stage teaching-learning-based optimization

Experimental Study of Emilia Sonchifolia Combined with Coptidis Rhizoma for the Prevention and Treatment of Oral Ulcer

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Open Journal of Stomatology 2023年第8期13卷 233-242页

作者： Qiaomei Deng Chunying Wei Jieling Luo Xiaowei Wen mingbo su Zhuofei Ma School of Stomatology Youjiang Medical University for Nationalities Baise China Graduate School Guangxi University of Chinese Medicine Nanning China

Objective: This paper aims to investigate the therapeutic effect of the combination of Emilia Sonchifolia and Coptidis Rhizoma on oral ulcer rats. Methods: 36 SD rats of half male and half female were kept for 7 days, and 6 rats among them were selected as normal group by random sampling method, and the rest rats were randomly divided into model group, positive control group, Emilia Sonchifolia group, Coptidis Rhizoma group and combined group after the establishment of oral ulcer model. The normal group and model group were given blank film, the positive control group was given Guilin Watermelon Frost, and the Emilia Sonchifolia group, Coptidis Rhizoma group and combined group were given the corresponding oral film, which was administered to the ulcer for 7 days continuously, 2 times per day. The healing of oral ulcer was assessed at the end of the last day of administration, and the ulcer area was calculated on the 1st, 3rd, 5th and 7th days after successful modeling, and the serum levels of IL-2 and TNF-α in rats were detected by Emilia Sonchifolia. Results: The grading of ulcer healing in the positive control group and the combined group was better than the other groups, and the difference was statistically significant when compared with the model group (p Coptidis Rhizoma group, Emilia Sonchifolia group, combined group and positive control group was smaller than that in the model group, and the difference was statistically significant (p Emilia Sonchifolia group, Coptidis Rhizoma group and combined group were all effective in reducing the area of oral ulcer, among which the combined group was more effective. The level of pro-inflammatory factor TNF-α was reduced and the level of anti-inflammatory factor IL-2 was increased in the Emilia Sonchifolia group, Coptidis Rhizoma group and combined group, and the difference was statistically significant (p Conclusion: The combination of Coptidis Rhizoma and Emilia Sonchifolia is effective in the treatment of oral ulcer i

关键词： Emilia Sonchifolia Coptidis Rhizoma Oral Ulcer IL-2 TNF-α

Identification of the Worst-case Static Voltage Stability Margin Interval of AC/DC Power System Considering Uncertainty of Renewables

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CSEE Journal of Power and Energy Systems 2024年第3期10卷 974-987页

作者： Wanbin Liu Shunjiang Lin Yuerong Yang mingbo Liu Qifeng Li School of Electric Power Engineering South China University of TechnologyGuangzhou 510640China Guangdong Key Laboratory of Clean Energy Technology South China University of TechnologyGuangzhou 511458China Department of Electrical and Computer Engineering University of Central FloridaOrlandoFL 32816USA CSEE IEEE

Calculation of static voltage stability margin(SVSM)of AC/DC power systems with lots of renewable energy sources(RESs)integration requires consideration of uncertain load growth and renewable energy generation *** paper presents a bi-level optimal power flow(BLOPF)model to identify the worst-case SVSM of an AC/DC power system with line commutation converter-based HVDC and multi-terminal voltage sourced converter-based HVDC transmission *** of uncertain load growth’s hypercone model and control mode switching of DC converter stations are considered in the BLOPF ***,uncertain RES output fluctuations are described as intervals,and two three-level optimal power flow(TLOPF)models are established to identify interval bounds of the system worst-case *** two TLOPF models are both transformed into max–min bi-level optimization models according to independent characteristics of different uncertain ***,transforming the inner level model into its dual form,max–min BLOPF models are simplified to single-level optimization models for direct *** results on the modified IEEE-39 bus AC/DC case and an actual large-scale AC/DC case in China indicate correctness and efficiency of the proposed identification method.

关键词： AC/DC power system control mode switching convex relaxation dual programming multi-level optimization optimal power flow static voltage stability margin

Efficacy and safety of low-dose cyclophosphamide combined with lenvatinib, pembrolizumab and TACE for unresectable hepatocellular carcinoma:A single-center, prospective,single-arm clinical trial

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Chinese Journal of Cancer Research 2024年第2期36卷 114-123页

作者： Yupeng Ren Yuxuan Li mingbo Cao Yongchang Tang Feng Yuan Gaoyuan Yang Zhiwei He Zheng Shi Xiaorui su Zhicheng Yao Meihai Deng Department of Hepatobiliary surgery the Third Affiliated HospitalSun Yat-sen UniversityGuangzhou 510630China Department of General surgery Qilu HospitalShandong UniversityJinan 250012China Department of Hepatobiliary surgery the First Affiliated Hospital of Guangzhou Medical UniversityGuangzhou 510120China Department of Hepatobiliary and Pancreatic surgery the Third Affiliated HospitalSun Yat-sen UniversityGuangzhou 510630China

