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Discovery of a potent and highly selective inhibitor of SIRT6 against pancreatic cancer metastasis in vivo

Acta Pharmaceutica Sinica B 2024年第3期14卷 1302-1316页

作者： Xinyuan Xu Qian Zhang Xufeng Wang Jing Jin Chengwei Wu Li Feng Xiuyan Yang Mingzhu Zhao Yingyi Chen Shaoyong Lu Zhen Zheng Xiaobing Lan Yi Wang Yan Zheng Xuefeng Lu Qiufen Zhang Jian Zhang State Key Laboratory of Medical Genomics National Research Center for Translational Medicine at ShanghaiRuijin HospitalShanghai Jiao Tong University School of MedicineShanghai 200025China Medicinal Chemistry and BioinformaticsCenter Shanghai Jiao Tong University School of MedicineShanghai 200025China Department of General Surgery Huashan HospitalCancer Metastasis InstituteFudan UniversityShanghai 200040China Institute of Immunology and the CAS Key Laboratory of Innate Immunity and Chronic Disease School of Basic Medicine and Medical CenterUniversity of Science and Technology of ChinaHefei 230026China Department of Assisted Reproduction Shanghai Ninth People’s HospitalShanghai Jiao Tong University School of MedicineShanghai 200011China College of Pharmacy Ningxia Medical UniversityYinchuan 750004China Department of Pancreatic Surgery Shanghai General HospitalShanghai Key Laboratory of Pancreatic DiseaseInstitute of Pancreatic DiseaseShanghai Jiao Tong University School of MedicineShanghai 200080China

Pancreatic cancer,one of the most aggressive malignancies,has no effective treatment due to the lack of targets and drugs related to tumour ***6 can promote the migration of pancreatic cancer and could be a potential target for antimetastasis of pancreatic ***,highly selective and potency SIRT6 inhibitor that can be used in vivo is yet to be ***,we developed a noveSIRT6 allosteric inhibitor,compound 11e,with maximal inhibitory potency and an IC_(50) value of 0.98±0.13μmol/***,compound 11e exhibited significant selectivity against other histone deacetylases(HADC1-11 and SIRT1-3)at concentrations up to 100μmol/*** allosteric site and the molecular mechanism of inhibition were extensively elucidated by cocrystal complex structure and dynamic structural ***,we confirmed the antimetastatic function of such inhibitors in four pancreatic cancer cell lines as well as in two mouse models of pancreatic cancer liver *** our knowledge,this is the first study to reveal the in vivo effects of SIRT6 inhibitors on liver metastatic pancreatic *** not only provides a promising lead compound for subsequent inhibitor developmentargeting SIRT6 but also provides a potential approach to address the challenge of metastasis in pancreatic cancer.

关键词： SIRT6 inhibitor Allosteric Selectivity Cocrystal Pancreatic cancer metastasis

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Synthesis and evaluation of poly(N-vinyl caprolactam)-co-tert-butyl acrylate as kinetic hydrate inhibitor

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Chinese Journal of Chemical Engineering 2022年第10期50卷 317-325页

作者： Xing Huang Ran Zhu Liwei Cheng Yijian Zhu Peng Xiao Xiaohui Wang Bei Liu Changyu Sun Weixin Pang Qingping Li Guangjin Chen Xinjing Xu Jinfeng Ji State Key Laboratory of Natural Gas Hydrates/College of Chemical Engineering and Environment China University of PetroleumBeijing 102249China State Key Laboratory of Natural Gas Hydrate CNOOCBeijing 100010China College of Chemistry and Chemical Engineering Neijiang Normal UniversityNeijiang 641100China Faculty of Engineering China University of GeosciencesWuhan 430074China Hainan Longpan Oilfield Technology Co. LtdHainan 571900China

