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Acta Pharmacologica Sinica 2005年第12期26卷 1485-1491页

作者： Chuan WANG Xiao-na DU Qing-zhong JIA Hai-lin ZHANG~2 Department of Pharmacology Hebei Medical University,Shijiazhuang 050017,China Department of Pharmacology Hebei Medical University Shijiazhuang China

Aim:To investigate the effects of the pleckstrin homology(PH)domain of phos-pholipase Cδ1(PLCδ1PH)on inhibition of phospholipase C(PLC)-mediated hy-drolysis of phosphatidylinositol 4,5-bisphosphate[PtdIns(4,5)P2]by ***:A fusion construct of green fluorescent protein(GFP)and PLCδ1PH(PLCδ1PH-GFP),which is known to bind PtdIns(4,5)P2specifically,together withlaser-scanning confocal microscopy,was used to trace PtdIns(4,5)***:Stimulation of the type 1 muscarinic receptor and the bradykinin 2 recep-tor induced a reversible PLCδ1PH-GFP translocation from the membrane to thecytosol in COS-7 *** inhibitor U73122 blocked the ***,a known PtdIns kinase inhibitor,did not affect the translocationinduced by ACh,but blocked recovery after translocation,indicating thatPtdIns(4,5)P2hydrolysis occurs through receptor-mediated PLC ***,a commonly used phospholipase C blocker,failed to block the recep-tor-induced PLCδ1PH-GFP translocation,indicating that neomycin is unable toblock PLC-mediated Ptdlns(4,5)Pe ***,in the absence of PLCδ1PH-GFP expression,neomycin abolished the receptor-induced hydrolysis ofPtdIns(4,5)P2 by ***:Although PLCδ1PH and neomycin bind toPtdIns(4,5)P2 in a similar way,they have distinct effects on receptor-mediatedactivation of PLC and PtdIns(4,5)P2 hydrolysis.

关键词： phosphatidylinositol 4,5-bisphosphate neomycin phospholipase C pleckstrin homology domains competitive binding acetylcholine green fluorescent proteins

Fractionation and fixation of rare earth elements in soils:Effect of spiking with lanthanum,cerium,and neodymium chlorides

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Journal of Rare Earths 2022年第1期40卷 143-152页

作者： Olga B.Rogova Petr S.Fedotov Rustam Kh.Dzhenloda Vasily K.Karandashev V.V.Dokuchaev Soil Science Institute Russian Academy of Sciences7 Building 2 Pyzhevskiy Side StreetMoscow119017Russia V.I.Vernadsky Institute of Geochemistry and Analytical Chemistry Russian Academy of Sciences19 Kosygin StreetMoscow119991 Russia National University of Science and Technology'MISiS' 4 Leninsky ProspectMoscow119049Russia The Institute of Microelectronics Technology and High-Purity Materials Russian Academy of Sciences6 Institution StreetChernogolovka142432Russia

Industrial and agricultural activities lead to the release of rare earth elements(REEs)in wastewater and aquatic ecosystems,and their accumulation in ***,the behavior of REEs in soils remains somewhat *** the present work the fractionation and fixation of REEs in soddy-podzolic and chernozem soils spiked with La,Ce,and Nd chlorides were studied using dynamic(continuous flow)extraction,which allows natural conditions to be mimicked and artefacts to be *** eluents applied are aimed to dissolve exchangeable,specifically sorbed,bound to Mn oxides,bound to metal-organic complexes,and bound to amorphous and poorly ordered Fe/Al oxides fractions extractable by 0.05 mol/L Ca(NO_(3))2,0.43 mol/L CH_(3)COOH,0.1 mol/L NH_(2)OH·HCl,0.1 mol/L K_(4)P_(2)O_(7) at pH 11,and 0.1 mol/L(NH4)_(2)C_(2)O_(4) at pH 3.2,*** is found that the fixations of added La,Ce,and Nd in the form of metal-organic complexes is predominant for both types of soils:35%-38%in soddy-podzolic soil and 50%-79%in *** fixation of added elements in the first three fractions(exchangeable,specifically sorbed,and bound to Mn oxides)is significant for soddy-podzolic soil(5%-25%).For chernozem,the relative contents of added Ce and Nd in these fractions are nearly *** the content of exchangeable La is notable,about 5%.Adding any of three elements(La,Ce,or Nd)at the level of100 mg/kg to an initial sample results in changing the fractionation and bioaccessibility of other REEs present in *** contents increase in the first three fractions and decrease in fifth(oxalate extractable)fraction for both soddy-podzolic soil and *** main difference is the behavior of REEs in pyrophosphate extractable *** soddy-podzolic soil,adding La,Ce,or Nd results in decreasing the contents of other REEs associated with organic *** chernozem,on the contrary,the contents of REEs in the form of metal-organic complexes slightly *** processes

