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排序方式: 共有214条查询结果,搜索用时 15 毫秒
211.
Verdoes M Florea BI Menendez-Benito V Maynard CJ Witte MD van der Linden WA van den Nieuwendijk AM Hofmann T Berkers CR van Leeuwen FW Groothuis TA Leeuwenburgh MA Ovaa H Neefjes JJ Filippov DV van der Marel GA Dantuma NP Overkleeft HS 《Chemistry & biology》2006,13(11):1217-1226
The proteasome is an essential evolutionary conserved protease involved in many regulatory systems. Here, we describe the synthesis and characterization of the activity-based, fluorescent, and cell-permeable inhibitor Bodipy TMR-Ahx(3)L(3)VS (MV151), which specifically targets all active subunits of the proteasome and immunoproteasome in living cells, allowing for rapid and sensitive in-gel detection. The inhibition profile of a panel of commonly used proteasome inhibitors could be readily determined by MV151 labeling. Administration of MV151 to mice allowed for in vivo labeling of proteasomes, which correlated with inhibition of proteasomal degradation in the affected tissues. This probe can be used for many applications ranging from clinical profiling of proteasome activity, to biochemical analysis of subunit specificity of inhibitors, and to cell biological analysis of the proteasome function and dynamics in living cells. 相似文献
212.
Martijn de Vries 《Topology and its Applications》2009,156(3):652-657
Let q>1 be a real number and let m=m(q) be the largest integer smaller than q. It is well known that each number can be written as with integer coefficients 0?ci<q. If q is a non-integer, then almost every x∈Jq has continuum many expansions of this form. In this note we consider some properties of the set Uq consisting of numbers x∈Jq having a unique representation of this form. More specifically, we compare the size of the sets Uq and Ur for values q and r satisfying 1<q<r and m(q)=m(r). 相似文献
213.
Daniel Volland Jan Niedens Patrick T. Geppert Dr. Martijn J. Wildervanck Felix Full Prof. Agnieszka Nowak-Król 《Angewandte Chemie (International ed. in English)》2023,62(30):e202304291
We report the concise synthesis and chir(optical) properties of an azaborathia[9]helicene consisting of two thienoazaborole motifs. The key intermediate, a highly congested teraryl with nearly parallel isoquinoline moieties, was generated as a mixture of atropisomers upon fusion of the central thiophene ring of the dithienothiophene moiety. These diastereomers were characterized by single crystal X-ray analysis revealing intriguing interactions in the solid state. Subsequent insertion of boron into the aromatic scaffold via silicon-boron exchange involving triisopropylsilyl groups fixed the helical geometry, thereby establishing a novel method for the preparation of azaboroles. The ligand exchange at boron in the final step afforded the blue emitter displaying a fluorescence quantum yield of 0.17 in CH2Cl2 and excellent configurational stability. Detailed structural and theoretical investigation of unusual atropisomers and the helicene provide insights into their isomerization processes. 相似文献
214.