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排序方式: 共有78条查询结果,搜索用时 31 毫秒
1.
Alexopoulos T Allen C Anderson EW Areti H Banerjee S Beery PD Biswas NN Bujak A Carmony DD Carter T Cole P Choi Y De Bonte RJ Erwin AR Findeisen C Goshaw AT Gutay LJ Hirsch AS Hojvat C Kenney VP Lindsey CS LoSecco JM McMahon T McManus AP Morgan N Nelson KS Oh SH Piekarz J Porile NT Reeves D Scharenberg RP Stampke SR Stringfellow BC Thompson MA Turkot F Walker WD Wang CH Wesson DK 《Physical review letters》1990,64(9):991-994
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Lazarus EA Navratil GA Greenfield CM Strait EJ Austin ME Burrell KH Casper TA Baker DR DeBoo JC Doyle EJ Durst R Ferron JR Forest CB Gohil P Groebner RJ Heidbrink WW Hong R Houlberg WA Howald AW Hsieh C Hyatt AW Jackson GL Kim J Lao LL Lasnier CJ Leonard AW Lohr J La Haye RJ Maingi R Miller RL Murakami M Osborne TH Perkins LJ Petty CC Rettig CL Rhodes TL Rice BW Sabbagh SA Schissel DP Scoville JT Snider RT Staebler GM Stallard BW Stambaugh RD St John HE Stockdale RE Taylor PL Thomas DM 《Physical review letters》1996,77(13):2714-2717
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Schmidt R Blaich T Elze TW Emling H Freiesleben H Grimm K Henning W Holzmann R Keller JG Klingler H Kulessa R Kratz JV Lambrecht D Lange JS Leifels Y Lubkiewicz E Moore EF Wajda E Prokopowicz W Schütter C Spies H Stelzer K Stroth J Walus W Wollersheim HJ Zinser M Zude E 《Physical review letters》1993,70(12):1767-1770
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Engel CK Pirard B Schimanski S Kirsch R Habermann J Klingler O Schlotte V Weithmann KU Wendt KU 《Chemistry & biology》2005,12(2):181-189
Inhibitors for matrix metalloproteinases (MMPs) are under investigation for the treatment of cancer, arthritis, and cardiovascular disease. Here, we report a class of highly selective MMP-13 inhibitors (pyrimidine dicarboxamides) that exhibit no detectable activity against other MMPs. The high-resolution X-ray structures of three molecules of this series bound to MMP-13 reveal a novel binding mode characterized by the absence of interactions between the inhibitors and the catalytic zinc. The inhibitors bind in the S1' pocket and extend into an additional S1' side pocket, which is unique to MMP-13. We analyze the determinants for selectivity and describe the rational design of improved compounds with low nanomolar affinity. 相似文献
7.
Anton Amadeus Hrmann Elisabeth Plhak Maximilian Klingler Christine Rangger Joachim Pfister Gert Schwach Herbert Kvaternik Elisabeth von Guggenberg 《Molecules (Basel, Switzerland)》2022,27(6)
The new minigastrin analog DOTA-MGS8 targeting the cholecystokinin-2 receptor (CCK2R) used in this study displays the combination of two site-specific modifications within the C-terminal receptor binding sequence together with an additional N-terminal amino acid substitution preventing fast metabolic degradation. Within this study, the preparation of 68Ga-labeled DOTA-MGS8 was validated using an automated synthesis module, describing the specifications and analytical methods for quality control for possible clinical use. In addition, preclinical studies were carried out to characterize the targeting potential. [68Ga]Ga-DOTA-MGS8 showed a high receptor-specific cell internalization into AR42J rat pancreatic cells (~40%) with physiological expression of rat CCK2R as well as A431-CCK2R cells transfected to stably express human CCK2R (~47%). A favorable biodistribution profile was observed in BALB/c nude mice xenografted with A431-CCK2R cells and mock-transfected A431 cells as control. The high tumor uptake of ~27% IA/g together with low background activity and limited uptake in non-target tissue confirms the potential for high-sensitivity positron emission tomography of stabilized MG analogs in patients with MTC and other CCK2R-related malignancies. 相似文献
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Woelk K Zwank BL Trautner P Lehnhof E Bargon J Klingler RJ Gerald RE Rathke JW 《Journal of magnetic resonance (San Diego, Calif. : 1997)》2000,145(2):276-290
A finite-difference approach has been developed for precisely determining diffusion coefficient and T1 relaxation time in fluid samples analyzed by magnetization-grating rotating-frame imaging (MAGROFI) with either a surface coil or a toroid cavity detector (TCD). This approach avoids shortcomings of phenomenologically based approximations, such as neglect of sample geometries with singularities at the confines of the sample volume, and accounts for the diffusive edge enhancement observed in fluid imaging. Error limits are discussed. The new method has been applied to the determination of the self-diffusion coefficient for MAGROFI experiments using TCDs filled with acetone. 相似文献
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Lee Klingler 《代数通讯》2013,41(8):2303-2330