Low dosage kinetic hydrate inhibitors(KHIs)are a kind of alternative chemical additives to high dosage thermodynamic inhibitors for preventing gas hydrate formation in oil&gas production wells and transportation *** this paper,a new KHI,poly(N-vinyl caprolactam)-co-tert-butyl acrylate(PVCapco-TBA),was successfully synthesized with N-vinyl caprolactam(NVCap)and tert-butyl *** kinetic inhibition performances of PVCap-co-TBA on the formations of both structureⅠmethane hydrate and structureⅡnatural gas hydrate were investigated by measuring the onset times of hydrate formation under different conditions and compared with commercial KHIs such as PVP,PVCap and inhibex *** results indicated that PVCap-co-TBA outperformed these widely applied inhibitors for both structureⅠand structureⅡ*** the same dosage of KHI,the maximum tolerable degree of subcooling under which the onset time of hydrate formation exceeded 24 hours for structureⅠhydrate was much lower than that for structureⅡ*** inhibition strength increased with the increasing dosage of PVCap-co-TBA;The maximum tolerable degree of subcooling for the natural gas hydrate is more than10 K when the dosage was higher than 0.5%(mass)while it achieved 12 K when that dosage rose to0.75%(mass).Additionally,we found polypropylene glycol could be used as synergist at the dosage of 1.0%(mass)or so,under which the kinetic inhibition performance of PVCap-co-TBA could be improved *** evaluation results demonstrated that PVCap-co-TBA was a very promising KHI and a competitive alternative to the existing commercial KHIs.

关键词： Hydrate Kinetics inhibitor Poly(N-vinyl aprolactam)–co-tert-butyl acrylate Synergist Synthesis

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Testing the polar auxin transport model with a selective plasma membrane H^(+)-ATPase inhibitor

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Journal of Integrative Plant Biology 2022年第6期64卷 1229-1245页

作者： Yongqing Yang Xiaohui Liu Wei Guo Wei Liu Wei Shao Jun Zhao Junhong Li Qing Dong Liang Ma Qun He Yingzhang Li Jianyong Han Xiaoguang Lei State Key Laboratory of Plant Physiology and Biochemistry College of Biological SciencesChina Agricultural UniversityBeijing 100193China Beijing National Laboratory for Molecular Sciences Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of EducationDepartment of Chemical BiologyCollege of Chemistry and Molecular EngineeringSynthetic and Functional Biomolecules Centerand Peking‐Tsinghua Center for Life SciencesPeking UniversityBeijing 100871China Institute of Food Science and Technology Chinese Academy of Agricultural SciencesBeijing 100193China Department of Dermatology Peking University First HospitalBeijing 100034China Iomics Biosciences Inc. Beijing 100102China College of Biological Sciences China Agricultural UniversityBeijing 100193China

Auxin is unique among plant hormones in that its function requires polarized transport across plant cells.A chemiosmotic model was proposed to explain how polar auxin transport is derived by the H^(+)gradient across the plasma membrane(PM)established by PM H^(+)-adenosine triphosphatases(ATPases).However,a classical genetic approach by mutations in PM H^(+)-ATPase members did not result in the ablation of polar auxin distribution,possibly due to functional redundancy in this gene *** confirm the crucial role of PM H^(+)-ATPases in the polar auxin transport model,we employed a chemical genetic *** a chemical screen,we identified protonstatin-1(PS-1),a selective small-molecule inhibitor of PM H^(+)-ATPase activity that inhibits auxin *** with transgenic plants and yeast strains showed that the activity of PM H^(+)-ATPases affects auxin uptake as well as acropetal and basipetal polar auxin *** propose that PS-1 can be used as a tool to interrogate the function of PM H^(+)-*** results support the chemiosmotic model in which PM H^(+)-ATPase itself plays a fundamental role in polar auxin transport.

关键词： Arabidopsis auxin transport inhibitor plasma membrane H^(+)-ATPase

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inhibitor tolerance and bioethanol fermentability of levoglucosan-utilizing Escherichia coli were enhanced by overexpression of stress-responsive gene ycfR:The proteomics-guided metabolic engineering

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Synthetic and Systems Biotechnology 2021年第4期6卷 384-395页

