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Targeting SPOP with small molecules provides a novel strategy for kidney cancer therapy

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Science China(Life Sciences) 2017年第1期60卷 91-93页

作者： Tong Zheng cai-guang yang Laboratory of Chemical Biology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences Beijing 100049China

Renal cell carcinoma （RCC）, accounting for 4% of all can- cers, is the second most common cancer in urology. The most common form of RCC is clear cell RCC （ccRCC）, with a ratio over 70%. Early-phase kidney diseases usually show rare symptoms in clinic; unfortunately, most patients are di- agnosed with kidney cancer at the end stage, at which point the cancer is both resistant to chemotherapy and metastatic, thus leading to high mortality. Understanding cancer biology enables manipulation of disease targets by using small-mole- cule modulators, which eventually drive the development of novel therapeutic agents for ccRCC. In this insight, we would like to briefly outline several promising and revolutionizing targets and the target-based design of therapeutic agents for ccRCC.

关键词：小分子调节剂治疗药物肾细胞癌症肾脏疾病恶性肿瘤泌尿系统驱动技术

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Chemical Intervention on Staphylococcus aureus Virulence

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Chinese Journal of Chemistry 2019年第2期37卷 183-193页

作者： Lin-Lin Zhou cai-guang yang State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of the Chinese Academy of Sciences Beijing 100049China

Resistance to conventional antibiotics has raised worldwide attention. Notably, Methicillin-resistant Staphylococcus aureus (MRSA) has become one of the most life-threatening health concerns. Although effective against bacterial infections, conventional antibiotics have also showed a series of side effects such as gut microbiota imbalance.

关键词： Chemical Intervention Staphylococcus aureus Virulence

RNA Methylation m6A:A New Code and Drug Target?

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Chinese Journal of Chemistry 2020年第4期38卷 420-421页

作者： Gan-Qiang Lai Lin-Lin Zhou cai-guang yang State Key Laboratory of Drug Research Shanghai Institute of Materia MedicoChinese Academy of SciencesShanghai 201203China University of the Chinese Academy of Sciences Beijing 100049China

The m^6A-RNA modification is a dynamic and reversible process,which has emerged as a new RNA code for the regulation of gene *** functional network of methyltransferases(writers),demethylases(erasers),and binding proteins(readers)modulate the level of m^6A *** of RNA methylation has been associated with various fundamental biological processes and human ***,we briefly introduce an understanding-enabled manipulation on m^6A RNA modification with an emphasis on the use of small-molecule intervention.

关键词： expression. manipulation modification

Simulation study on cavity growth in ductile metal materials under dynamic loading

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Frontiers of physics 2013年第4期8卷 394-404页

作者： Ai-Guo Nu guang-cai Zhang yang-Jun Ying Xi-Jun Yu National Key Laboratory of Computational Physics Institute of Applied Physics and Computational Mathematics P. O. Box 8009-26 Beijing 100088 China

Cavity growth in ductile metal materials under dynamic loading is investigated via the material point method. Two typical cavity effects in the region subjected to rarefaction wave are identified：（i） part of material particles flow away from the cavity in comparison to the initial loading velocity, （ii） local regions show weaker negative or even positive pressures. Neighboring cavities interact via coalescence of isobaric contours. The growth of cavity under tension shows staged behaviors. After the initial slow stage, the volume and the dimensions in both the tensile and transverse directions show linear growth rate with time until the global tensile wave arrives at the upper free surface. It is interesting that the growth rate in the transverse direction is faster than that in the tensile direction. The volume growth rate linearly increases with the initial tensile velocity. After the global tensile wave passed the cavity, both the maximum particle velocity in the tensile direction and the maximum particle velocity in the opposite direction increase logarithmically with the initial tensile speed. The shock wave reflected back from the cavity and compression wave from the free surface induce the initial behavior of interracial instabilities such as the Richtmyer-Meshkov instability, which is mainly responsible for the irregularity in the morphology of deformed cavity. The local temperatures and distribution of hot spots are determined by the plastic work. Compared with the dynamical process, the heat conduction is much slower.