关键词： Rare earth elements Soddy-podzolic soil Chernozem Fractionation competitive binding

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Development of a quantitative,cell-based,high-content screening assay for epidermal growth factor receptor modulators

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Acta Pharmacologica Sinica 2007年第10期28卷 1698-1704页

作者： Jue WANG~2,Xin XIE~(2,3)~2 The National Center for Drug Screening,Shanghai Institute of Materia Medica,Chinese Academy of Sciences Graduate School of Chinese Academyof Sciences Shanghai 201203,China The National Center for Drug Screening Shanghai Institute of Materia Medica Chinese Academy of Sciences Graduate School of Chinese Academy of Sciences Shanghai China

Aim:To develop a robust,cell-based,high-content screening （HCS） assay basedon receptor internalization for the identification of novel modulators of the epi-dermal growth factor receptor （EGFR）.Methods:Agonist-induced receptorinternalization is part of the signaling cascade of ***-taggedepidermal growth factor （EGF） was used to visualize the internalized receptor-ligand *** fluorescent intracellular spots were detected and mea-sured with an ArrayScan HCS *** that can competitively bind toEGFR or interfere with EGFR internalization process would result in a reducednumber and intensity of intracellular fluorescent *** assay was validated,optimized,and applied to a large-scale screening of a library containing 48 000synthetic ***:The competition between fluorescent EGF andunlabeled EGF reveals the IC50of unlabeled EGF is approximately 0.2 nmol/L,which is comparable with other published *** compounds with arelatively high degree of interference with EGFR internalization were *** of the compounds was proven to be agonist of the EGFR since it inducedphosphorylation of the receptor and extracellular signal-regulated protein ki-nase （ERK）.Conclusion:This automated,objective,and easy-to-use assay pro-vided abundant information,quantitative results,and demonstrated the potentialuse of HCS methods in searching membrane receptor modulators.

关键词： high-content screening epidermal growth factor receptor receptor internalization competitive binding

Host-guest inclusion for enhancing anticancer activity of pemetrexed against lung carcinoma and decreasing cytotoxicity to normal cells

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Chinese Chemical Letters 2021年第10期32卷 3034-3038页

作者： Junyi Chen Yahan Zhang Yadan Zhang Liang Zhao Longming Chen Yao Chai Zhao Meng Xueshun Jia Qingbin Meng Chunju Li College of Environmental and Chemical Engineering Shanghai UniversityShanghai 200444China State Key Laboratory of Toxicology and Medical Countermeasures Beijing Institute of Pharmacology and ToxicologyBeijing 100850China Department of Chemistry Center for Supramolecular Chemistry and CatalysisShanghai UniversityShanghai 200444China

Advanced chemotherapy strategies are in urgent demand for improving anticancer ***,a water-soluble pillar[6]arene(WP6 A)was used to load chemotherapeutic agent pemetrexed(PMX)by forming direct host-guest inclusion,which is beneficial for decreasing cytotoxicity of PMX on BEAS-2 B *** and florescence titration served to confirm the complexation between WP6 A and ATP with higher affinity[(5.67?0.31)x 10^(5)L/mol],favoring competitive replacement of *** ATP by WP6 A effectively prevented ATP from being hydrolyzed in presence of alkaline *** formed host-guest complex was further used to block the efflux pump by cutting off energy source from ATP hydrolysis,which was accompanied with releasing PMX to produce synergistic enhancement of anticancer performance towards A549 *** supramolecular strategy would also be extended to other clinical chemotherapeutic agents and it was expected to provide salutary profits for cancer patients.

关键词： Supramolecular chemotherapy Host-guest complexation Pemetrexed ATP competitive binding

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SAR by MS

Chemical Research in Chinese Universities 2001年第Z1期17卷 110-页

作者： HOFSTADLER Steven RNAs have recently emerged as an exciting new target for small molecule therapeutics. Conventional HTS discovery strategies measuring disruption of RNAprotein interactions have proven unsuccessful. We describe a ligand-based drug discovery strategy that

RNAs have recently emerged as an exciting new target for small molecule therapeutics. Conventional HTS discovery strategies measuring disruption of RNAprotein interactions have proven unsuccessful. We describe a ligand-based drug discovery strategy that addresses the inherent difficulties RNA targets. The strategy is based on: 1) using a MS spectrometry (MS)-based assay to measure the affinity of compounds for a target; 2) performing competitive binding experiments and molecular modeling with the motifs to determine the binding site(s) of the ligands; 3) design and synthesis of derivatives of interesting binders to establish the linking sites; 4) identifying the appropriate linker group using MS; 5) fusing motifs into a more complex structure to afford higher affinity compounds. Example of applying this strategy to identify new classes of lead molecules with affinity and specificity for ribosomal RNA targets will be presented.

关键词： competitive binding molecular modeling complex structure small molecule drug discovery binding site