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911.
Reticulate scales develop as radial symmetrical anlagen, in contrast to scuttate scales which appear initially as “epidermal placodes.” Unlike scuttate scales whose outer and inner epidermal surfaces elaborate β-and α-type keratins, respectively, reticulate scales elaborate only one type of epidermal surface which has been reported to give an α-type, X-ray diffraction pattern. We find that, histologically and ultrastructurally, this surface differs from either epidermal surface of scuttate scales. The keratinizing cells become filled with long interweaving bundles of α-filaments which aggregate into rather homogeneous α-fibrils. Keratohyalin granules, which have been shown to be associated with other keratinizing regions in the bird, do not form during the keratinization of reticulate scale epidermis. 相似文献
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Maurice Manning Ling Ling Cheng Stoytcho Stoev Krzysztof Bankowski Jozef Przybyiski Wieslaw A. Klis Wilbur H. Sawyer Nga Ching Wo W. Y. Chan 《Journal of peptide science》1995,1(1):66-79
We have investigated the effects of mono-substitutions with the conformationally restricted amino acid, 1,2,3,4 tetrahydroisoquinoline-3-carboxylic acid (Tic) at position 3 in arginine vasopressin (AVP), at positions 2, 3 and 7 in potent non-selective cyclic AVP V2/V1a antagonists, in potent and selective cyclic and linear AVP V1a antagonists, in a potent and selective oxytocin antagonist and in a new potent linear oxytocin antagonist Phaa-D -Tyr(Me)-Ile-Val-Asn-Orn-Pro-Orn-NH2 (10). We report here the solid-phase synthesis of peptide 10 together with the following Tic-substituted peptides: 1, [Tic3]AVP; 2, d(CH2)5[D -Tic2]VAVP; 3, d(CH2)5[D -Tyr(Et)2Tic3]VAVP; 4, d(CH2)5[Tic2Ala-NH29]AVP; 5, d(CH2)5[Tyr(Me)2, Tic3, Ala-NH29]AVP; 6, d(CH2)5 [Tyr(Me)2, Tic7]AVP; 7, Phaa-D -Tyr(Me)-Phe-Gln-Asn-Lys-Tic-Arg-NH2; 8, desGly-NH2,d(CH2)5[Tic2,Thr4]OVT; 9, desGly-NH2d(CH2)5[Tyr(Me)2Thr4, Tic7]OVT; 11, Phaa-D-Tic-Ile-Val-Asn-Orn-Pro-Orn-NH2, using previously described methods. The protected precursors were synthesized by the solid-phase method, cleaved, purified and deblocked with sodium in liquid ammonia to give the free peptides 1–11 which were purified by methods previously described. Peptides 1–11 were examined for agonistic and antagonistic potency in oxytocic (in vitro, without Mg2+) and AVP antidiuretic (V2-receptor) and vasopressor (V1a-receptor) assays. Tic3 substitution in AVP led to drastic losses of V2, V1a and oxytocic agonistc activities in peptide 1.L - and D -Tic2 substitutions led to drastic losses of anti-V2/anti-V1a and anti-oxytocic potencies in peptides 2, 4, 8 and 11 (peptide 2 retained substantial anti-oxytocic potency; pA2 = 7.25 ± 0.25). Whereas Tic3 substitution in the selective V1a antagonist d(CH2)5[Tyr(Me)2, Ala-NH29]APV(C) led to a drastic reduction in anti-V1a potency (from anti-V1a pA2) 8.75 to 6.37 for peptide 5, remarkably, Tic3 substitution in the V2/V1a antagonist d(CH2)5[D -Tyr(Et)2]VAVP(B) led to full retention of anti-V2 potency and a 95% reduction in anti-V1a potency. With an anti-V2 pA2 = 7.69 ± 0.05 and anti-V1a pA2 = 6.95 ± 0.03, d(CH2)5[D -Tyr(Et)2,Tic3]VAVP exhibits a 13-fold gain in anti-V2/anti-V1a selectivity compared to (B). Tic7 substitutions are very well tolerated in peptides 6, 7 and 9 with excellent retention of the characteristic potencies of the parent peptides. The findings on the effects of Tic3 substitutions reported here may provide promising leads to the design of more selective and possibly orally active V2 antagonists for use as pharmacological tools and as therapeutic clinical agents for the treatment of the syndrome of the inappropriate secretion of antidiuretic hormone (SIADH). 相似文献
915.
Among the more recently discovered agents of human disease are small, free-living amebae belonging to the generaNaegleria andAcanthamoeba. An overview of the distribution ofAcanthamoeba in recent surveys of the near shore waters of the northeastern United States is presented. There appears to be a particular association between the presence ofAcanthamoeba in marine sediments and the sites of oceanic sludge dumping. Amebae belonging to the genusNaegleria have not been isolated from these marine sediments which routinely yieldedAcanthamoeba. Starch gel electrophoretic analysis of enzymes suggests that some isolates ofAcanthamoeba from oceanic sludge dump-sites are not members of previously recognized pathogenic species. 相似文献
916.
Qi-xuan Wu M.A King G.R Donovan D Alewood P Alewood W.H Sawyer B.A Baldo 《Biochimica et Biophysica Acta (BBA)/General Subjects》1998,1425(1):74-80
The synthetic peptide pilosulin 1, corresponding to the largest defined allergenic polypeptide found in the venom of the jumper ant Myrmecia pilosula, inhibited the incorporation of [methyl-3H]thymidine into proliferating Epstein–Barr transformed (EBV) B-cells. The LD50 was four-fold lower in concentration than melittin, a cytotoxic peptide found in honey bee venom. Loss of cell viability was assessed by flow cytometry by measuring the proportion of cells that fluoresced in the presence of the fluorescent dye 7-aminoactinomycin D. Examination of proliferating EBV B-cells indicated that the cells lost viability within a few minutes exposure to pilosulin 1. Partial peptides of pilosulin 1 were less efficient in causing loss of cell viability and the results suggest that the 22 N-terminal residues are critical to the cytotoxic activity of pilosulin 1. Normal blood white cells were also labile to pilosulin 1. T- and B-lymphocytes, monocytes and natural killer cells, however, were more labile than granulocytes. Analysis of pilosulin 1 using circular dichroism indicated that, in common with melittin and other Hymenoptera venom toxins, it had the potential to adopt an α-helical secondary structure. 相似文献
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Various techniques for generation of peptide and peptidomimetic libraries are summarized in this article. Multipin, tea bag, and split-couple-mix techniques represent the major methods used to make peptides and peptidomimetics libraries. The synthesis of these libraries were made in either discrete or mixture format. Peptides and peptidomimetics combinatorial libraries were screened to discover leads against a variety of targets. These targets, including bacteria, fungus, virus, receptors, and enzymes were used in the screening of the libraries. Discovered leads can be further optimized by combinatorial approaches. 相似文献