Objective: Unresectable hepatocellular carcinoma(uHCC) continues to pose effective treatment options. The objective of this study was to assess the efficacy and safety of combining low-dose cyclophosphamide with lenvatinib, pembrolizumab and transarterial chemoembolization(TACE) for the treatment of ***: From February 2022 to November 2023, a total of 40 patients diagnosed with uHCC were enrolled in this small-dose, single-center, single-arm, prospective study. They received a combined treatment of low-dose cyclophosphamide with lenvatinib, pembrolizumab, and TACE. Study endpoints included progression-free survival(PFS), objective response rate(ORR), and safety assessment. Tumor response was assessed using the modified Response Evaluation Criteria in Solid Tumors(mRECIST), while survival analysis was conducted through KaplanMeier curve analysis for overall survival(OS) and PFS. Adverse events(AEs) were evaluated according to the National Cancer Institute Common Terminology Criteria for Adverse Events(version 5.0).Results: A total of 34 patients were included in the study. The median follow-up duration was 11.2 [95% confidence interval(95% CI), 5.3-14.6] months, and the median PFS(mPFS) was 15.5(95% CI, 5.4-NA) *** OS(mOS) was not attained during the study period. The ORR was 55.9%, and the disease control rate(DCR) was 70.6%. AEs were reported in 27(79.4%) patients. The most frequently reported AEs(with an incidence rate >10%) included abnormal liver function(52.9%), abdominal pain(44.1%), abdominal distension and constipation(29.4%), hypertension(20.6%), leukopenia(17.6%), constipation(17.6%), ascites(14.7%), and insomnia(14.7%). Abnormal liver function(14.7%) had the most common grade 3 or higher ***: A combination of low-dose cyclophosphamide with lenvatinib, pembrolizumab, and TACE is safe and effective for u HCC, showcasing a promising therapeutic strategy for managing uHCC.

关键词： Hepatocellular carcinoma lenvatinib low-dose cyclophosphamide pembrolizumab transarterial chemoembolization

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Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors

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Chinese Journal of Chemistry 2021年第1期39卷 115-120页

作者： Na Luo Xiaoyu Fang mingbo su Xinwen Zhang Dan Li Honglin Li Shiliang Li Zhenjiang Zhao Shanghai Key Laboratory of New Drug Design School of PharmacyEast China University of Science and Technology130 Meilong RoadShanghai 200237China State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences555 Zhuchongzhi RoadShanghai 201203China Shandong Biopolar Dichang Pharmaceutical Co. LtdRM2306No.786 Linzi AvenueZiboShandong 255400China

Dipeptidyl peptidase 4(DPP-4)is a clinically validated target for the treatment of type 2 diabetes mellitus(T2DM).To discover novel and potent DPP-4 inhibitors,three series of compounds were designed and synthesized in this study based on our previously identified novel scaffold of 2-phenyl-3,4-dihydro-2H-benzo[f]*** the designed compounds,41d-1 was the most po tent one with an IC_(50) value of 16.00 nM.

关键词： TypeⅡdiabetes Dipeptidyl peptidaseⅣ Inhibitors Molecular docking Structure-activity relationship

P2P Energy Trading Considering Prosumer Preference and System Risk

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CSEE Journal of Power and Energy Systems 2024年第3期10卷 1179-1194页

作者： Xinyu He Ping Dong mingbo Liu Xuewei Huang Wenli Deng Ruijin He School of Electric Power Engineering South China University of TechnologyGuangzhou 510640China IEEE

As an important means of mobilizing demand-side resources,peer-to-peer(P2P)energy trading has drawn more and more attention from *** paper constructs a P2P energy trading framework considering prosumers’trading partner preferences(TPPs)and system *** first,we build the P2P trading models of prosumers equipped with different distributed energy resources(DERs),and TPP ***,to solve the established energy trading problem,a fully distributed double-consensus alternating direction method of multipliers(DC-ADMM)is proposed,which can achieve transaction consensus when considering market players’***,a risk-based security constrained economic dispatch(RBSCED)model based on AC power flow is established for the first time,by which a distribution system operator(DSO)checks system security and obtains risk-based locational marginal prices(RLMPs).Moreover,double-regulated price signals related to RLMPs which contain grid utilization prices(GUPs)and DSO’s retail prices realize management of players’*** the end,the proposed method is applied to an IEEE33 bus distribution *** show the proposed method effectively reduces system risk and ensures secure operation of system without direct management.

关键词： Double-consensus ADMM grid utilization price price signal risk-based locational marginal price trading partner preference

Drag reduction characteristics of recirculation flow at rocket base in an RBCC engine under ramjet/scramjet mode

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Chinese Journal of Aeronautics 2024年第3期37卷 104-115页

作者： Menglei LI mingbo suN Peibo LI Daoning YANG Bin AN Yizhi YAO Jikai CHEN Taiyu WANG Jiaoru WANG Hypersonic Technology Laboratory National University of Defense TechnologyChangsha 410073China Department of Aerospace Science and Technology Space Engineering UniversityBeijing 101416China

To reduce the drag generated by the recirculation flow at the rocket base in a RocketBased Combined Cycle(RBCC)engine operating in the ramjet/scramjet mode,a novel annular rocket RBCC engine based on a central plug cone was *** performance loss mechanism caused by the recirculation flow at the rocket base and the influence of the plug cone configuration on the thrust performance were *** indicated that the recirculation flow at the rocket base extended through the entire combustor,which creates an extensive range of the"low-kineticenergy zone"at the center and leads to an engine thrust *** plug cone serving as a surface structure had a restrictive effect on the internal flow of the engine,making it smoothly transit at the position of the large separation *** model RBCC engine could achieve a maximum thrust augmentation of 37.6%with a long plug cone that was twice diameter of the inner ***,a shorter plug cone that was half diameter of the inner isolator proved less effective at reducing the recirculation flow for a supersonic flow and induced an undesirable flow fraction that diminished the thrust ***,the effectiveness of the plug cone increased with the flight Mach number,indicating that it could further broaden the operating speed range of the scramjet mode.

关键词： Rocket-based combined cycle Ramjet/scramjet mode Plug cone Drag reduction k-x SST turbulent model

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