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MA‐NOTMP: A Triazacyclononane Trimethylphosphinate Based Bifunctional Chelator for Gallium Radiolabelling of Biomolecules 下载免费PDF全文
Sophie Poty Dr. Pauline Désogère Dr. Jakub Šimeček Dr. Claire Bernhard Dr. Victor Goncalves Dr. Christine Goze Dr. Frédéric Boschetti Dr. Johannes Notni Prof. Dr. Hans J. Wester Prof. Dr. Franck Denat 《ChemMedChem》2015,10(9):1475-1479
In the past few years, gallium‐68 has demonstrated significant potential as a radioisotope for positron emission tomography (PET), and the optimization of chelators for gallium coordination is a major goal in the development of radiopharmaceuticals. Methylaminotriazacyclononane trimethylphosphinate (MA‐NOTMP), a new C‐functionalized triazacyclononane derivative with phosphinate pendant arms, presents excellent coordination properties for 68Ga (low ligand concentration, labelling at low pH even at room temperature). A “ready‐to‐be‐grafted” bifunctional chelating agent (p‐NCS‐Bz‐MA‐NOTMP) was prepared to allow 68Ga labelling of sensitive biological vectors. Conjugation to a bombesin(7–14) derivative was performed, and preliminary in vitro experiments demonstrated the potential of MA‐NOTMP in the development of radiopharmaceuticals. This new chelator is therefore of major interest for labelling sensitive biomolecules, and further in vivo experiments will soon be performed. 相似文献
13.
Characterization of Early Enzymes Involved in TDP‐Aminodideoxypentose Biosynthesis en Route to Indolocarbazole AT2433 下载免费PDF全文
Dr. Pauline Peltier‐Pain Dr. Shanteri Singh Prof. Jon S. Thorson 《Chembiochem : a European journal of chemical biology》2015,16(15):2141-2146
The characterization of TDP‐α‐d ‐glucose dehydrogenase (AtmS8), TDP‐α‐d ‐glucuronic acid decarboxylase (AtmS9), and TDP‐4‐keto‐α‐d ‐xylose 2,3‐dehydratase (AtmS14), involved in Actinomadura melliaura AT2433 aminodideoxypentose biosynthesis, is reported. This study provides the first biochemical evidence that both deoxypentose and deoxyhexose biosynthetic pathways share common strategies for sugar 2,3‐dehydration/reduction and implicates the sugar nucleotide base specificity of AtmS14 as a potential mechanism for sugar nucleotide commitment to secondary metabolism. In addition, a re‐evaluation of the AtmS9 homologue involved in calicheamicin aminodeoxypentose biosynthesis (CalS9) reveals that CalS9 catalyzes UDP‐4‐keto‐α‐d ‐xylose as the predominant product, rather than UDP‐α‐d ‐xylose as previously reported. Cumulatively, this work provides additional fundamental insights regarding the biosynthesis of novel pentoses attached to complex bacterial secondary metabolites. 相似文献
14.
Pauline Hibon Heinz von Seggern Hsin-Rong Tseng Christoph Leonhard Manuel Hamburger Gaëlle Béalle 《应用聚合物科学杂志》2020,137(29):48895
Interface control remains a top challenge of solution-processed organic light emitting diodes (OLED) stacks since the device performance heavily relies on it. Film stability of an inkjet deposited and crosslinked layer against subsequent exposure to a suitable inkjet printed solvent has been investigated. Impact of processing solvent (solvent used to prepare the polymer layer) on solution-cast thin film properties has already been shown for polymer films. To our knowledge, this study is the first one analyzing thin films stability against solvent exposure using technology relevant materials processed via inkjet printing (IJP). The outcome of this research showed that the stability of the crosslinked films is affected by the solvent used for ink formulation. These findings are of great interest for multilayered semiconductors devices, such as OLEDs, field-effect transistors and dye-sensitized solar cells. Differential scanning calorimetry (DSC) was used to quantify the efficiency of the polymer crosslinking reaction in pure powder and in thin films, as processed from different solvents. Crosslinking efficiency measured by DSC correlated well with the deformation induced by the solvent and observed on layer surfaces. The interaction in solution between polymer and solvent has also been evaluated to explain its impact on thin film stability against successive solvent printing. © 2020 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2020 , 137, 48895. 相似文献
15.
Pauline Glatz Monique Comte Lionel Montagne Bertrand Doumert Fabrice Cousin Laurent Cormier 《Journal of the American Ceramic Society》2020,103(9):4969-4982
Li2O-Al2O3-SiO2 (LAS) glass-ceramics have important industrial applications and bulk nucleation is usually achieved by using nucleating agents. In particular, P2O5 is an efficient agent in glasses containing a low level of Al2O3 but its role in the first stages of nucleation is not well established. In this study, we combine structural investigations from local to mesoscales to describe the structural evolution during crystallization of LAS glass-ceramics. Local environment is probed using 29Si and 31P MAS-NMR, indicating organization of P in poorly crystallized Li3PO4 species prior to any crystallization. To better understand the detailed nanoscale changes of the glass structure, 31P-31P DQ-DRENAR homonuclear correlation experiments have been carried out, revealing the gradual segregation of P atoms associated with the formation of disordered Li3PO4. Small-angle neutron scattering data also show the apparition of nanoscale heterogeneities associated with Li3PO4 species upon heating treatments and allow the determination of their average sizes. These new structural information enhance our understanding of the role of P in nucleation mechanisms. Nucleation is initiated by gradual change in P environment implying P segregation upon heating treatments, forming disordered Li3PO4 heterogeneities. The segregation of P atoms enables the precipitation of meta- and disilicate phases. 相似文献
16.