关键词： material point method cavity growth dynamic loading interracial instability

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Lattice Boltzmann model for combustion and detonation

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Frontiers of physics 2013年第1期8卷 94-110页

作者： Bo Yan Ai-Guo Xu guang-cai Zhang yang-Jun Ying Hua Li National Key Laboratory of Computational Physics Institute of Applied Physics and Co~putational Mathe'maties P. O. Box 8009-26 Beijing 100088 China

In this paper we present a lattice Boltzmann model for combustion and detonation. In this model the fluid behavior is described by a finite-difference lattice Boltzmann model by Gan et al. [Physica A, 2008, 387: 1721]. The chemical reaction is described by the Lee-Tarver model [Phys. Fluids, 1980, 23: 2362]. The reaction heat is naturally coupled with the flow behavior. Due to the separation of time scales in the chemical and thermodynamic processes, a key technique for a successful simulation is to use the operator-splitting scheme. The new model is verified and validated by well-known benchmark tests. As a specific application of the new model, we studied the simple steady detonation phenomenon. To show the merit of LB model over the traditional ones, we focus on the reaction zone to study the non-equilibrium effects. It is interesting to find that, at the von Neumann peak, the system is nearly in its thermodynamic equilibrium. At the two sides of the von Neumann peak, the system deviates from its equilibrium in opposite directions. In the front of von Neumann peak, due to the strong compression from the reaction product behind the von Neumann peak, the system experiences a sudden deviation from thermodynamic equilibrium. Behind the von Neumann peak, the release of chemical energy results in thermal expansion of the matter within the reaction zone, which drives the system to deviate the thermodynamic equilibrium in the opposite direction. From the deviation from thermodynamic equilibrium, Δ m *, defined in this paper, one can understand more on the macroscopic effects of the system due to the deviation from its thermodynamic equilibrium.

关键词： lattice Boltzmann method Lee-Tarver model viscous detonation deviation from equilibrium

Synthesis and Structure-Activity Relationships of Ring-Opened Bengamide Analogues against Methicillin-Resistant Staphylococcus aureus

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Chinese Journal of Chemistry 2021年第3期39卷 671-676页

作者： Chen-Xi Yu Bing-Yan Wei Xue-Qing Kong cai-guang yang Fa-Jun Nan State Key Laboratory of Drug Research the National Center for Drug ScreeningShanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China School of Pharmaceutical Science and Technology Hangzhou Institute for Advanced StudyUCASHangzhouZhejiang 310024China Yantai Key Laboratory of Nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaYantaiShandong 264000China

Main observation and conclusion Methicillin-resistant Staphylococcus aureus(MRSA)has become a major threat on public health because of the increase of clinically isolated strains that exhibit resistance to many ***,development of new antibiotics for the treatment of MRSA in-fection is a sustained *** have previously identified a ring-opened bengamide analogue L472-2 that displays moderate ac-tivity against the growth of *** our previous work,we started from L472-2 and identified a class of analogues containing al-kynyl groups which have the potential to activate SaCIpP activity but moderate antibacterial ***,we focused on the anti-bacterial activity of L472-2,and a novel series of ring-opened bengamide analogues were synthesized and their activities were evalu-ated against *** conducting a compact analysis of the structure-activity relationships(SAR)of these analogues,we found that an adamantane ethanol ester bengamide 2j showed excellent antibacterial activity towards six *** strains,including MRSA,while it does not activate ***,these bengamide analogues represent a new class of candidates that suppress MRSA via-bility..