作者： Dongdong Chang Zia Ul Islam Junfang Zheng Jie Zhao Xiaoyong Cui Zhisheng Yu College of Resources and Environment University of Chinese Academy of SciencesBeijing100049PR China Department of Chemistry Mississippi State UniversityMississippi StateMS 39762USA Department of Biochemistry and Molecular Biology School of Basic Medical SciencesCapital Medical UniversityBeijing100069PR China Yanshan Earth Critical Zone and Surface Fluxes Research Station Chinese Academy of SciencesNo.380 Huaibei TownHuairou DistrictBeijing101408PR China RCEES-IMCAS-UCAS Joint-Lab of Microbial Technology for Environmental Science Beijing100085PR China

Pretreatment of lignocellulosic biomass is crucial for the release of biofermentable sugars for biofuels production,which could greatly alleviate the burgeoning environment and energy crisis caused by the massive usage of traditional fossil *** is a cost-saving pretreatment process that can readily decompose biomass into levoglucosan,a promising anhydrosugar;however,many undesired toxic compounds inhibitory to downstream microbial fermentation are also generated during the pyrolysis,immensely impeding the bioconversion of levoglucosan-containing ***,we took the first insight into the proteomic responses of a levoglucosan-utilizing and ethanol-producing Escherichia coli to three representative biomass-derived inhibitors,identifying large amounts of differentially expressed proteins(DEPs)that could guide the downstream metabolic engineering for the development of inhibitor-resistant *** up-and eight down-regulated DEPs were further identified as the biomarker stress-responsive proteins candidate for cellular tolerance to multiple *** these biomarker proteins,YcfR exhibiting the highest expression fold-change level was chosen as the target of overexpression to validate proteomics results and develop robust strains with enhanced inhibitor tolerance and fermentation ***,based on four plasmid-borne genes encoding the levoglucosan kinase,pyruvate decarboxylase,alcohol dehydrogenase,and protein YcfR,a new recombinant strain *** LGE-ycfR was successfully created,showing much higher acetic acid-,furfural-,and phenol-tolerance levels compared to the control without overexpression of *** specific growth rate,final cell density,ethanol concentration,ethanol productivity,and levoglucosan consumption rate of the recombinant were also remarkably *** the proteomics-guided metabolic engineering and phenotypic observations,we for the first time corroborated that YcfR is a stress-induced protein responsi

关键词： Lignocellulosic biomass Levoglucosan inhibitor Proteomics Gene overexpression Bioethanol

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inhibitorY PROPERTY CHARACTERIZATION AND REACTIVE SITE EXPLORATION OF THE ARROWHEAD PROTEINASE inhibitor

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Science China Chemistry 1991年第7期34卷 832-839页

作者：杨慧玲王丽秀朱德煦戚正武 Shanghai Institute of Biochemistry Academia Sinica Shanghai 200031 PRC

Affinity chromatography was used to separate two components A and B of the crystalline arrowhead proteinase inhibitor. Both A and B are double-headed and multifunctional proteinase inhibitors. inhibitor A is capable of inhibiting equimolarly trypsin and chymo-trypsin simultaneously, and has a weak inhibitory activity toward kallikrein; whereas inhibitor B can inhibit two molecules of trypsin simultaneously, and shows rather higher inhibitory activity toward kallikrein than inhibitor A, but its inhibitory activity toward chymo-trypsin is much weaker than that of inhibitor A. The results of chemical modification and the competitive binding of trypsin and chymotrypsin with inhibitor A showed that the two reactive sites of both inhibitors A and B are Lys and Arg residues. Among them the Lys reactive site is specific for inhibiting mainly trypsin, whereas the active domain composed of the Arg reactive site appears to be multifunctional and capable of inhibiting many different Ser proteinases. Based on the structural characteristics of inhibitors A and B, it was predicated that the two reactive sites should be located in the positions Lys-Ser (44-45) and Arg-Tyr-Lys (76-78), respectively. In inhibitor A, there exists another hydrophobic residue involved in inhibiting chymotrypsin. This residue might be situated in the reactive region composed of the Arg reactive site.

关键词： Ser proteinase inhibitor arrowhead chemical modification.

