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101.
Cameron J. Smith Amjad Ali Liya Chen Milton L. Hammond Matt S. Anderson Ying Chen Suzanne S. Eveland Qiu Guo Sheryl A. Hyland Denise P. Milot Carl P. Sparrow Samuel D. Wright Peter J. Sinclair 《Bioorganic & medicinal chemistry letters》2010,20(1):346-349
A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure–activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC50 of 28 nM. 相似文献
102.
Lu Z Napolitano JB Theberge A Ali A Hammond ML Tan E Tong X Xu SS Latham MJ Peterson LB Anderson MS Eveland SS Guo Q Hyland SA Milot DP Chen Y Sparrow CP Wright SD Sinclair PJ 《Bioorganic & medicinal chemistry letters》2010,20(24):7469-7472
A new class of CETP inhibitors was designed and prepared. These compounds are potent both in vitro and in vivo. The most active compound (12d) has shown an ability to raise HDL significantly in transgenic mouse PD model. 相似文献
103.
Suneth S. Sooriyapathirana Amjad Khan Audrey M. Sebolt Dechun Wang Jill M. Bushakra Kui Lin-Wang Andrew C. Allan Susan E. Gardiner David Chagné Amy F. Iezzoni 《Tree Genetics & Genomes》2010,6(6):821-832
Sweet cherry (Prunus avium L.) skin and fruit colors vary widely due to differences in red and yellow pigment profiles. The two major market classes
of sweet cherry represent the two color extremes, i.e., yellow skin with red blush and yellow flesh and dark mahogany skin
with mahogany flesh. Yet, within these extremes, there is a continuum of skin and flesh color types. The genetic control of
skin and flesh color in sweet cherry was investigated using a quantitative trait locus (QTL) approach with progeny derived
from a cross between cherry parents representing the two color extremes. Skin and flesh colors were measured using a qualitative
color-card rating over three consecutive years and also evaluated quantitatively for darkness/lightness (L*), red/green (a*),
and yellow/blue (b*). Segregations for the color measurements (card, L*, a*, and b*) did not fit normal distributions; instead,
the distributions were skewed towards the color of the dark-fruited parent. A major QTL for skin and flesh color was identified
on linkage group (LG) 3. Two QTLs for skin and flesh color were also identified on LG 6 and LG 8, respectively, indicating
segregation for minor genes. The significance and magnitude of the QTL identified on LG 3 suggests the presence of a major
regulatory gene within this QTL interval. A candidate gene PavMYB10, homologous to apple MdMYB10 and Arabidopsis AtPAP1, is within the interval of the major QTL on LG 3, suggesting that PavMYB10 could be the major determinant of fruit skin and flesh coloration in sweet cherry. 相似文献
104.
Bhojani MS Hamstra DA Chang DC Coppola JM Khan AP Reddy GR Ross BD Rehemtulla A 《Molecular imaging》2006,5(2):129-137
Programmed cell death (apoptosis) is a ubiquitous means utilized by multicellular organisms for elimination of unwanted cells during development and homeostasis. Dysregulated apoptosis is implicated in an array of clinical disorders including cancer, autoimmune diseases, neurodegenerative disorders, and ischemia. During programmed cell death, a series of proteases, known as caspases, with different specificities play crucial roles in the apoptotic process. Caspase-3, a group II cysteine aspartate protease, recognizes and cleaves substrates harboring the amino acid sequence aspartic acid-glutamic acid-valine-aspartic acid (DEVD), and it plays an important role in the terminal phase of apoptosis. Here we report the development of a novel imaging platform for sensing the activation of cellular proteases. A recombinant chimeric protein was constructed, composed of a cell-surface-targeted single-chain antibody (sFv) fused to a Golgi retention signal. The DEVD tetrapeptide sequence was included between the single-chain antibody and the Golgi retention signal as a caspase-3 protease cleavage site. When expressed in cultured cells this fusion protein was localized to Golgi bodies and was not detected on the cell surface. Induction of apoptosis resulted in cleavage of the fusion protein releasing the single-chain antibody from the Golgi retention signal in a caspase-dependent manner. As a result, in cells undergoing apoptosis the single-chain antibody was visualized at the cell surface by immunofluorescence microscopy. The expression of sFv on the surface of cells in a protease-dependent manner provides a unique opportunity for real-time imaging through the use of targeted nanoparticles. This methodology may provide for a multimodal noninvasive real-time imaging of apoptosis and a new opportunity for high-throughput screening of cell-death-modulating therapeutic agents. 相似文献
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Six cases that required soft-tissue replacement in the central midface are presented. The greatest number of flaps were used for large defects in patients with cleft palates who had undergone multiple previous operations. Several were for palatal defects attributable to cocaine abuse, and one was used for lining in a nasal reconstruction. There were no flap losses and, on the basis of these experiences, it is concluded that this is an excellent method for providing soft tissue in these difficult situations. 相似文献
108.
Regulation of the bone-specific osteocalcin gene by p300 requires Runx2/Cbfa1 and the vitamin D3 receptor but not p300 intrinsic histone acetyltransferase activity 下载免费PDF全文
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