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21.
Inhibition of insulin-dependent lipogenesis and anti-lipolysis by protein tyrosine kinase inhibitors. 总被引:4,自引:0,他引:4 下载免费PDF全文
Protein tyrosine kinase (PTK) blockers which competitively inhibit the kinase activity of insulin receptors were synthesized and their properties examined. The best insulin receptor kinase (IRK) inhibitors possess either one hydroxyphenyl ring and two carboxyl groups or two phenyl rings and one carboxyl group. All the inhibitors, except tBoc-tyrosine aminomalonate, effectively block the IRK-catalyzed phosphorylation of exogenous substrate, but only partially block receptor autophosphorylation. These PTK blockers inhibit the insulin induced [14C]glucose assimilation into lipids (lipogenesis), but fail to inhibit the anti-lipolytic effect of the hormone. Only tBocTyr-aminomalonate was found to inhibit all the effects of insulin measured: insulin-stimulated phosphorylation of exogenous substrate, IRK autophosphorylation, insulin-dependent lipogenesis and the insulin-dependent anti-lipolytic effect. This inhibitor is the first blocker which is reported to block insulin-dependent anti-lipolysis. The inhibitors examined are devoid of general adverse effects since they have no effect on insulin-independent lipolysis, on [U14C]fructose assimilation or on (-)isoproterenol-stimulated lipolysis. These studies suggest that insulin-dependent lipogenesis and anti-lipolysis may be mediated by two distinguishable signalling pathways. This study also suggests that PTK inhibitors may become useful tools in the investigation of the signalling pathways of PTKs. 相似文献
22.
Christiane Wloczyk Achim Kröger Thomas Göbel Gabriele Holdt Ralf Steudel 《Archives of microbiology》1989,152(6):600-605
Wolinella succinogenes grown on formate and elemental sulphur was found to use the polysulphide derivatives 2,2-tetrathiobispropionate (R2S4) or pentathionate (S5O
6
=
) as acceptors for formate oxidation. The specific activities of formate oxidation with these acceptors were similar to those with elemental sulphur. The main reaction products of R2S4 reduction were 2,2-dithiobispropionate (R2S2) and sulphide. Pentathionate was converted to thiosulphate and some elemental sulphur. The electrochemical proton potential
across the cytoplasmic membrane of the bacterium was measured in the steady state of electron transport from formate to R2S4. The electrical proportion () of the
determined through the distribution of labeled tetraphenylphosphonium cation was obtained as 0.17 Volt. The was zero, when a protonophore was present. The pH-difference across the membrane was negligible. Thus the
generated by sulphur respiration is close to that measured earlier with fumarate as the terminal acceptor of electron transport.Abbreviations DMO
5,5-dimethyloxazolidine-2,4-dione
- R2Sn (n=2–5)
2,2-polythiobispropionate
- TTFB
4,5,6,7-tetrachloro-2-trifluoromethylbenzimidazol
- TPP
tetraphenylphosphonium cation 相似文献
23.
The immobilization of penicillin G acylase on chitosan 总被引:3,自引:0,他引:3
24.
The rho gene product expressed in E. coli is a substrate of botulinum ADP-ribosyltransferase C3 总被引:14,自引:0,他引:14
K Aktories U Braun S R?sener I Just A Hall 《Biochemical and biophysical research communications》1989,158(1):209-213
The ras-related rho A protein expressed in E. coli, was ADP-ribosylated by botulinum ADP-ribosyltransferase C3. C3 also modified the valine-14 mutant rho protein but not the products of H-ras, R-ras, ral, ypt, and rap 1 genes. A ras-rho chimaera consisting of 60 amino acids from the amino terminus of ras fused to 133 amino acids from the carboxy terminus of rho was not modified by C3. Antibodies raised against the porcine brain cytosolic substrate of C3 cross reacted with the rho, valine-14 rho and ras-rho proteins, but not with the gene products of H-ras, R-ras, ral or rap 1. Polyclonal anti-H-ras antibodies cross reacted with H-ras but not with ral, rho, or the C3 substrate purified from porcine brain. 相似文献
25.