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Effects of chitosan inhibitor on the electrochemical corrosion behavior of 2205 duplex stainless steel

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International Journal of Minerals,Metallurgy and Materials 2017年第11期24卷 1260-1266页

作者： Se-fei Yang Ying Wen Pan Yi Kui Xiao Chao-fang Dong Department of Stomatology General Hospital of the People’s Liberation Army Beijing 100853 China Institute for Advanced Materials and Technology University of Science and Technology Beijing Beijing 100083 China Journals Publishing Center University of Science and Technology Beijing Beijing 100083 China

The effects of chitosan inhibitor on the corrosion behavior of 2205 duplex stainless steel were studied by electrochemical measurements, immersion tests, and stereology microscopy. The influences of immersion time, temperature, and chitosan concentration on the corrosion inhibition performance of chitosan were investigated. The optimum parameters of water-soluble chitosan on the corrosion inhibition performance of 2205 duplex stainless steel were also determined. The water-soluble chitosan showed excellent corrosion inhibition performance on the 2205 duplex stainless steel. Polarization curves demonstrated that chitosan acted as a mixed-type inhibitor. When the stainless steel specimen was immersed in the 0.2 g/L chitosan solution for 4 h, a dense and uniform adsorption film covered the sample surface and the inhibition efficiency(IE) reached its maximum value. Moreover, temperature was found to strongly influence the corrosion inhibition of chitosan; the inhibition efficiency gradually decreased with increasing temperature. The 2205 duplex stainless steel specimen immersed in 0.4 g/L water-soluble chitosan at 30°C displayed the best corrosion inhibition among the investigated specimens. Moreover, chitosan decreased the corrosion rate of the 2205 duplex stainless steel in an FeCl_3 solution.

关键词： inhibitor chitosan stainless steel corrosion behavior electrochemistry

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Texture and inhibitor features of grain-oriented pure iron produced by different cold-rolling processes

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Journal of Iron and Steel Research International 2018年第10期25卷 1026-1032页

作者： Jian-jun Deng Hai-jun Wang Zhe Rong Li Xiang Sheng-tao Qiu Yong Gan National Engineering Research Center of Continuous Casting Technology Central Iron and Steel Research Institute Beijing 100081 China Wuyang Iron and Steel Co. Ltd. Hebei Iron and Steel Group Wuyang 462400 Hebei China School of Metallurgical Engineering Anhui University of Technology Ma'anshan 243032 Anhui China

To promote the manufacture of grain-oriented pure iron, the texture and inhibitor features of two samples A and B produced by different cold-rolling processes were studied by optical microscopy, X-ray diffraction, and transmission electron microscopy. The results showed that a higher content of inhibitor elements directly resulted in a greater number of fine inhibitors, which exhibited strong inhibitory ability, leading to more fine precipitates of appropriate size effectively inhibiting the growth of primary grains in decarburized bands （sheets） during the single-stage cold-rolling process. The formation of the component with { 110}〈001〉 Goss orientation was greatly suppressed in the stage of primary recrystallization, and this component could hardly be observed in the decarburized band; by contrast, the {411 }〈148〉-oriented grains grew. During the process of high-temperature annealing, abnormal growth occurred and secondary recrystallized grains （Goss orientation） merged with other matrix grains such as { 111 }〈112〉 and {411 }〈148〉. The magnetic induction of samples A and B at 800 Aim was 1.939 T and 1.996 T, respectively.

关键词： Grain-oriented pure iron Microstructure Texture inhibitor Cold rolling

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Red tetrazolium as an effective inhibitor for the corrosion of cold rolled steel in 7.0 mol·L^(-1) H_2SO_4 solution

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Chinese Journal of Chemical Engineering 2018年第12期26卷 2641-2653页

作者： Xianghong Li Shuduan Deng Xiaoguang Xie Faculty of Chemical Engineering Southwest Forestry University Faculty of Materials Science and Engineering Southwest Forestry University School of Chemical Science and Technology Yunnan University