Sarah Gilgunn Keefe Murphy Henning Stckmann Paul J. Conroy T. Brendan Murphy R. William Watson Richard J. OKennedy Pauline M. Rudd Radka Saldova 《International journal of molecular sciences》2020,21(23)
The diagnosis and treatment of prostate cancer (PCa) is a major health-care concern worldwide. This cancer can manifest itself in many distinct forms and the transition from clinically indolent PCa to the more invasive aggressive form remains poorly understood. It is now universally accepted that glycan expression patterns change with the cellular modifications that accompany the onset of tumorigenesis. The aim of this study was to investigate if differential glycosylation patterns could distinguish between indolent, significant, and aggressive PCa. Whole serum N-glycan profiling was carried out on 117 prostate cancer patients’ serum using our automated, high-throughput analysis platform for glycan-profiling which utilizes ultra-performance liquid chromatography (UPLC) to obtain high resolution separation of N-linked glycans released from the serum glycoproteins. We observed increases in hybrid, oligomannose, and biantennary digalactosylated monosialylated glycans (M5A1G1S1, M8, and A2G2S1), bisecting glycans (A2B, A2(6)BG1) and monoantennary glycans (A1), and decreases in triantennary trigalactosylated trisialylated glycans with and without core fucose (A3G3S3 and FA3G3S3) with PCa progression from indolent through significant and aggressive disease. These changes give us an insight into the disease pathogenesis and identify potential biomarkers for monitoring the PCa progression, however these need further confirmation studies. 相似文献
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18.
Kyriacos Zygourakis Hao Sun Pauline Markenscoff 《American Institute of Chemical Engineers》2013,59(9):3412-3420
The development of a novel nanoscale model that can accurately describe the reactivity of solids consisting of multiple components and having ordered and random pores is presented. Domains of multiple solid phases are distributed on a computational grid to simulate reactants with different specific reactivities and dispersions. Sub‐nanometer slit pores and larger cylindrical pores with given size distributions are also distributed on the grid in regular and random arrangements respectively. The generated solids are then eroded using rules that simulate a gas‐solid, non‐catalytic reaction occurring in the kinetic control regime. A parametric study is first carried out to demonstrate how key pore structural parameters affect the reactivity patterns. Model predictions are found to be in excellent agreement with experimental thermogravimetric data for the combustion of biochars, both when the slit and random cylindrical pores are fully accessible to the reactant and when diffusional limitations appear in the smaller slit pores. © 2013 American Institute of Chemical Engineers AIChE J, 59: 3412–3420, 2013 相似文献
19.
Nina Pauline Holzapfel Boris Michael Holzapfel Simon Champ Jesper Feldthusen Judith Clements Dietmar Werner Hutmacher 《International journal of molecular sciences》2013,14(7):14620-14646
Lycopene is a phytochemical that belongs to a group of pigments known as carotenoids. It is red, lipophilic and naturally occurring in many fruits and vegetables, with tomatoes and tomato-based products containing the highest concentrations of bioavailable lycopene. Several epidemiological studies have linked increased lycopene consumption with decreased prostate cancer risk. These findings are supported by in vitro and in vivo experiments showing that lycopene not only enhances the antioxidant response of prostate cells, but that it is even able to inhibit proliferation, induce apoptosis and decrease the metastatic capacity of prostate cancer cells. However, there is still no clearly proven clinical evidence supporting the use of lycopene in the prevention or treatment of prostate cancer, due to the only limited number of published randomized clinical trials and the varying quality of existing studies. The scope of this article is to discuss the potential impact of lycopene on prostate cancer by giving an overview about its molecular mechanisms and clinical effects. 相似文献
20.
Pauline V. Marck Marco T. Pessoa Yunhui Xu Laura C. Kutz Dominic M. Collins Yanling Yan Cierra King Xiaoliang Wang Qiming Duan Liquan Cai Jeffrey X. Xie Jerry B. Lingrel Zijian Xie Jiang Tian Sandrine V. Pierre 《International journal of molecular sciences》2021,22(7)
The Na/K-ATPase is the specific receptor for cardiotonic steroids (CTS) such as ouabain and digoxin. At pharmacological concentrations used in the treatment of cardiac conditions, CTS inhibit the ion-pumping function of Na/K-ATPase. At much lower concentrations, in the range of those reported for endogenous CTS in the blood, they stimulate hypertrophic growth of cultured cardiac myocytes through initiation of a Na/K-ATPase-mediated and reactive oxygen species (ROS)-dependent signaling. To examine a possible effect of endogenous concentrations of CTS on cardiac structure and function in vivo, we compared mice expressing the naturally resistant Na/K-ATPase α1 and age-matched mice genetically engineered to express a mutated Na/K-ATPase α1 with high affinity for CTS. In this model, total cardiac Na/K-ATPase activity, α1, α2, and β1 protein content remained unchanged, and the cardiac Na/K-ATPase dose–response curve to ouabain shifted to the left as expected. In males aged 3–6 months, increased α1 sensitivity to CTS resulted in a significant increase in cardiac carbonylated protein content, suggesting that ROS production was elevated. A moderate but significant increase of about 15% of the heart-weight-to-tibia-length ratio accompanied by an increase in the myocyte cross-sectional area was detected. Echocardiographic analyses did not reveal any change in cardiac function, and there was no fibrosis or re-expression of the fetal gene program. RNA sequencing analysis indicated that pathways related to energy metabolism were upregulated, while those related to extracellular matrix organization were downregulated. Consistent with a functional role of the latter, an angiotensin-II challenge that triggered fibrosis in the α1r/rα2s/s mouse failed to do so in the α1s/sα2s/s. Taken together, these results are indicative of a link between circulating CTS, Na/K-ATPase α1, ROS, and physiological cardiac hypertrophy in mice under baseline laboratory conditions. 相似文献