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DISCOVERY OF TRIKETONE-QUINOXALINE HYBRIDS AS POTENT HPPD INHIBITORS USING STRUCTURE-BASED DRUG DESIGN

Frontiers of Agricultural Science and Engineering 2022, Volume 9, Issue 1,   Pages 133-145 doi: 10.15302/J-FASE-2021401

Abstract: HPPD has proved to be a promising target in herbicide research and development.A battery of novel triketone-quinoxaline compounds has been designed using a structure-based drug designadjacent carbonyls of the triketone moiety of the representative compound 2-(2,3-dimethyl-8-(o-tolyl)quinoxalinein a bidentate pose, and its quinoxaline scaffold forms two sets of parallel π-stacking interactionThis study indicates that triketone-quinoxaline is a promising scaffold for discovering HPPD inhibitors

Keywords： herbicide / HPPD / inhibitor / quinoxaline / triketon    

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Discovery for New Herbicide Sites of Action by Quantification of plant Primary Metabolite and Enzyme Perspective

Franck E. Dayan, Stephen O. Duke

Engineering 2020, Volume 6, Issue 5,   Pages 509-514 doi: 10.1016/j.eng.2020.03.004

Abstract:

No herbicide with a new molecular site of action (SOA) has been introduced since the 1980s.Two untried strategies for the discovery on new herbicide SOAs are discussed.Targeting SOAs that result in accumulation of phytotoxic compounds is the first novel approach to herbicideWe know that higher numbers of enzyme molecules for a SOA requires more herbicide to kill a plant.Modern proteomic methods can identify low enzyme level SOAs for biorational herbicide discovery.

Keywords： Natural products     Biorational discovery     Mode of action     Herbicide    

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Renin--angiotensin system inhibitor is associated with the reduced risk of all-cause mortality in COVID

Frontiers of Medicine 2022, Volume 16, Issue 1,   Pages 102-110 doi: 10.1007/s11684-021-0850-9

Abstract: January 2020 to March 2020 to investigate the association between the use of renin–angiotensin system inhibitorAssociations between the use of RAS-I (angiotensin-converting enzyme inhibitor (ACEI) or angiotensin

Keywords： COVID-19     RAS inhibitor     hypertension     all-cause mortality    

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Comparison between inhibitor and uncoupler for minimizing excess sludge production of an activated sludge

CHEN Guowei, XI Pengge, XU Deqian, YU Hanqing

Frontiers of Environmental Science & Engineering 2007, Volume 1, Issue 1,   Pages 63-66 doi: 10.1007/s11783-007-0012-6

Abstract: minimization of excess sludge production, the reduction in the excess sludge production in the presence of an inhibitor

Keywords： uncoupling coefficient     Cu     minimization     presence     uncoupling    

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Endogenous tissue factor pathway inhibitor in vascular smooth muscle cells inhibits arterial thrombosis

Jichun Yang, Kaiyue Jin, Jiajun Xiao, Jing Ma, Duan Ma

Frontiers of Medicine 2017, Volume 11, Issue 3,   Pages 403-409 doi: 10.1007/s11684-017-0522-y

Abstract:

Tissue factor pathway inhibitor (TFPI) is the main inhibitor of tissue factor-mediated coagulation

Keywords： arterial thrombosis     conditional knockout mice     tissue factor pathway inhibitor     vascular smooth muscle    

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Estimating the effect of urease inhibitor on rice yield based on NDVI at key growth stages

Kailou LIU,Yazhen LI,Huiwen HU

Frontiers of Agricultural Science and Engineering 2014, Volume 1, Issue 2,   Pages 150-157 doi: 10.15302/J-FASE-2014028

Abstract: The effect of the urease inhibitor, N-(n-butyl) thiophosphoric triamide (NBPT) at a range of applicationTherefore, it was feasible to estimate rice yield for different amounts of urease inhibitor using NDVI

Keywords： normalized difference vegetation index (NDVI)     N-(n-butyl) thiophosphoric triamide (NBPT)     rice     grain yield    

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A small-molecule pan-HER inhibitor alone or in combination with cisplatin exerts efficacy against nasopharyngeal

Frontiers of Medicine 2023, Volume 17, Issue 2,   Pages 275-289 doi: 10.1007/s11684-022-0945-y

Abstract: treatment of nasopharyngeal carcinoma (NPC) and explored the anti-tumor effects of the novel pan-HER inhibitorThe pan-HER inhibitor HM781-36B alone or in combination with cisplatin represents promising therapeutic

Keywords： epidermal growth factor receptor     ErbB receptors     HM781-36B     nasopharyngeal carcinoma     molecular targeted therapy     cisplatin    

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Genomic regions associated with the sex-linked inhibitor of dermal melanin in Silkie chicken