Eckhard Fischer Birgit Strehlow Dieter Hartz Volkmar Braun 《Archives of microbiology》1990,153(4):329-336
After uptake of microbial ferrisiderophores, iron is assumed to be released by reduction. Two ferrisiderophore-reductase activities were identified in Escherichia coli K-12. They differed in cellular location, susceptibility to amytal, and competition between oxygen and ferrichrome-iron(III) reduction. The ferrisiderophore reductase associated with the 40,000×g sediment (membrane-bound enzyme) was inhibited by 10 mM amytal in contrast to the ferrisiderophore reductase present in the 100,000×g supernatant (soluble enzyme). Reduction by the membrane-bound enzyme followed sigmoid kinetics, but was biphasic in the case of the soluble enzyme. The soluble reductase could be assigned to a protein consisting of a single polypeptide of M
r
26000. Reduction of iron(III) by the purified enzyme depended on the addition of NADH or NADPH which were equally active reductants. The cofactor FMN and to a lesser degree FAD stimulated the reaction. Substrate specificity of the soluble reductase was low. In addition to the hydroxamate siderophores arthrobactin, schizokinen, fusigen, aerobactin, ferrichrome, ferrioxamine B, coprogen, and ferrichrome A, the iron(III) complexes of synthetic catecholates, dihydroxy benzoic acid, and dicitrate, as well as carrier-free iron(III) were accepted as substrates. Both ferrisiderophore reductases were not controlled by the fur regulatory system and were not suppressed by anaerobic growth.Abbreviations DHB
dihydroxybenzoic acid
- MECAM
1,3,5-N,N,N-tris-(2,3-dihydroxybenzoyl)-triamino-methylbenzene
- MECAMS
2,3-dihydroxy-5-sulfonyl-derivative of MECAM 相似文献
26.
Ralf Steudel Gabriele Holdt Pieter T. Visscher Hans van Gemerden 《Archives of microbiology》1990,153(5):432-437
Cultures of Chromatium vinosum, devoid of sulfur globules, were supplemented with sulfide and incubated under anoxic conditions in the light. The concentrations of sulfide, polysulfides, thiosulfate, polythionates and elemental sulfur (sulfur rings) were monitored for 3 days by ion-chromatography and reversed-phase HPLC. While sulfide disappeared rapidly, thiosulfate and elemental sulfur (S6, S7 S8 rings) were formed. After sulfide depletion, the concentration of thiosulfate decreased fairly rapidly, but elemental sulfur was oxidized very slowly to sulfate. Neither polysulfides (S
x
2–
), polythionates (SnO
6
2–
, n=4–6), nor other polysulfur compounds could be detected, which is in accordance with the fact that sulfide-grown cells were able to oxidize polysulfide without lag. The nature of the intracellular sulfur globules is discussed. 相似文献
27.
28.
Soils contain two different activities for oxidation of hydrogen 总被引:1,自引:0,他引:1
Abstract Hydrogen oxidation rates were measured in a neutral compost soil and an acidic sandy loam at H2 mixing ratios of 0.01 to 5000 ppmv. The kinetics were biphasic showing two different K m values for H2 , one at about 10–40 nM dissolved H2 , the other at about 1.2–1.4 μM H2 . The low- K m activity was less sensitive to chloroform fumigation than the high- K m activity. If sterile soil was amended with Paracoccus denitrificans or a H2 -oxidizing strain isolated from compost soil, it exhibited only a high- K m (0.7–0.9 μM) activity. It also failed to utilize H2 mixing ratios below a threshold of 1.6–3.0 ppmv H2 (160–300 mPa). A similar result was obtained when fresh soil samples were suspended in water, and H2 oxidation was determined from the decrease of dissolved H2 . However, H2 was again utilized to mixing ratios lower than 0.05 ppmv, if the supernatant of the soil suspension or the settled soil particles were dried onto sterile soil or purified quarz sand. Obviously, soils contain two different activities for oxidation of H2 : (1) a high- K m , high-threshold activity which apparently is due to aerobic H2 -oxidizing bacteria, and (2) a low- K m , low-threshold activity whose origin is unknown but presumably is due to soil enzymes. 相似文献
29.
30.
Sequence of the fhuE outer-membrane receptor gene of Escherichia coli K12 and properties of mutants 总被引:15,自引:0,他引:15
The fhuE gene of Escherichia coli codes for an outer-membrane receptor protein required for the uptake of iron(III) via coprogen, ferrioxamine B and rhodotorulic acid. The amino acid sequence, deduced from the nucleotide sequence, consisted of 729 residues. The mature form, composed of 693 residues, has a calculated molecular weight of 77,453, which agrees with the molecular weight of 76,000 determined by polyacrylamide gel electrophoresis. The FhuE protein contains four regions of homology with other TonB-dependent receptors. A valine to proline exchange in the 'TonB box' abolished transport activity. Phenotypic revertants with substitutions of arginine, glutamine, or leucine at the valine position exhibited increasing iron-coprogen transport rates. Point mutations resulting in the replacement of glycine (127) in the second homology region with either alanine, aspartate, valine, asparagine or histidine exhibited decreased transport rates (listed in descending order). A truncated FhuE protein lacking 24 amino acids at the C-terminal end was exported to the periplasm but failed to be inserted into the outer membrane. 相似文献