The Three-component One-pot Synthesis of 4,6-Diarylpyrimidin-2(1h)-ones and 9-Phenyl-8-oxa-10,12-diaza-tricyclo[7.3.1.0~(2,7)]trideca-2(7),3,5-trien-11-one

1 Results Pyrimidinones (PMs) are a class of important heterocycles which have been well documented throughout the literature due to their biological importance. They exhibit a wide range of pharmaceutical and therapeutic properties[1].A rapid and efficient one-pot method for the synthesis of 4,6-diarylpyrimidin-2(1H)- ones and related heterocycles is described.The condensation of acetophenone derivatives,aldehydes and urea in the presence of sulfamic acid was employed to synthesize a variety of pyrimid...     

Innovation on Petroleum Engineering Technology of China Beach and Shallow Water Areas

1Chinaoffshoreoil&gasresourcesandtheircharacteristicfeatures　Chinaoffshoreoil&gasexplorationstartedduringthe1 95 0s .Until 1 971 ,thecommercialHai 4fieldwasfoundinBohai.Subsequentlytwoproductionplatformswereconstruc ted ,thefirstChinaoffshoreoilfieldwasformed .Fromthenon ,Chinaoffshoreoil&gasexplorationandexploitationspeedbecameprogressivelyfaster.Afteralargeamountofexplorationwork ,theoilandgasresourcesinChinacoastalareasweremadeclearpreliminarily .AccordingtoState sSecondaryResourceEva…     

我国最薄炉墙焦炉的设计、施工与生产

减薄炭化室炉墙是提高焦炉产量,节约能源,减少投资的重要途径之一。本文介绍我国厚80毫米炉墙焦炉的设计、施工与生产情况。     

试论"代表先进社会生产力发展要求"是对历史唯物主义的新发展

中国共产党始终代表中国先进生产力的发展要求的论断,是站在历史唯物主义的角度,揭示出我们党兴旺发达的根本动力.     

学生体质,健康调研数据微机统计计算系统

全国学生体质、健康调研工作所涉及的指标多、数据量大、计算内容多,因此,有必要研制一套功能较齐全完备、便于使用的微机统计计算系统.该文介绍了该系统的设计思想、特点、结构、功能以及使用效果,该系统适用于全国各地及各高等院校,可处理以前的体质调研数据或其他有关数据,通用性与实用性较强.     

负反馈电桥在电阻传感器线性化中的应用

本文介绍利用信号流图及梅森公式分析设计负反馈电桥电路,以及在电阻传感器测量线性化中的应用。     

Nuclear localization and signalling activity of phosphoinositidase C beta in Swiss 3T3 cells.

The hydrolysis of phosphatidylinositol 4,5-bisphosphate (PtdInsP2) is a widespread receptor-coupled signalling system at the plasma membrane of most eukaryotic cells. The existence of an entirely separate nuclear phosphoinositide signalling system is suggested from evidence that purified nuclei synthesize PtdInsP2 and phosphatidylinositol 4-phosphate (PtdInsP) in vitro and that a transient decrease in the mass of these lipids occurs when Swiss 3T3 cells are cultured in the presence of insulin-like growth factor-1 (IGF-1). These IGF-1-dependent changes in inositol lipids coincide with an increase in nuclear diacyglycerol and precede translocation to the nucleus and activation of protein kinase C (refs 5, 6). Circumstantial evidence that links these changes with mitosis comes from the isolation of a 3T3 clone that expresses the type-1 IGF receptor and binds IGF-1 peptide but does not respond mitogenically or show transient mass changes in nuclear inositol lipids. A key question is how IGF-1 initiates the rapid breakdown of PtdInsP and PtdInsP2 in the nucleus. Here we present evidence that nuclei of 3T3 cells contain the beta-isozyme of phosphoinositidase C, whereas the gamma-isozyme is confined to the cytoplasm and that IGF-1 treatment stimulates exclusively the activity of nuclear phosphoinositidase C.     

Prediction of the structure of a receptor-protein complex using a binary docking method.

To validate procedures of rational drug design, it is important to develop computational methods that predict binding sites between a protein and a ligand molecule. Many small molecules have been tested using such programs, but examination of protein-protein and peptide-protein interactions has been sparse. We were able to test such applications once the structures of both the maltose-binding protein (MBP) and the ligand-binding domain of the aspartate receptor, which binds MBP, became available. Here we predict the binding site of MBP to its receptor using a 'binary docking' technique in which two MBP octapeptide sequences containing mutations that eliminate maltose chemotaxis are independently docked to the receptor. The peptides in the docked solutions superimpose on their original positions in the structure of MBP and allow the formation of an MBP-receptor complex. The consistency of the computational and biological results supports this approach for predicting protein-protein and peptide-protein interactions.