Ming TIAN,Rui HAO,Suyun FANG,Yanqiang WANG,Xiaorong GU,Chungang FENG,Xiaoxiang HU,Ning LI

Frontiers of Agricultural Science and Engineering 2014, Volume 1, Issue 3,   Pages 242-249 doi: 10.15302/J-FASE-2014018

Abstract: This dermal hyperpigmentation phenotype is controlled by the sex-linked inhibitor of dermal melanin gene

Keywords： sex-linked inhibitor of dermal melanin (Id)     Silkie     chromosome Z    

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Rapamycin enhances the anti-tumor activity of cabozantinib in cMet inhibitor-resistant hepatocellular

Frontiers of Medicine 2022, Volume 16, Issue 3,   Pages 467-482 doi: 10.1007/s11684-021-0869-y

Abstract: resistance to cMet inhibitors, and the combination of cabozantinib and mammalian target of rapamycin (mTOR) inhibitorformation of human umbilical vascular endothelial cells and human growth factor-induced invasion of cMet inhibitor-resistant

Keywords： hepatocellular carcinoma     cabozantinib     primary resistance     rapamycin    

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Medical oncology management of advanced hepatocellular carcinoma 2019: a reality check

Amy Lee, Fa-Chyi Lee

Frontiers of Medicine 2020, Volume 14, Issue 3,   Pages 273-283 doi: 10.1007/s11684-019-0728-2

Abstract: Up until 2017, treatment of advanced HCC was largely limited to sorafenib, an oral tyrosine kinase inhibitor

Keywords： hepatocellular carcinoma     tyrosine kinase inhibitor     check point inhibitor     anti-angiogenesis    

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Hypoxia-induced activity loss of a photo-responsive microtubule inhibitor azobenzene combretastatin A4

Yang An, Chao Chen, Jundong Zhu, Pankaj Dwivedi, Yanjun Zhao, Zheng Wang

Frontiers of Chemical Science and Engineering 2020, Volume 14, Issue 5,   Pages 880-888 doi: 10.1007/s11705-019-1864-6

Abstract: The conformation-dependent activity of azobenzene combretastatin A4 (Azo-CA4) provides a unique approach to reduce the side-effects of chemotherapy, due to the light-triggered conformation transition of its azobenzene moiety. Under hypoxic tumor microenvironment, however, the high expression of azoreductase can reduce azobenzene to aniline. It was postulated that the Azo-CA4 might be degraded under hypoxia, resulting in the decrease of its anti-tumor activity. The aim of this study was to verify such hypothesis in HeLa cells . The quantitative drug concentration analysis shows the ratiometric formation of degradation end-products, confirming the bioreduction of Azo-CA4. The tubulin staining study indicates that Azo-CA4 loses the potency of switching off microtubule dynamics under hypoxia. Furthermore, the cell cycle analysis shows that the ability of Azo-CA4 to induce mitotic arrest is lost at low oxygen content. Therefore, the cytotoxicity of Azo-CA4 is compromised under hypoxia. In contrast, combretastatin A4 as a positive control maintains the potency to inhibit tubulin polymerization and break down the nuclei irrespective of light irradiation and oxygen level. This work highlights the influence of hypoxic tumor microenvironment on the anti-tumor potency of Azo-CA4, which should be considered during the early stage of designing translational Azo-CA4 delivery systems.

Keywords： hypoxia     microtubule inhibitor     drug delivery     azo-combretastatin A4     photo-responsive    

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Adenovirus-mediated tissue inhibitor of metalloproteinase-3 gene transfection inhibits rabbit intervertebral

Xudong YU MM, Zengwu SHAO MD, Liming XIONG MD, Weiwei XU MM, Hezhong WANG MM, Huifa XU MM,

Frontiers of Medicine 2009, Volume 3, Issue 4,   Pages 415-420 doi: 10.1007/s11684-009-0072-z

Abstract: this study was to investigate the inhibitory effects of recombinant adenovirus vector carrying tissue inhibitor

Keywords： tissue inhibitor of metalloproteinase-3     intervertebral disc     rabbit     gene therapy    

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Fe–Cr–Ni based alloys exposed to molten MgCl2–KCl–NaCl salt with over-added Mg corrosion inhibitor

Frontiers of Chemical Science and Engineering 2023, Volume 17, Issue 10,   Pages 1608-1619 doi: 10.1007/s11705-023-2349-1

Abstract: Adding Mg into molten MgCl2–NaCl–KCl salt as a corrosion inhibitor is one of the most effectivedirect contact of liquid Mg with Ni-containing alloys should be avoided during using Mg as a corrosion inhibitor

Keywords： concentrated solar power (CSP)     Mg corrosion inhibitor     Mg–Ni intermetallic     salt purification     thermal    