The corrosion inhibition of cold rolled steel(CRS) in 7.0 mol·L^(-1) H_2 SO_4 solution by red tetrazolium(RTZ) was carefully investigated using both experimental procedures and theoretical techniques. The results show that RTZ acts as an effective inhibitor for the corrosion of CRS in 7.0 mol·L^(-1) H_2SO_4, and the maximum inhibition efficiency is higher than 95% with a RTZ concentration of 2.0 mmol·L^(-1). The adsorption of RTZ on CRS surface follows Langmuir isotherm. RTZ effectively retards both cathodic and anodic reactions, and acts as a mixed-type inhibitor. EIS exhibits two capacitive loops, and their resistances increase drastically in the presence of RTZ. SEM and AFM confirm that the addition of RTZ could significantly retard the corrosion of CRS surface. A series of characterizations like FTIR, RS, XRD and XPS reveal that the corrosion CRS surface is composed of the corrosion products of iron sulfates, iron oxides and iron hydroxide, as well as inhibitor. Theoretical results of quantum chemical calculation and molecular dynamics(MD) indicate that the adsorption center of RTZ+(organic cationic part of RTZ) mainly relies on its tetrazole ring,and the adsorption of RTZ+on Fe(001) surface is in a nearly flat orientation mode.

关键词： Steel Sulfuric acid Red tetrazolium Corrosion inhibitor Adsorption

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Crystal Structure of the MAP3K TAO2 Kinase Domain Bound by an inhibitor Staurosporine

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Acta Biochimica et Biophysica Sinica 2006年第6期38卷 385-392页

作者： Elizabeth J.GOLDSMITH USA TX 75390-9038 Department of Biochemistry University of Texas Southwestern Medical Center at Dallas

Mitogen-activated protein kinase (MAPK) signal transduction pathways are ubiquitous ineukaryotic cells,which transfer signals from the cell surface to the nucleus,controlling multiple *** are activated by MAPK kinases [MAP2Ks or MAP/extracellular signal-regulated kinase(ERK) kinases (MEK)],which in turn are activated by MAPK kinase kinases (MAP3Ks).TAO2 is a MAP3Klevel kinase that activates the MAP2Ks MEK3 and MEK6 to activate p38 *** p38 MAPKs arekey regulators of expression of inflammatory cytokines,they appear to be involved in human diseases suchas asthma and *** an upstream activator of p38s,TAO2 represents a potential drug *** we report the crystal structure of active TAO2 kinase domain in complex with staurosporine,a broad-range protein kinase inhibitor that inhibits TAO2 with an ICof 3 μ*** structure reveals that staurosporineoccupies the position where the adenosine of ATP binds in TAO2,and the binding of the inhibitor mimicsmany features of ATP *** polar and nonpolar interactions contribute to the *** induces conformational changes in TAO2 residues that surround the inhibitormolecule,but causes very limited global changes in the *** structure provides atomic details forTAO2-staurosporine interactions,and explains the relatively low potency of staurosporine against *** structure presented here should aid in the design of inhibitors specific to TAO2 and related kinases.

关键词： TAO2 MAP3K inhibitor staurosporine crystal structure

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Thermodynamic and Adsorption Behaviour of Medicinal Nitramine as a Corrosion inhibitor for AISI Steel Alloy in HCl Solution

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Journal of Materials Science & Technology 2013年第9期29卷 884-892页

作者： Ali Reza Hosein Zadeh Iman Danaee Mohamad Hosein Maddahy Abadan Faculty of Petroleum Engineering Petroleum University of Technology

The inhibition ability of 2-amino-5-nitrothiazole （Nitramine） against the corrosion of AISI steel 4130 in 1 mol/L HCI solution was evaluated by polarization, electrochemical impedance spectroscopy （EIS） and chronoamperometry. Polarization studies indicated that nitramine retards both the cathodic and anodic reactions through chemical adsorption and blocks the active corrosion sites. The adsorption of this compound obeyed the Temkin＇s adsorption isotherm. The inhibition efficiency was increased with inhibitor concentration as well as temperature. EIS data were analysed by equivalent circuit model shows that as the inhibitor concentration increased the charge transfer resistance of steel increased whilst double layer capacitance decreased. Kinetic and thermodynamic parameters such as activation energy, enthalpy, entropy and free energy of activation and adsorption were calculated. Atomic force microscopy and optical microscopy were used to study the steel surface with and without inhibitor.

关键词： Steel 4130 Corrosion inhibitor Adsorption isotherm Temkin

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