关键词： Bengamides Staphylococcus aureus Antibiotics Structure-activity relationships Pharmacokinetic

Multi-omics for COVID-19:driving development of therapeutics and vaccines

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National Science Review 2023年第9期10卷 307-336页

作者： Mengyu Guo Muya Xiong Jinying Peng Tong Guan Haixia Su Yanyi Huang cai-guang yang yang Li Diana Boraschi Thanigaimalai Pillaiyar Guanbo Wang Chengqi Yi Yechun Xu Chunying Chen CAS Key Laboratory of Biomedical Effects of Nanomaterials and Nanosafety and CAS Center for Excellence in Nanoscience National Center for Nanoscience and Technology of China State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences University of Chinese Academy of Sciences State Key Laboratory of Protein and Plant Gene Research School of Life Sciences Peking University Biomedical Pioneering Innovation Centre Peking University 6. Institute for Cell AnalysisShenzhen Bay Laboratory Peking-Tsinghua Center for Life Sciences Peking University College of Chemistry and Molecular Engineering Beijing National Laboratory for Molecular SciencesPeking University 9. State Key Laboratory of Drug Research Centre for Chemical BiologyShanghai Institute of Materia MedicaChinese Academy of Sciences 10. Laboratory of Immunology and Nanomedicine and China-Italy Joint Laboratory of Pharmacobiotechnology for Medical ImmunomodulationShenzhen Institute of Advanced TechnologyChinese Academy of Sciences 11. Institute of Biochemistry and Cell Biology National Research Council 12. Institute of PharmacyPharmaceutical/Medicinal Chemistry and Tuebingen Center for Academic Drug Discovery Eberhard Karls University Tübingen 13. Department of Chemical Biology and Synthetic and Functional Biomolecules CenterCollege of Chemistry and Molecular Engineering Peking University 14. GBA National Institute for Nanotechnology Innovation

The ongoing COVID-19 pandemic caused by SARS-CoV-2 has raised global concern for public health and *** development of therapeutics and vaccines to combat this virus is continuously ***-omics approaches,including genomics,transcriptomics,proteomics,metabolomics,epigenomics and metallomics,have helped understand the structural and molecular features of the virus,thereby assisting in the design of potential therapeutics and accelerating vaccine development for ***,we provide an up-to-date overview of the latest applications of multi-omics technologies in strategies addressing COVID-19,in order to provide suggestions towards the development of highly effective knowledge-based therapeutics and vaccines.

关键词： COVID-19 SARS-CoV-2 multi-omics antibodies small-molecule drugs vaccines

Design,Synthesis and Biological Evaluation of Bengamide Analogues as ClpP Activators

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Chinese Journal of Chemistry 2020年第10期38卷 1111-1115页

作者： Xue-Qing Kong Bing-Yan Wei Chen-Xi Yu Xiang Na Guan Wei-Ping Ma Gang Liu cai-guang yang Fa-Jun Nan Chinese National Center for Drug Screening CAS Key Laboratory of Receptor ResearchStote Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences555 Zuchongzhi RoadShanghai 201203China University of Chinese Academy of Sciences No.19A Yuquan RoadBeijing 100049China Yantai Key Laboratory of Nanomedicine&Advanced Preparations Yantai Institute of Materia MedicaNo.39Science and Technology AvenueHigh-tech Industrial Development ZoneYantaiShandong 264000China

Summary of main observation and conclusion To combat multidrug-resistant Gram-positive bacteria,new antimicrobials particularly those with novel mechanism of action are badly *** with conventional antibiotics which are typical inhibitors,small-molecule activators of bacterial CIpP represent a new class of *** ClpP activator has been developed for clinical ***,we conducted a screening on our library of benga-mide-like ring opened analogues and found that L472-2 possesses a low minimum inhibitory concentration(MIC)against *** and shows no activity for ClpP activation in vitro,but it displayed reduced antibacterial activity against *** with clpP *** order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity,we perform further structural modifications starting from *** 37 re-mains the antimicrobial activity and activation of ClpP protein in vitro,which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.

关键词： analogues activation starting

Oxidation sensing and regulation of human bacterial pathogens

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Oxidation sensing and regulation of human bacterial pathogen...