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The secondary laticifer differentiation in rubber tree is induced by trichostatin A, an inhibitor of

Shixin ZHANG,Shaohua WU,Weimin TIAN

Frontiers of Agricultural Science and Engineering 2016, Volume 3, Issue 4,   Pages 357-362 doi: 10.15302/J-FASE-2016125

Abstract: using an experimental morphological technique, the present study revealed that trichostatin A (TSA), an inhibitor

Keywords： Hevea brasiliensis     histone acetylation     laticifer differentiation     trichostatin     vascular cambia    

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Catalytic activity of manganese oxide supported on alumina in the synthesis of quinoxalines

Rekha M., H. Kathyayini, N. Nagaraju

Frontiers of Chemical Science and Engineering 2013, Volume 7, Issue 4,   Pages 415-421 doi: 10.1007/s11705-013-1360-3

Abstract: Two catalysts, alumina and manganese oxide supported on alumina, have been prepared by calcination and precipitation-impregnation methods, respectively. The catalysts are characterised by the following techniques: Brunner-Emmett-Teller-N adsorption-desorption for surface area, temperature programmed desorption of NH and -butyl amine back titration methods for surface acidity, powder X-ray diffraction for textural properties, and Fourier transform infrared spectroscopy for the anionic radicals. The catalytic activity has been determined under heterogeneous conditions in the condensation reaction between -phenylenediamine and benzil. The product purity is checked by thin-layer chromatography and melting point. The products are also analysed by LC-MS and H-NMR techniques. The yields of the products have been found to be good and catalysts exhibited excellent recyclability. The effect of changing the reaction parameters such as temperature, reaction time, amount of the catalyst, nature of solvent and molar ratio of reactants on the yield of the product has been studied. The surface acidity of the catalysts plays an important role in activating the reaction.

Keywords： alumina     manganese oxide deposited on alumina     quinoxaline synthesis    

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Title Author Date Type Operation

DISCOVERY OF TRIKETONE-QUINOXALINE HYBRIDS AS POTENT HPPD INHIBITORS USING STRUCTURE-BASED DRUG DESIGN

Journal Article

Discovery for New Herbicide Sites of Action by Quantification of plant Primary Metabolite and Enzyme

Franck E. Dayan, Stephen O. Duke

Journal Article

Renin--angiotensin system inhibitor is associated with the reduced risk of all-cause mortality in COVID

Journal Article

Comparison between inhibitor and uncoupler for minimizing excess sludge production of an activated sludge

CHEN Guowei, XI Pengge, XU Deqian, YU Hanqing

Journal Article

Endogenous tissue factor pathway inhibitor in vascular smooth muscle cells inhibits arterial thrombosis

Jichun Yang, Kaiyue Jin, Jiajun Xiao, Jing Ma, Duan Ma

Journal Article

Estimating the effect of urease inhibitor on rice yield based on NDVI at key growth stages

Kailou LIU,Yazhen LI,Huiwen HU

Journal Article

A small-molecule pan-HER inhibitor alone or in combination with cisplatin exerts efficacy against nasopharyngeal

Journal Article

Genomic regions associated with the sex-linked inhibitor of dermal melanin in Silkie chicken

Ming TIAN,Rui HAO,Suyun FANG,Yanqiang WANG,Xiaorong GU,Chungang FENG,Xiaoxiang HU,Ning LI

Journal Article

Rapamycin enhances the anti-tumor activity of cabozantinib in cMet inhibitor-resistant hepatocellular

Journal Article

Medical oncology management of advanced hepatocellular carcinoma 2019: a reality check

Amy Lee, Fa-Chyi Lee

Journal Article

Hypoxia-induced activity loss of a photo-responsive microtubule inhibitor azobenzene combretastatin A4

Yang An, Chao Chen, Jundong Zhu, Pankaj Dwivedi, Yanjun Zhao, Zheng Wang

Journal Article

Adenovirus-mediated tissue inhibitor of metalloproteinase-3 gene transfection inhibits rabbit intervertebral

Xudong YU MM, Zengwu SHAO MD, Liming XIONG MD, Weiwei XU MM, Hezhong WANG MM, Huifa XU MM,

Journal Article

Fe–Cr–Ni based alloys exposed to molten MgCl2–KCl–NaCl salt with over-added Mg corrosion inhibitor

Journal Article

The secondary laticifer differentiation in rubber tree is induced by trichostatin A, an inhibitor of

Shixin ZHANG,Shaohua WU,Weimin TIAN

Journal Article

Catalytic activity of manganese oxide supported on alumina in the synthesis of quinoxalines

Rekha M., H. Kathyayini, N. Nagaraju

Journal Article